MXPA97005234A - Cosmetic compositions anhydration with agents dermatologically acti - Google Patents

Abstract

Novel cosmetic compositions are disclosed which contain local application systems for polar dermatologically active agents. The active agents, for example, skin-reviving alpha-hydroxy acids, are absorbed or adsorbed onto preferably porous carrier particles, with the assistance of a viscous polar solvent such as glycerin, if necessary, and dispersed in a base. anhydrous cosmetics together with a film-forming system. These compositions can be formulated into a variety of different cosmetic products, for example eye shadows, eye treatment bases, and lip treatments, each providing significant immediate cosmetic benefits, and a longer term dermatological activity.

Description

ANHYDRATIC COSMETIC COMPOSITIONS WITH DERMATOLOGICALLY ACTIVE AGENTS TECHNICAL FIELD The present invention relates to cosmetic compositions, including application systems, that provide new ways to apply dermatologically active agents to cosmetically significant areas of the stratum corneum. The compositions of the invention are particularly, but not exclusively, useful as eye enhancers to provide cosmetic benefits to the areas of the eyes, such as the eyelids, areas under the eyes, and the edge or outer corner of the eye. , and they are also useful for the cosmetic treatment of the lips and other local areas. The invention includes novel film forming systems to help apply the active ingredient. These film forming systems provide complementary improvements, and are useful regardless of the application system.

BACKGROUND The eyes themselves are the focus of any person's identity and personality, as well as a focal point of attention for others. In any face-to-face encounter, the eyes provide a powerful means of communication not spoken. The appearance of the eyelids and facial areas around the eyes is critical to the appearance of the eyes, and therefore, to the impression that one person receives from another. In accordance with the foregoing, the compositions for the treatment of the eyes comprise an important segment of the cosmetic industry. The eyes are cosmetically a sensitive area and sometimes difficult to treat. They are subject to congenital defects, deficiencies and disorders, and the appearance of the eye areas can deteriorate rapidly due to aging, the effects of weather, diet, and so on. A quality cosmetic treatment of the eye areas can provide great visual and psychological benefits to an individual, making amazing improvements in their appearance. Some common problems of the eye area include wrinkles, cracking, fine lines, blemishes and discoloration. These problems can damage the upper and lower eyelids, particularly the area under the eye, and also the corners of the eye, especially the external noxious corner such as "the ridge", which are likely to form cracks and lines, often referenced in a way little elegant, like "crow's feet". In response to these problems, the cosmetics industry has offered a wide range of remedies to hide, fill, color, or otherwise modulate the appearance of unattractive areas of the eyes. Mascara, eyeliners, and other eyelash treatments are used to improve and define the appearance of the eyelashes, eyebrows and eyelid edges, and can have a beneficial and sometimes theatrical impact on the eyes. a whole. More significant for the purposes of the present invention, are the cosmetics used for the treatment of larger skin areas in the vicinity of the eye, notably the eyelids, the area under the eye, and the areas of the outer corner of the eye. These cosmetics are eye shadows, eye creams, and eyeliners. Although general-purpose cosmetics such as foundation and make-up may be used in the eye area, caution is needed because of the risk of contaminating the eye with allergenic or spicy allergenic ingredients, or the induction of bacterial swelling or infection. There is a wide range of cosmetics for the treatment of the eyes available in any cosmetics store, and the patent literature is replete with hundreds, if not thousands, of propositions and solutions for the different problems that arise when providing a level desired improvement of the eye area. See, for example, Market, U.S. Patent Number 4,783,333, and Giezendanner, U.S. Patent Number 5, 073,364, the descriptions of which are incorporated herein by reference. However, at the date of this application, none of these proportions and solutions provides a treatment of the cosmetic eye area completely satisfactory to many users. Existing eye shadows usually begin to fade within a few hours of application, may develop different cracks in susceptible complexions, and can easily be subject to water damage from tears, rain, sweat, or the like. The eyeshadow bases can alleviate these problems, but they do not provide structural dermatological benefits. A cosmetic for eyes may be difficult to apply in a smooth or even manner, and may have an unpleasant or sticky feeling, or poor film forming abilities (being difficult to spread), or have a high drag or may be difficult to remove. Few eye cosmetics provide long-term structural dermatological improvements, with the exception of eye creams and moisturizers for special purposes that contain skin-revitalizing ingredients. In general, these eye creams are intended to be used at night, and will not stop eye shadow in a satisfactory manner, so that they can not be used for use at the normal time of day, because they do not provide significant improvement in appearance. Theoretically, it would be desirable to avoid separate application steps for cosmetically effective and dermatologically active ingredients, by directly incorporating a dermatologically active ingredient into a cosmetic eye composition. However, there are difficulties. The term "dermatologically active" is used herein to describe materials that act on the skin to provide long-term improvement of one kind or another, with an improvement lasting or starting after the cosmetic makeup is removed. Therefore, the dermatological activity must be distinguished from the cosmetic properties that are only effective while the cosmetic is present on the skin. There are many chemical compounds that have a profound physiological effect on the skin. A group of these dermatologically active compounds is that of alpha-hydroxy-carbolic acids of a relatively low molecular weight, for example with 10 carbon atoms or less. Popularly called "alpha-hydroxy-acids", it is known that these acids have a number of useful effects on the skin. Referenced as "AHA" in the present, which is a common abbreviation in both the popular press and the technical literature, alpha-hydroxy-acids can moisten dry skin and improve different disorders, including acne and psoriasis, and other skin abnormalities. AHAs are also effective in revitalizing the skin. Depending on the concentration and the duration of application, they can cause, or stimulate, the exfoliation, which is the removal of layers of external keratinous or callus tissue, and stimulate the renewal of new skin layers to provide a significant improvement in the appearance of the skin Some AHAs that have been used to provide these benefits are the simplest alpha-hydroxy acid, ie, glycolic acid, as well as lactic acid, citric acid, and malic acid. These acids are also known as "fruit acids", because they are found in fruit, and in the case of glycolic acid, in sugar cane. There are many other AHA, or alpha-keto-acid equivalents and the like, which are known, or which have been suggested to be used in the revitalization of the skin, or which otherwise provide useful dermatological skin functions. Some beta-hydroxy acids, for example, salicylic acid, also have useful dermatological properties. Some of these "skin acids" are disclosed in Yu et al., U.S. Patent No. 5,091,171, the disclosure of which is incorporated herein by reference. Although the poor cosmetic condition of the eye areas of many individuals suggests that these areas are a primary objective for the use of these beneficial dermatological agents such as AHA, there are problems in the use of AHA in the eye area. The AHAs of interest are usually very hydrophilic, they dissolve easily in water, and in the case of lactic acid, they become liquids around room temperature (approximately 16.8 ° C). This hydrophilicity is normally incompatible with cosmetics for men. Common hydrophobic eyes, such as eye shadows, or eye bases. The anhydrous nature of these eye cosmetics means that small amounts of active hydrophilic agents, for example AHA, may lose their activity due to the chemical or physicochemical combination, or fail to apply to the surface of the skin in an adequately hydrophilic environment or watery, to be effective. In addition, the preferred environments for these agents are significantly acidic, a condition that is difficult to provide on skin surfaces treated with anhydrous cosmetics, or substantially hydrophobic. A critical problem with any cosmetic for the eyes, is to avoid irritation, or the stimulation of allergic or pathogenic reactions in the eye. AHAs can be very acidic, and are known to be significantly irritating, even when applied to durable areas of the skin. Avoidance of irritation is of special significance for products intended for daily use, in the eye or in other areas of sensitive skin. One way to apply dermatologically or cosmetically active agents in a cosmetic vehicle is by containing the active agents in or on a suitable particulate carrier. They are of particular interest to be used as a carrier, small particles or porous polymer microspheres. A problem with this approach is that having employed an affinity between a medium containing the active agent and the microsphere to cause the active agent to charge in the microsphere, then it is necessary to overcome this affinity to release the active agent. It is also important that the application vehicle does not possess a higher affinity for the dermatologically active agent than the vehicle, or else the active agent may prematurely discharge from the porous vehicle into the vehicle, and may be dissipated. Schaefer et al., U.S. Patent No. 5,292,512, discloses a cosmetic composition for local application, wherein dermatologically active agents, such as acne treatments, for example retinoids and benzoyl peroxide, hormones, antifungals, antibiotics. , etc., are absorbed onto vehicle particles to be applied to the skin. Typical carrier particles are organic polymeric microspheres. The active products are introduced into the microspheres by dissolving them in a suitable solvent such as water, glycerol, or the like (column 4, lines 47-54). The goal of Schaefer et al. Is to apply the active products in the sebaceous follicles to be released under the epidermis. For this purpose, Schaefer et al. Employ rather small microspheres, of which 80 percent have a diameter between 3 microns and 10 microns, which is apparently an appropriate size for them to travel to the follicles through the epidermis. (See column 1, line 45 to column 2, line 40). Schaefer et al. Does not provide an element for application of the dermatologically active agents to the outer surface of the stratum corneum, nor an element for the controlled release of the active agents, especially the hydrophilic active agents, from an anhydrous cosmetic composition on that surface. Schaefer and colleagues provide subdermal penetration, and not a superficial release. The charged microspheres of Schaefer et al. Are formulated in different hydrophilic or hydrophobic gel compositions, and are reported to provide excellent anti-acne properties, presumably due to the penetration of the vehicle particles loaded with active ingredient into the sebaceous follicles. The compositions of Schaefer et al. Are clearly intended as single-purpose preparations, providing a better application of a specified active agent, and lacking independent cosmetic benefits. If the user wants to obtain additional cosmetic benefits to the treatment of acne or other therapeutic treatments, it will be necessary to apply a separate cosmetic preparation, whose cosmetic can be incompatible with the treatment of acne. Schaefer et al. Do not try to incorporate microspheres loaded with active agent in a cosmetic base, or solve the problems that may arise when doing so. More specifically, Schaefer et al. Do not solve the problem of applying a hydrophilic active agent to the surface of the skin from a cosmetic composition that includes an anhydrous base, whose base provides its own useful cosmetic properties independently of, or additionally a, the cosmetic properties associated with the application of the active agent.

COMPENDIUM OF THE INVENTION The invention, as claimed, is intended to provide a remedy. It solves the problem of how to apply a dermatologically active hydrophilic agent to the eye and to other areas of the surface of sensitive skin, in an essentially hydrophobic cosmetic composition. To solve these problems, the invention provides a cosmetic composition wherein a dermatologically active hydrophilic agent constituted in a liquid hydrophilic medium is adsorbed or absorbed in or on a suitable particulate carrier. This active agent system with vehicle can be incorporated into a substantially anhydrous cosmetic base, for example a suspension of cream. The anhydrous base preferably comprises one or more film-forming agents to provide a novel cosmetic composition that can be applied locally to deliver the hydrophilic agent to the skin. Preferred embodiments of the invention provide solutions to the problem of providing a useful cosmetic composition containing an effective concentration of a dermatologically active agent that can provide a controlled release of the dermatologically active agent to the skin. The cosmetic compositions according to the invention can be formulated in a wide range of cosmetic products, for example, pigmented eye shadows, leftover bases for non-pigmented eyes, lipsticks, moisturizers, lip treatments, bottoms, and the like. These new cosmetic products, in addition to having valuable cosmetic properties, have a dermatological activity, and provide lasting benefits. Accordingly, for example, an eye shadow can be formulated with a skin revitalizing agent, for example an alpha-hydroxy acid, to provide both immediate and long-term improvements to the eyelids. The tests and studies reported hereinafter, show that these cosmetic compositions containing dermatologically active agents loaded onto microspheres, for example AHA, according to the invention, can effectively apply the AHAs to the skin in an active, outward form. of a substantially anhydrous vehicle in which a film forming agent or system is dispersed. The data reported herein shows that the AHAs incorporated in the compositions of the invention are effectively applied to the skin, and provide valuable dermatological benefits, for example skin revitalization, as evidenced by a substantial increase in wetting after four or more weeks of use. Surprisingly, it has been discovered that dermatologically active agents are released or successful from the microsphere carrier vehicle despite the strange hydrophobic environment of the cream or gelled vehicle where they were formulated for testing. The hydrophobicity of the vehicle should tend to inhibit the egress of the hydrophilic active medium from the microsphere. Although we are not forced by any particular theory, it is a concept of the invention that the extension and massage actions that normally accompany the local application of the product, act to put the microspheres loaded with AHA in contact with the skin, where the Skin moisture directs the hydrophilic medium containing AHA out of the microspheres. When the cosmetic compositions of the invention are applied to particular areas of the skin, such as around the eyes and on the lips, they are subject to a constant kneading action as the eyelids flicker and the lips move or clean, providing a continuous change of the microspheres that make contact with the surface of the skin, and a filling of the hydrophilic medium containing AHA supplied to that surface. Furthermore, according to the theory, it seems that the film-forming nature of the anhydrous base produces a barrier to the loss of water on the surface of the skin., inhibiting the transpiration of water from the skin. This control of water loss makes it possible for the upper skin level to increase its water content, thus promoting the release of the dermatologically active agent from the vehicle to the skin. Additionally, any water or other solvent suitable for the dermatologically active agent that is introduced by the subsequent application of a secondary cosmetic product using the composition of the invention as a base, can also assist in the egress of the active agent from the vehicle to the skin. The organic polymeric microsphere tends to be skid and not to adhere to the skin. Strong adhesive properties can be provided to the microspheres by incorporating them into anhydrous cosmetic compositions containing suitable film-forming agents, including novel film-forming systems according to the invention. When this film system is used in microspheres containing cosmetic compositions, a good anhydrous film can be obtained with an excellent possibility of extension and no stickiness or entrainment. Other valuable cosmetic properties can be obtained with the compositions of the invention. The fine lines of the skin can be masked or concealed cosmetically, by means of a filling action and light diffusion of the microspheres, while they are also dermatologically reduced by an action of revitalization of the skin of the AHA.

Preferred formulations can also diffuse light to reduce the appearance of dark circles under the eyes, and provide a soft focus effect. Preferred embodiments of the invention can also improve the water barrier properties of the skin surfaces in which they are applied, potentially promoting the action of dermatologically active hydrophilic agents applied through the cosmetic, and increasing the durability of applied cosmetics. on the product of the invention. Many of the above properties can be combined into a single, multi-functional cosmetic composition that provides both immediate and long-term benefits to consumers.

DETAILED DESCRIPTION OF THE PREFERRED MODALITIES Some embodiments of the invention, and one or more ways of practicing the invention, including the best mode contemplated by the inventor for carrying out the invention, will now be described in greater detail. Some illustrative, non-limiting examples of the preferred embodiments of the invention will also be described. Preferred embodiments of the invention relate to novel cosmetic compositions containing an effective amount of a polar dermatologically active agent, a sufficient amount of adsorbent or absorbent vehicle suitable to support the dermatologically active agent, and one or more film-forming agents in a substantially anhydrous vehicle or base formulated to apply the dermatologically active agent to the surface of the stratum corneum. This composition provides properties that make it possible for a user to enjoy his usual attractive, cosmetically-assisted appearance, while at the same time earning one or more dermatological benefits that will last after removing the cosmetic. The essentially or substantially anhydrous base provides a means or vehicle for dispersing the carrier particles charged with active agent, which medium can be liquid or semi-solid, for example, a dispersant or solvent for other cosmetic ingredients that cause desired cosmetic properties to the composition. The anhydrous base, therefore, may comprise a more or less volatile hydrophobic cosmetic solvent, wherein optionally a gelling agent is dispersed to provide a desired consistency.

Absorbing vehicle According to the invention, a variety of materials can be used as a vehicle to apply a dermatologically active ingredient or agent, for example an alpha-hydroxy acid to the skin, in an active agent form, while protecting the active from other cosmetic ingredients that can deactivate it. Suitable carrier materials include, but are not limited to, organic polymeric microspheres and inorganic particles. Some commercially available microspherical powders useful in the preparation of the cosmetic materials of this invention include organic polymeric materials, for example, polyethylene, polypropylene and copolymers thereof, polyurethane, polyesters, polyamides, polymethyl methacrylate, nylon, ethylene-acrylate copolymers and polyvinylidene copolymers. Any substantially non-toxic, non-irritating, cosmetically compatible organic polymeric material that can be provided in a satisfactorily adsorptive or absorbent form for the purposes of this invention and compatible with the anhydrous carrier can be used. Some examples of inorganic particles include talcs, clays, modified organic clays, kaolin, mica, calcium salicylate, and different carbonates of different metals, for example calcium and magnesium. The vehicle particles should not be too large, or their presence as a component of the composition will be apparent to the user, and may give a feeling of coarse or gritty particles, rather than a soft feeling, to the cosmetic. Therefore, at least 80 percent of the particles should not exceed 50, and preferably should not exceed 20 microns. Neither the particles should be too small, or they can be absorbed into the sebaceous follicles, which is not desired, and will provide too small a storage volume for the dermatologically active passenger agent. Within the limits of providing a satisfactorily cosmetic sensation upon spreading, the vehicle particles must be relatively large in order to be able to release the active ingredient passenger from the surface or through the surface openings from the internal volumes of the particles. Preferably, at least 80 percent of the particles of vehicles are larger than 10 microns in diameter. A particularly preferred range for at least 80 percent of the particles is 10 to 20 microns, more preferably 10 to 15 microns. A useful average particle size is 12 to 20 microns. A porous vehicle particle is particularly preferred where a liquid phase can be absorbed inside the particle, to occupy, for example 10 to 90 percent of the particle's volume, instead of simply being retained on the surface of the particle . An absorbent matrix powder that serves as a vehicle for local application of the dermatologically active agent or the dermatologically active solution may comprise porous synthetic organic polymer microspheres, for example a cosmetically acceptable polyamide, such as nylon 12, in a ratio of about 0.1 to about 40.0 percent, preferably from about 5.0 to about 20.0 percent, and more preferably from about 6.5 to about 10.0 percent by weight of the cosmetic composition. In addition to carrying the AHAs, or other dermatologically active hydrophilic agents, the organic polymeric microspheres impart desirable feeling properties, for example creamy, powdery, and silky qualities, to the consumer formulations, and improve the light scattering qualities of the formulation. When the AHAs or other dermatologically active agents are discharged, the organic polymeric microspheres are available to absorb skin oils, helping to control the breakdown of the oil.

Dermatologically active agents. Examples of suitable dermatologically active agents, which can be applied to the skin by the compositions of the invention, include, but are not limited to, the following. anesthetics, for example, benzyl alcohol, lidocaine and menthol; astringents, for example, scotch elm, benzoic acid, and aluminum or aluminum / zirconium salts; keratolytics, for example resorcinol, salicylic acid, ascorbic acid, and acetic acid; exfoliants, for example lactic acid, glycolic acid, and other alpha- or beta-hydroxy acids; vasoconstrictors, for example, phenylepinephrine hydrochloride, external analgesics, for example tripelenamine and camphor hydrochloride, anti-inflammatory agents, for example salts of glycyrrhizic acid, alpha-bisabolol; salicylate and ibuprofen derivatives, anti-irritants, for example allantoin, proteins, trimethylglycine, glycine, ascorbic acid, ferulic acid, sodium lactate; bleaching agents, for example magnesium ascorbic phosphate, hydrogen peroxide, kojic acid, and hydroquinone; lipolytic agents, for example caffeine, aminophylline, and other xanthine bases; pigment enhancers, for example dihydroxyacetone, • sunscreens, for example diethylamine amine parametoxycinnamate, glyceryl aminobenzoate, 2-hydroxy-4-methoxy-benzophenone-5-sulfonic acid, 2-phenylbenzimidazole sulfonic acid; humectants, for example panthenol, trimon lactamiopropyl chloride, salts of pyrrolidonecarboxylic acid, and polyethylene glycol, with molecular weights of from about 40 to about 10,000 Daltons, copolymers of propylene glycol / ethylene glycol, glycerin, polyglyceryl polymers, mono- , di-, tri-, or poly-saccharides, or mono-, di-, tri-, or reduced poly-saccharides or their derivatives, propylene glycol, polypropylene glycol with molecular weights of about 100 to about 10,000 daltons, hygroscopic amino acids , peptides and polypeptides or their derivatives, glucosaminoglycans, amides or esters of alpha- or beta-hydroxy-acids, ethoxylated derivatives of glycerin, propylene glycol, butanol or pentanoi, inositol, and choline chloride; nutrients, for example vitamin C, vitamin B, folic acid, and minerals, for example calcium, magnesium, iron, zinc, manganese, selenium, and phosphorus. The equivalents for the above examples and other guidelines herein, will suggest other dermatologically active agents suitable for inclusion in the compositions of the invention. Some of these agents are mentioned in the OTC Monographs, and in the Physician's Desk Reference, which are included herein as a reference. Some of these agents, and others, are described in Schaefer et al., U.S. Patent No. 5,292,512, the disclosure of which is also incorporated herein by reference. As discussed above, the cosmetic application system of Schaefer et al. Is very different from that of the present invention. Schaefer et al. Employ ultra-microscopic vehicle particles, small enough to enter the instructions or openings of the skin, to apply the charged particles with the active agents subcutaneously in the sebaceous or follicular openings of the skin. The vehicle particles of Schaefer et al. Are necessarily less than 10 microns in diameter, in order to be transported in the sebaceous follicular openings, for subcutaneous and systemic application. Since the active material is to be absorbed onto or absorbed into a particulate vehicle, which in turn is dispersed in a substantially anhydrous cosmetic base or vehicle, it is preferred that the dermatologically active agent or ingredient be polar, and have little or no affinity for the components of the essentially anhydrous base. One or more dermatologically active agents may be incorporated, in a range from about 0.01 to about 10.0 weight percent of the composition, in the preferred embodiments of the present composition. More preferably, these agents can be added from about 0.5 to about 8.0 percent, and still more preferably from about 1.0 to about 5.0 percent. Other active agents can be used in equivalent proportions, depending on their activity; however, proportions are preferred in the sensitive area of the eye. The preferred dermatologically active agents are the kinds of exfoliants known as alpha- and beta-hydroxy acids, respectively. These materials can be used both to moisturize and revitalize the skin, resulting in better structural and visual qualities. These benefits can only begin to be seen after a long-term use of the cosmetic composition of the invention, on a regular basis, for example daily, for a period from days to weeks, for example, beginning at fourteen or twenty-one days, and continuing up to three to six months of daily or twice daily applications, or even continuing indefinitely. For this purpose, the novel substantially anhydrous cosmetic eye or lip composition of this embodiment of the invention contains, as the dermatologically active hydrophilic agent, at least one alpha-hydroxy acid ("AHA" herein), for example lactic acid, citric acid, malic acid, mixed fruit acids or mixtures thereof, supported on a matrix, or in a vehicle in porous particles. The AHA is preferably supported on the carrier particles, to be present in the surface pores of the vehicle particles, and also in the internal pores communicating with those surface pores, whereby, the hydrophilic medium carrying AHA can be released on the surface of the particle, and removed from the vehicle particle by the moisture of the skin, possibly by capillary action. Some other alpha-hydroxy acids that can be used in the practice of this invention, include a straight or branched chain aliphatic acid, with no more than three substituents on the aliphatic base structure, these non-basic substituents being, and being selected from from the group consisting of hydroxy, aldehyde, keto, carboxyl, chlorine and nitro. Acidity and solubility in water or hydroalcoholic are desirable characteristics of the alpha-hydroxy acids used in the present invention. Some preferred alpha-hydroxy acids contain at least one hydrophobic moiety which is a carbon atom having four substantially non-polar bonds, for example carbon-carbon or carbon-hydrogen bonds. This hydrophobicity is believed to be useful for balancing the hydroxy and carboxyl-electronegative radicals, for better biological compatibility and efficiency. Some other aliphatic alpha-hydroxy acids are preferably monocarboxylic acids selected from the group consisting of normal 2-hydroxy-butanoic acids, 2-hydroxy-isobutanoic acid, normal 2-hydroxy-pentanoic acid, 2-hydroxy-isopentanoic acid , normal 2-hydroxy-hexanoic acid, 2-hydroxy-isohexanoic acid. Di- or polyhydric analogues thereof can also be used, for example, 2, X-dihydroxy analogues thereof, wherein "X" is an integer from 3 to 6, as appropriate for the respective monohydroxy acid. , indicating the location of the carbon atom of a second hydroxyl substituent on a carbon atom different from the number of one or two carbon atoms. Preferably, these dihydroxy acids balance the additional electronegativity that can be attributed to the second hydroxyl with an additional hydrophobic fraction as described above. Although some dermatologically active agents possess properties, for example, a sufficiently low melting point, which makes it possible for them to be absorbed or adsorbed directly in or on the vehicle matrix, others are in crystalline form at room temperature, and are preferably dissolved in a suitable hydrophilic solvent system for the active agent. Preferably, also the solvent system should have little or no affinity for the essentially anhydrous base. This is important to retain both the solvent and its dermatologically active solute in or on the vehicle, and to preserve the intended functionality of the dermatologically active agent. Additionally, the solvent must be suitably viscous to further assist in retarding the migration of the dermatologically active agent from the vehicle. Also, the solvent must be inert or inactive with respect to, or at least should not adversely impact the functionality of the dermatologically active agent.

Hydrophilic solvents. Some kinds of liquid hydrophilic solvents or dispersed phase media that can be used alone or in combinations as auxiliaries to assist in loading the dermatologically active agent or agents on or into the particular vehicle, include, but are not limited to, water, alcohols , and ethers. A suitable class of alcohols comprises mono-, di-, tri-, or polyhydroxy alcohols having the formula: (OH) R - (CH)? - (C) - (CH2) Z - R1 | | (OH) (OH) wherein R = H, CH 3, or a saturated, unsaturated, cyclic or branched alkyl radical containing 1 to 20 carbon atoms X = 0 to 1,000,000; Y = from 0 to 100; Z = from 0 to 10; Y R1 = H, CH3, 0-CH3, 0-CH2-CH3 Suitable examples of these compounds include glycerin, propylene glycol, dipropylene glycol, propanol, isopropanol, butanol, isobutanol, pentanoi, isopentanol, neopentanol, diglycerol, polyglycerol, sorbitol, polyethylene glycerol, and polyol. Suitable ethers include unsubstituted and substituted ethers, for example Fluid UCON (registered trademark), Union Carbide Corp., or fluids DOWANOL (registered trademark), Dow Chemical Company, or solvents CARBITOL (registered trademark) and CELLOSOLVE (trademark) registered) of Union Carbide. In principle, suitable viscous hydrophilic solvents, or mixtures of solvents, can be used with the dermatologically active agent in a proportion of about 99 parts: 1 part to about 1 part: 99 parts. However, the preferred proportions are selected to exploit the physical or physicochemical characteristics of the solvent, to deliver to the dermatologically active agent, an active form in a liquid phase to be recovered by absorbent carrier particles. For this purpose, although in some circumstances a lower proportion of solvent may have merit, higher properties of the solvent are preferred, for example a ratio of about 1: 1 to about 1:20 parts of agent to solvent, on a weight basis . Although these proportions may be effective for intercellularly active agents, the more potent intracellular agents, for example, hydrophilic or water soluble hormones, such as corticosteroids, may be present in smaller relative proportions, eg, from about 1:99 to 1:20 parts of the agent to the solvent. A preferred solvent for a dermatologically active agent, for example, an alpha-hydroxy acid (AHA) is glycerin. The viscosity of the solvent helps retain the AHA in or on the particulate vehicle, while the hydrophilicity allows skin moisture to direct the dissolved AHA out of the microparticle.

Film forming agents. Preferably, the invention provides a film-forming agent to aid in the adhesion of the vehicle to charged particles on the skin, and to help form an occlusion barrier, to improve the accumulation of water on or near the surface of the skin. . Film former means that an essentially continuous layer of the product is formed on the surface of the skin. Occlusion means that a barrier is placed on the surface of the skin, whose barrier substantially blocks or retards the loss of volatile materials from the surface of the skin, and makes it possible for them to accumulate in the upper layers of the skin. For the purpose of this invention, the barrier film is preferably hydrophobic. Some kinds of suitable cosmetic film forming agents that can be used alone or in combination include, but are not limited to, metal soaps, waxes, and film-forming emollients. Some non-limiting examples of each of these kinds of cosmetic film forming agents will now be described. Others will be known by experts in this field. Metal soaps are useful materials that work to help adhesion, and to promote the formation of a hydrophobic film. The metal soap gelling agent or agents can be an alkaline earth or an aluminum alkanoate of 6 to 20 carbon atoms, for example, the salts of laurate, oleate, or calcium, magnesium, zinc, aluminum, or lithium stearate , or mixtures thereof. A cosmetic metal soap, for example, zinc laurate, can be used in a ratio of about 1.0 to about 5.0 percent, preferably about 3.0 percent by weight of the composition. The metallic soap works as an ionic gelling agent to aid adhesion, and is added to the formation of hydrophobic film. Other useful film-forming agents are waxes. Many waxes that can function as suitable film-forming agents in the compositions of the present invention are known in the cosmetic art. Typically, these materials are composed of the formula RX, wherein R is a cyclic or branched chain alkyl chain, long chain, saturated, or unsaturated, from 8 to 1,000,000 carbon atoms, X is -H, -OR1 or -C-OR11, wherein R is H, or a cyclic or branched, saturated or unsaturated chain alkyl radical of 1 to 24 carbon atoms; R is H or a residue of a mono-, di-, tri-, or poly-hydroxy compound capable of forming a mono-, di-, tri-, or poly-ester. Preferred waxes have melting points that exceed 38 ° C. Materials such as esters of glyceryl wax, beeswax, ceresin wax, carnauba wax, candelilla wax, and other cosmetically acceptable waxes can be used. A total wax content of 0 to 10.0 percent is suitable for formulating satisfactory cosmetics according to the invention. Preferably, the total wax content does not exceed 5.0 percent, and more preferably does not exceed 3.0 percent. Suitable waxes are, for example, glyceryl tribehenate, ceresin wax, and microcrystalline wax used in proportions from about 0.00 to about 5.00 percent, preferably from about 0.1 to 1.5 percent. More preferably about 0.25 to 0.5 percent of waxes, such as glyceryl tribehenate, and a slightly higher proportion of about 1 to 2 percent of a ceresin wax are used. The low wax content that can be obtained with the cosmetic compositions according to the invention, has the advantage of providing a low drag and a better possibility of removal. The useful functions of the wax are adhesion, which imparts a creamy feel to the product, film formation, and viscosity increase. Other useful film-forming agents are emollients. These materials are usually liquid at temperatures between 0 ° C and 38 ° C. Emollients are useful in the present invention include those with the following formula CnH (2n + 2-?) < wherein n is an integer from 6 to more than 1 million, and x is 0 or an even integer no greater than n, and may include saturated, unsaturated, branched, and cyclic hydrocarbon chains. Examples include: mineral oil, petrolatum, fluids PERMETHYL (registered trademark), and polybutylenes. Other useful film-forming emollients include mono-, di-, tri-, or poly-branched, -cyclic, -saturated, or -unsaturated alkyl esters or ethers, of di-, tri-, or poly-hydroxy compounds, for example ethylene glycol, propylene glycol, glycerin, sorbitol, or polyol. Examples of these emollients include, but are not limited to, vegetable oils, for example soybean oil, babassu oil, castor oil, cottonseed oil, Chinese tallow oil, crambe oil, oil perilla, oil of Danish rape seed, brown rice oil, palm oil, palm kernel oil, olive oil, linseed oil, coconut oil, sunflower oil, saffron oil, peanut oil, and corn oil. Preferred saturated and unsaturated vegetable oils are those having fatty acid components with 6 to 24 carbon atoms. Additional suitable emollient film forming agents include the esters of the formula: Ri-C-OR? or Ri-O-C- (CH) n-C-0-R9 I II II 0 0 0 wherein Rt and R2 are saturated, unsaturated branched, or cyclic alkyl radicals of 2 to 24 carbon atoms, and n is an integer from 0 to about 20.

Auxiliary film forming agents based on silicone. The novel cosmetic compositions of the invention may also contain a silicone material to provide some measure of auxiliary film-forming ability. Suitable silicone materials are preferably insoluble in water, and are cyclomethicone, polyalkylsiloxanes, polyarylsiloxanes, polyalkylaryl siloxanes, polysiloxane gums, amino-functional polysiloxanes, and polyethersiloxane copolymers. The teachings directed to additional suitable silicone materials can be found in U.S. Patent Nos. U.S. 4,788,006; U.S. 4,341,799; 4,152,416; 3,964,500; 3,208,911; 4,364,837 and U.S. 4,465,619, the disclosures of which are incorporated herein by reference.

Auxiliary film forming agents of polyalkylene oxide. Another class of suitable auxiliary film forming agents comprises substances formed by the polymerization of alkylene oxide monomers of the formula: O / \ H (CH2) n - HC - CH2 wherein n is an integer from 0 to about 3. These materials may be a homogeneous polymer or a copolymer of 2 or more monomers. Examples of the homogeneous polymers include polypropylene oxide and polybutylene oxide. Typically, the molecular weights of these materials are between 100 and 10,000 Daltons. Additionally, these materials can be condensed with a mono- or poly-hydroxyalkyl alcohol, as exemplified by the UCON fluids (registered trademark) of Union Carbide Corp. The film forming agent can be used alone or in combination with other forming agents of film, to achieve the desired aesthetic properties in the final preparation. A preferred range of film-forming agents is from 1 to 99 percent, more preferably from about 1 to 50 percent by weight of the composition. Suitable non-hardening film formers, for example, dimethicone, may be used in proportions of about 0.5 to about 5.0 percent, preferably about 0.6 to 1.5 percent, and more preferably about 1.0 percent. Preferred functions include film formation, skin protection, or water barrier forming agent, lubricating and silky emollient. Film-improving agents can be used, for example, mica treated with aluminum myristate, in a ratio of about 4.0 to about 20.0 percent by weight of the composition, preferably from about 5.0 to 8.0 percent, and more preferably 6.5 percent. Preferred functions of the film improver include adhesion to the skin, imparting a creamy and silky feel to the composition, and improvement of hydrophobic film formation. Although strong adhesive properties can be introduced into the anhydrous cosmetic compositions by the incorporation of waxy film-forming agents, too high a wax content causes drag and an unwanted sticky feeling when the cosmetic is applied, and can result in a cosmetic that is difficult to remove. To solve this problem, the invention also provides a novel film-forming system comprising relatively high proportions of a particulate mineral gelling agent, for example a gelling agent based on bentonite clay, and a metal soap gelling agent, such as for example zinc laurate, while only a small proportion of wax is used, if it is used. When this film system is used in cosmetic compositions containing microspheres, you can get a good anhydrous film with an excellent possibility of extension and no stickiness or drag. These desirable properties appear to result from a unique combination of the skin adhesion properties of the metal soap with the "ball bearing" lubricity properties of the microspheres. In a practical embodiment of the invention, the loading in the vehicle of our AHA is achieved by dissolving the AHA in glycerin, and by absorbing the AHA dissolved in glycerin on porous microspheres or fine polymeric particles. This system is intended for use in a hydrophobic environment, where the AHAs remain in storage contained in the porous microspheres. When applied to the skin, when the cosmetic is rubbed or massaged into the skin, the microspheres are rubbed across the surface of the skin, bringing them into contact with moisture, which releases the hydrophilic system of AHA- glycerin from the microporous polymer particles. Once discharged from the glycerin-AHA system, now hollow microspheres are available to absorb oil, moderating the oil's decomposition tendencies.

The AHA is preferably loaded onto carrier particles, for example, porous nylon particles in a liquid medium that must be sufficiently viscous to be contained in the pores of the particles during formulation. The lactic acid melts at 16.8 ° C, and can be absorbed into porous vehicle particles, without the need for any auxiliary, at temperatures higher than this melting point, by mixing in appropriate proportions, for example, about 1 : 1 in weight, until the lactic acid is absorbed. Similarly, other acids, such as a mixture of fruit acids, can be charged onto vehicle particles by stirring, ie mixing, by using fine powders with a particle size small enough to be contained in the pores of the vehicle. . The skin revitalization benefits provided by the AHAs result in better structural and visual qualities of the skin, whose benefits can only begin to be seen after a long-term use of the cosmetic composition of the invention, on a regular basis. , for example daily, over a period of weeks, for example, four or six weeks or more. For this purpose, the novel substantially anhydrous cosmetic or eye composition for this embodiment of the invention contains, as the dermatologically active hydrophilic agent, at least one AHA, for example lactic acid or mixed fruit acids, supported on a matrix, or a vehicle in porous particles in powder form, of a synthetic organic polymer, for example nylon. The AHA is preferably present in the surface pores of the carrier particles, and also in the internal pores communicating with these surface pores, such that the AHA can be released at the surface of the particle, and can be removed. of the vehicle particle through the moisture of the skin. The invention also provides a low-wax, or zero-wax, film-to-powder film-forming vehicle for the above AHA loaded system. This low wax vehicle is made possible by a unique combination of a relatively high proportion of a gelling agent, such as a bentonite, and a high proportion of a metal soap, preferably in a volatile solvent system, such as a cyclomethicone. , for example dimethicone or a non-polar solvent, for example a volatile hydrocarbon. Surprisingly, by including the microspheres loaded with AHA in the system, a vehicle with good film-forming capabilities is obtained which is nevertheless under drag or stickiness, apparently due to the "rolling skid" effect referenced above. Single metal soaps are remarkably sticky or adhesive, and these adhesive properties are in fact used, or exploited, to stop the cosmetic base in the skin, and in the case of a base composition, to provide a suitably adhesive base for a finishing coat of, for example, a shadow for eyes. A desirable result obtained with these novel cosmetics is a silky smooth powdery feel. Also, apparently by virtue of their adhesive and yet non-tacky properties, the novel eye enhancers according to the invention are surprisingly durable, as shown by the comparative data. While traditional eye makeups may need a soda after a few hours, and typically fade markedly in about 6 hours, the cosmetics for eyes produced in accordance with the invention can last satisfactorily for more than twelve hours without unacceptable fading. . The cream-to-powder products according to the invention are fast drying. The solvent is evaporated in a matter of a few seconds to provide a silky smooth powder film. The inclusion of a light diffusing agent disperses light in the shadows between cracks in wrinkles or other skin defects and helps give the product a soft focus appearance. These eye enhancers according to the invention work in a synergistic manner the film forming system and the porous microspheres loaded with AHA, to provide a better appearance when applied, giving the skin an illusion of better quality of the skin, while the alpha-hydroxy acid released on contact with the skin, actively conditions or revitalizes the skin, so that after a Period of regular use, which can be as low as four weeks, improves the appearance of the skin without cosmetics. The absorbency of the AHA in the pores of the microsphere particles, using glycerin as an AHA solvent, effectively isolates the hydrophilic from the hydrophobic ingredients, without creating a separate aqueous phase for the dispersion. Another benefit of the use of microspheres is the reduced diffusion into the tissue of the sensitive eye, due to the binding effect of the microsphere. A preferred hydrophobic vehicle for the microsphere particles loaded with active agent, is a silicone gel, which is preferably formulated using a volatile silicone solvent, such as a dimethicone. A preferred gelling agent is a bentonite powder. As described above, the invention preferably employs a low wax cosmetic film forming system comprising, in percent by weight, based on the weight of the composition, from 5.0 to 13.0 percent of a particulate mineral gelling agent, by weight. example a bentonite, and at least 1.0 percent of a metal soap gelling agent, with not more than 5.0 percent of a cosmetic wax material, if present, dispersed in a volatile cosmetic solvent, preferably a cyclomethicone in a proportion of approximately 30.0 to 70.0 percent. A volatile solvent, for example a cyclomethicone, preferably the pentamer form, can be used as a hydrophobic carrier, for example for a cream-to-powder composition. Suitable proportions are from about 20.0 to about 70.0 weight percent of the composition, preferably from about 30 to 40 percent, and more preferably from about 33.0 percent. It works as a wetting agent while it evaporates quickly when applied. Some alternative or additional volatile silicone solvents are described hereinafter. A suitable gelling agent for a volatile solvent, for example quaternium-18 bentonite, from about 1.0 to about 15.0 percent, more preferably from about 3 to 10 percent, and most preferably from about 5.0 to 6.0 percent . Physically stabilizes the composition and functions as a pigment suspension vehicle, and absorbs oil and reduces shine.

Wetting agents A wetting agent, for example sorbitan isostearate, may be used from about 1.0 to about 10.0 weight percent of the composition, preferably from about 3.5 to 4.5 weight percent, and more preferably from about 4.0 percent. Preferred wetting agents allow a greater capacity of solid material, and impart a hydrophobic film.

Additional polymeric microspheres. The synthetic polymeric microspheres in addition to the AHA vehicle powder, for example, polymethyl methacrylate, may be used in a ratio of about 8.0 to about 20.0 weight percent of the composition, preferably about . 0 to 15.0 percent, and more preferably 12.0 percent. These additional polymeric microspheres act as enhancers of the sensation, providing a feeling of "ball bearing" on the application, and a dry sensation of velvet after the application and evaporation of the solvent. Additional functions include scattering of light and imparting a powdery senescence to the product.

Oily esters. An oily low volatility solvent ester, for example, isononyl isononanoate is useful for controlling the volatility and molecular weight of the solvent system in a ratio of about 1.0 to about 10.0 weight percent, preferably about 4.0 to 6.0 percent, and more preferably about 5.0 percent of a solvent. Preferred solvents also function as lipophilic emollients, aid in the solubilization of the ingredients, and are miscible with the volatile carrier solvent (for example dimethicone).

Humectants. One or more oil-soluble humectants, for example lauryl PCA, may be used in a ratio of about 0.4 to about 2.5 percent, preferably about 0.5 percent, or cetyl dimethicone, in a proportion of about 1.0 to about 5.0 weight percent of the composition, to improve wetting. Cetyl Dimethicone provides a dry and light sensation, and aids in film formation.

Oil Absorbents Kaolin or other oil absorbers can be used in a ratio of about 0.50 to about 3.0 weight percent of the composition, preferably from about 0.7 to 1.5 percent, and more preferably 1.00 percent. Preferred functions of the oil absorber include the absorption of excess oils from the skin, adhesion to the skin, diffusion of light, and opacification.

Opacifiers. An opacifier, for example titanium dioxide, may be used in a ratio of from about 0.10 to about 5.0 weight percent of the composition, preferably from about 0.3 to 1.0 percent, and more preferably 0.50 percent, to provide coverage and help hide skin defects.

Plasticizers A volatile polar activating solvent can be used for the gelling agent, for example of hexylene glycol, in a ratio of about 0.75 to about 1.75 weight percent of the composition, preferably about 0.85 percent. This will act as a plasticizer, binder, solvent, and softener, while providing resistance to moisture and oxidation.

Conservatives Conservatives such as, for example, methyl- or propyl-paraben can be used, in proportions of, for example, 0.1 to 0.3 percent by weight, as is known to those skilled in the art.

Other optional ingredients Other optional ingredients may be used, as is known to those skilled in the art, including pigments and fragrances. Some additional optional ingredients are: Vitamin E linoleate, in a percentage of about 0.10 percent, as a complementary humectant; Vitamin E acetate, at approximately 0.10 percent, works as a scavenger of free radicals and as an antioxidant; Retinyl palmitate, at approximately 0.1 percent, functions as a derivative of retinoic acid to reduce fine lines, - ceramides at a lower percentage of about 0.3 percent, function as a skin-firming agent; sphingolipids, serve to the function of affirming the skin in a smaller percentage of approximately 0.3 percent, they work to improve the skin barrier, increasing in this way the humidification and diminishing the penetration of irritating substances.

Alternative volatile silicone solvents. A class of cyclomethicone compounds that is preferred for use in the cosmetic compositions of this invention is illustrated by the compounds of the formula - [RjR2SiO] n-, wherein Rj and R2 are each, lower alkyl having from 1 to 4 carbon atoms, with or without innocuous substituents selected from the group consisting of halogen, hydroxyl, carboxyl, or methoxy, and n is from 3 to 6; whose compounds are cyclized. The volatile cyclomethicone solvent used may be one of the above compounds, or a mixture thereof, and the compound or compounds may be a homopolymer wherein all n-monomer units are similar, or a heteropolymer where they are different. Some preferred cyclomethicones are dimethicones, especially homopolymers where n is 4 or 5; and Rj and R2 are each methyl, such as octamethylcyclotetra-siloxane and decamethylcyclopentasiloxane. Depending on the character of the composition of the final product, for example, compound eye enhancer, eye shadow base, lipstick, blush, makeup, and the like, other optional ingredients may be used, as are known to those skilled in the art. , in proportions known to those skilled in the art. These ingredients include, but are not limited to, fragrance, color, pigments, preservatives, wetting agents, oil absorbers, opacifiers, and antioxidants. The following Examples illustrate the practice of the invention in greater detail. The proportions of the ingredients used in the Examples are stipulated in the different Tables, as identified in the Examples. Table I stipulates the ingredients used in Examples 1 and 2.

TABLE I EXAMPLE 1 Lactic Acid Powder Mix In Example 1, porous nylon 12 microspheres are loaded with lactic acid, using a glycerin solvent. The glycerin is mixed in a mixer with an equal amount of lactic acid, to form a phase A, using the proportions stipulated in Table II. The nylon powder 12 is then added to phase A in a ratio of two parts of phase A to three parts of nylon 12. The glycerin-lactic acid phase is absorbed substantially completely by the nylon 12 microspheres, increasing its density, to produce a free-flowing powder. This combination is mixed for one hour to produce a physically sticky, slightly sticky lactic acid powder mixture, which is subsequently used in Example 9.

EXAMPLE 2 Mixed Mixed Fruit Acid Powder Example 1 is repeated using mixed fruit acids in place of lactic acid in the proportions indicated in Table I. A physically sticky and slightly sticky powder is obtained, and is used in Example 10 TABLE II EXAMPLE 3 Dry Mix for OTOS Metorator A dry mixture is prepared for use in single-phase eye improving compositions, using the ingredients referred to in Table II. Powdered zinc laurate is combined with mica coated with aluminum [myristate], kaolin, and titanium dioxide, and mixed until a smooth, homogeneous powder is obtained. Table III stipulates the ingredients used in Examples 4-5.

TABLE III Example 4 Lactic Acid Mixture in Nylon Vehicle 12 Without Solvent In this Example, porous nylon 12 microspheres are loaded with lactic acid without the use of solvents. The ingredient in phase A is added slowly to the ingredient in phase B, while mixing in a mixer at room temperature. The preparation produces a 4: 1 mixture of Nylon 12 / lactic acid, used in Example 7.

EXAMPLE 5 Mixture of Mixed Fruit Acids in Nylon Vehicle 12 Solventless Example 4 is repeated, using mixed fruit acids to replace the lactic acid, and reducing the proportion of nylon 12 used, to give a product with a ratio of 1. : 1 of nylon 12 to mixed fruit acids. This preparation is used in Example 6. Table IV stipulates the ingredients used in Examples 6 to 8. TABLE IV FA &S DESCRIPTION! B emolo 6 E ßmolo 7 11emolo 8 A Dimethicone 0.50 0.50 0.50 A Sodium stearate 4.00 4.00 4.00 blen A Asonsonanoate of iso5.00 5.00 5.00 nonyl A Laurildone of lauryl 3.00 3.00 0.50 A Dimeticone SL88 10.00 10.00 A Dimethicone cetyl 10.00 10.00 3.10 A Glyceryl tribehenate 0.17 A Ceresin, low melting point 0.76 A Microcrystalline wax 0.17 A Propylparaben 0.10 0.10 0.10 A Methylparaben 0.30 0.30 0.30 A Cyclomethicone 18.00 B Zinc Laurate 3.00 3.00 3.00 B Aluminum mica-myristate 12.00 11.52 12.00 B Kaolin 1.00 1.00 1.00 B Titanium dioxide 1.00 B Nylon 12 5.00 C Nylon 12 / mix 4: 1 nylon 12 / lactic acid 5.00 C Mix 1: 1 Nylon 12 / mixed fruit acids 5.00 5.00 B MBX8C (PMMA) polymethyl methacrylate 5.87 12.00 12.00 D Tioxogel CYM 34.10 34.258 34.20 E Tocopherol linoleate 0.10 0.10 E Tocopherol acetate 0.10 0.10 E Retinyl palmitate 0.10 0.10 B Yellow (55-0242) 0.03 B Red (55-0241) 0.02 B Black (55-0016) 0.002 Example 6 Mixture of N vlon 12 / Mixed Fruit Acids Without Solvent. In an Anhydrous Base Example 6 incorporates the composition prepared as in Example 5 into an anhydrous base, according to the percentages mentioned in Table III. The ingredients of phase B are dispersed by mixing for at least three minutes at a high speed. Once dispersed, phase B is added to phase C, and mixed at low speed for 1 minute. The ingredients of phase A are mixed and heated to 65 degrees Celsius until transparent. When phase A remains transparent, the mixture of mixed phases B and C is added, in a mixer of propeller type, until it is uniform and free of lumps. Once this mixture is uniform, add the ingredients of phase D, and again mix until uniform.

Example 7 Lactic Acid Mixture in Nylon Vehicle 12 Solvent-free, in an Anhydrous Base Example 6 is repeated, with the addition of nylon 12 in phase B, to further improve the feel of the composition, and the substitution of the mixture of lactic acid in nylon vehicle 12 without solvent, as prepared in Example 4, by mixing mixed fruit acids in nylon vehicle 12 without solvent, as prepared in Example 5. Substitution with the acid mixture produces a composition with a higher percentage of alpha-hydroxy acid.

Example 8 Mixture of Nvlon 12 / Mixed Fruit Acids Without Solvent, in an Anhydrous Base as a Color Base Example 8 uses the procedure designed in Example 6, with the inclusion of an E phase comprising additives and colorants. This final phase involves the mixture that is set at 45 degrees Celsius at which point the ingredients of phase E are added and mixed until they are uniform. Cetyl dimethicone and dimethicone are substantially replaced with cyclomethicone. The less volatile ketone dimethicone and dimethicone "lead to the production of a creamy composition, while the more volatile cyclomethicone produces a composition that will be rubbed in a cream-to-powder vehicle.Different coloring agents can be used as evidenced by the inclusion of various coloring agents as ingredients of phase B. Table V stipulates the ingredients used in Examples 9-10.

TABLE V PHASE DESCRIPTION Example 9 Example 10 A Dimethicone 1.00 1.00 A Sorbitan isostearate 4.00 4.00 A isononyl ionsonanoate 5.00 5.00 A lauryl PCA 0.50 0.50 A Dimethyl ketone 2.13 2.13 A Glyceryl tribehenate 0.32 0.32 A Ceresin, low melting point 1.43 1.43 A Microcrystalline wax 0.32 0.32 A Propylparaben 0.10 0.10 A Methylparaben 0.30 0.30 B Cyclomethicone 17.60 17.60 C Dry mixes to improve eyes 11.00 11.00 D Nylon 12 5.00 5.00 C Mixed powder of mixed fruit acids 5.00 D Powdered mix of lactic acid 5.00 D MBX8C (PMMA) polymethyl methacrylate 12.00 12.00 E Tioxogel CYM 33.50 33.50 E Tocopherol linoleate 0.10 0.10 E Tocopherol acetate 0.10 0.10 E Retinyl palmitate 0.10 0.10 E Hydrophobic sphingolipid. 0.50 0.50 Tixogel CYM (Hexylene glycol / Quaternite-18 Bentonite / Cyclomethicone).

EXAMPLE 9 OIE MIXER WITH LACTIC ACID Example 9 shows the compositions prepared in Examples 1 and 5, and adds the ingredients mentioned in Table III. The procedure for preparing Example 9 is that used in Example 8. Example 9 makes use of the hydrophobic espingolipid complex to promote skin firming.

Example 10 01o Melonizer With Mixed Fruit Acids Example 9 is repeated using Example 2, mixed powder of mixed fruit acids, to replace Example 1, lactic acid powder mix. The products of Examples 9 and 10 were tested to determine their dermatological and cosmetic properties. Some of the results are reported later.

Physiological benefits. The controlled bisphysical studies, employing the cosmetic composition for eyes of Examples 9 (lactic acid) and 10 (mixed fruit acids), demonstrated valuable structural dermatological improvements. Some controlled tests showed significant increases in the moisture content of the ridge (external corner of the eye) and below the eye, accompanied by an increase in firmness and a reduction in fine lines and wrinkles. Twenty women were treated per product in a half-face design with the products of Examples 9 and 10. The product of Example 9 or 10 was only applied around one eye, and a moisturizing eye cream concentrate was applied, before product, around another eye. The treatments were applied to the face twice a day, but not on the morning when the measurements were taken. The characteristics of skin moistening, firmness, and edge texture were determined, as described below.

Moistening of the skin. Measurements of edge impedance and area under the eye of the cheeks with a dermal phase meter showed average increases in moisture content as stipulated later in Tables VI and VII, respectively, when compared to the measurements of the baseline taken in week 0 (not reported): TABLE VI Percentage of Me ora in the Moisture Content of the Canto Accordingly, at least a 20 percent increase in wetting was achieved with all the compositions after six weeks of use, the lactic acid formulation of Example 9 was more effective than the mixed fruit acid (MFA) formulation of Example 10, and the eye cream moisturizer provided a useful additional motorization benefit, in four or more weeks. Comparable, but slightly lower, results were obtained in the area under the eye, as shown in Table VII below. TABLE VII Percentage of Improvement in the Moisture Content Debaio of the EYE Firmness of the skin. Using a balestometer, the firmness of the song was determined at the indicated times, and compared with the baseline measurements taken at week 0 (not reported). The results are reported in the following Table VIII: TABLE VIII Percentage of Improvement in the Firmness of Singing These results show a significant 19 percent increase in firmness obtained with the lactic acid formulation of Example 9, after only four weeks of use. The mixed fruit acid (MFA) formulation of Example 10 was slightly less effective, but still produced a significant increase in skin firmness. er results are obtained after six weeks, and by using a humectant.

Improvements in the texture of the skin. Using computer assisted image analysis of ridge replicas, measurements were made of decreases in fine lines and wrinkles at the indicated times, comparing with the values of the baseline of week 0. The results are reported in the following Table IX.

TABLE IX Percentage of Improvement in Fine Lines and Wrinkles of the Ridge The results in Table IX show a significant 16 percent increase in firmness, obtained with the lactic acid formulation of Example 9, after only four weeks of use. The mixed fruit acid (MFA) formulation of Example 10 was slightly less effective, but still produced a significant increase in skin firmness. Better results are obtained after six weeks and by using a humectant. Other controlled tests showed that the compositions of the invention can be used as a foundation for eyeshadow to reduce cracking of eye shadow and loss of color, and to impart water resistance.

Cracking of the shadow for eyes. Eye shadow cracking is a well-known phenomenon often exhibited by people with oily skin, which is exhibited as an irregular color, or a shift of the eye shadow towards the ridges and grooves, which may develop within how many hours of the application of the shadow for eyes. A study listing twelve adult female panelists, each having a history of shadow cracking for eyes, showed that the use of the cosmetic composition for eyes of the invention, as a base, was effective in controlling the cracking of the shadow for eyes applied on the base. The eye shadow base composition of the invention was applied to one eyelid only of each panelist, and allowed to dry for one minute, followed by a pink eye shadow applied to both eyelids. The eyelids were videotaped immediately following the application of the eye shadow, and an image of the center of each eyelid was frozen for image analysis. The procedure was repeated three and six hours after the first application. The analysis of the image showed that the eyelids treated with base exhibited insignificant increases in the irregularity of the eye shadow, even after eeie horae. In contrast, the irregularity of the eye shadow coverage increased significantly at both the three and six hours on the eyelids that lacked the base.

Color of shadow for eyes. Other tests showed that the eye shadow base composition of Example 9 was effective in controlling the loss of color of the eye shadow. No formula changed the color of a superimposed eye shadow, as measured with a chromameter. The forehead was selected as an objective site for the color control tests, due to the difficulties to surely measure the eyelid color, and due to the physiological similarities between the forehead and the eyelids with respect to the presence of sebum and the like. Eye shadow and base were applied to one side of the forehead of each of twelve people. 'Eyeshadow was applied only to the other. Immediately after each application, color measurements were made with a chromameter, and repeated three and six hours later. In addition, skin color treated with base was not lost, even after sixteen hours. This was in contrast to unprepared skin, which showed a statistically significant loss of color. It is important that the color of the eye shadow was not changed by its application on the base composition of the invention.

The color losses of the eye shadow prepared with the composition of the invention were visually insignificant after six hours, and in fact were less than the side prepared at three hours.

Waterproof. Other tests with twelve people showed resistance to water. The eye shadow and the base composition of the invention as described above were applied to the comparative forearm areas. Immediately after taking the color measurements, the arm was rinsed, air dried, and the measurement was taken again. The resulting data showed a significant loss of blue color from the unprepared site, while there was no change in the prepared site. The color loss control suggested that the base imparted significant resistance to water.

Barrier properties and deposit of acids in the skin. Transepidermal water loss measurements showed that the products of Examples 9 and 10 can significantly reduce water loss, and therefore, provide an increase in skin barrier function. This increased barrier function can improve the penetration in the stratum corneum of the active ingredients applied below the applied barrier, for example, alpha-hydroxy acids trapped in porous microspheres. It is postulated that the microspheres loaded with alpha-hydroxy acid of the invention can participate in the best barrier function, while simultaneously depositing acids in the skin, the acids being directed from the microspheres by the affinity of the glycerol solvent with the moisture of the skin. Other studies showed that the products could improve skin tone in a short time, up to six hours, and did not impose an immediate physical threat to contact lenses of polymacon or surfilcon A.

INDUSTRIAL APPLICABILITY The present invention is particularly suitable for application to modern industrial processes. In particular, it is useful in the cosmetics industry, where it can provide new products that offer new benefits to consumers, as described herein. Although an illustrative embodiment of the invention has been described above, of course, it is understood that ordinary experts in this field will be able to enter into different modifications.

Claims (34)

1. An essentially anhydrous, locally applied cosmetic composition, which comprises: a) an effective amount of at least one dermatologically active polar agent; b) a sufficient amount of a vehicle with adsorbent or absorbent particles to support the dermatologically active polar agent; c) a cosmetic hydrophobic phase base, said essentially anhydrous base having a sufficient amount of a film-forming agent to produce a desired cosmetic film, when the cosmetic composition is applied to the skin, the vehicle loaded with active agent being dispersed on this basis cosmetic

2. A cosmetic composition according to claim 1, which comprises, in proportions by weight, based on the weight of the composition: a) from 0.01 to 10 percent of the dermatologically active polar agent, - b) from 0.1 to 40.0 percent of the particulate vehicle, having at least 80 percent of these vehicle particles a particle size greater than 10 microns; c) from 1.0 to 99.0 percent of the film-forming agent; whereby, the local application of the cosmetic composition to the skin produces a controlled release of the active agent to the surface of the stratum corneum.

3. A cosmetic composition according to claim 1, which further comprises a solvent in liquid phase for the polar active agent, this solvent being substantially immiscible with the base in hydrophobic phase in a weight ratio of the active agent to the solvent of about 1:99 to about 99: 1, with the dissolved polar agent being retained by the vehicle.

4. A cosmetic composition according to claim 1, wherein the dermatologically active agent comprises one or more substances selected from the group consisting of skin exfoliating acids, water soluble vitamins, astringents, dentifrices and care agents. dental, external analgesics, wart removers, anesthetics, keratolytics, anti-inflammatories, agents against dandruff, bleaching agents, chemical sunscreens, moisturizers, deodorants, color enhancers, intercellularly active agents, and hormones.

5. A cosmetic composition according to claim 3, wherein the dermatologically active agent is an alpha-hydroxy acid or a beta-hydroxy-skin revitalizing acid.

6. A cosmetic composition according to claim 3, wherein the dermatologically active agent is lactic acid.

7. A cosmetic composition according to claim 5, wherein the dermatologically active agent is incorporated in the cosmetic composition in a proportion of about 0.1 to about 4.0 weight percent.

A cosmetic composition according to claim 1, wherein the adsorbent or absorbent vehicle is selected from the group consisting of organic synthetic polymeric microspheres, silica, starch, polystyrene, spherical cellulose acetate, polyethylene, styrene, polytetrafluoroethylene , polymethyl methacrylate, acrylate polymers, talc, kaolin, mica, calcium silicates, nylon, magnesium carbonate and other salts, boron nitride, polyvinylidene copolymer, silicone resin, polyurethane, modified organic clays, and earth clays .

9. A cosmetic composition according to claim 8, wherein the absorbent carrier is porous.

10. A cosmetic composition according to claim 3, wherein the absorbent carrier is nylon 12, present in a ratio of about 5.0 to about 20.0 weight percent of the composition.

11. A cosmetic composition according to claim 3, wherein the solvent is selected from the group consisting of glycerin, a water-soluble glycol and cosmetically compatible; water, alcohol; sodium citrates; PPG 650 oleic ether; glycereth 4,5; lactates, ethoxydiglycol; nonoxynol 10, 12, 14, 40, 50; octoxynol 11, 40; PEG 4 dilaurate; glycereth 7, 26; methylated cyclodextrin; PEG 40; polysorbate 20; and dimethyldodecyl amine oxide.

12. A cosmetic composition according to claim 3, wherein the solvent is glycerin.

13. A cosmetic composition according to claim 3, wherein the vehicle is porous, and the solvent has a viscosity of about 5 cps at about 100,000 cps, to control the exit of the active agent from the pores of the vehicle.

14. A cosmetic composition according to claim 1, wherein the film-forming agent is selected from the group consisting of solid, liquid, or semi-solid, saturated, unsaturated, or branched fatty esters, amides, alcohols, soaps, waxes, and powders, and mixtures thereof.

15. A cosmetic composition according to claim 14, wherein the film-forming agents are selected from the group consisting of glyceryl tribehenate, ceresin, microcrystalline wax, volatile silicone, dimethicone, sorbitan isostearate, isononyl isononanoate, Cetyl dimethicone, and zinc laurate.

16. A hydrophobic, dermatologically active cosmetic eye area composition having cosmetic appearance improving properties combined with dermatological properties, this cosmetic composition comprising: a) a dermatologically acceptable and innocuous porous particulate carrier having a size of particles greater than 10 microns; b) a dermatologically active hydrophilic agent, this active agent being loaded into the pores in the particulate carrier; c) a hydrophobic, non-hardening film forming system for providing a film or bale including the particles of vehicle loaded with active agent, covering the film or bale the skin when the cosmetic composition is spread on the skin; and d) a film-forming adhesive to hold the film or bale on the skin.

17. A cosmetic composition according to claim 16, wherein the dermatologically active agent is an alpha-hydroxy-skin revitalizing acid.

18. A cosmetic composition according to claim 17, wherein the alpha-hydroxy acid is selected from the group consisting of lactic acid, glycolic acid, citric acid, malic acid, equivalents thereof and mixtures of the above ingredients, and is present in a proportion of 0.5 to 8.0 weight percent of the composition.

19. A cosmetic composition according to claim 16, wherein the particulate carrier is a porous synthetic polymeric organic microsphere, with a particle size from greater than 10 to 100 microns.

20. A cosmetic composition according to claim 16, having cosmetic appearance improving properties, with opaque coloring pigments, comprising 0.10 to 3.0 percent of the composition by weight.

21. A cosmetic composition according to claim 16, wherein the hydrophobic film forming system comprises: i) a solvent vehicle of hydrophobic phase, this carrier loaded with active agent being dispersed in the vehicle hydrophobic fae; ii) a particulate mineral gelling agent; iii) a metal soap gelling agent; and iv) a cosmetic wax material.

22. A cosmetic composition according to claim 21, wherein the vehicle in the hydrophobic phase is a volatile polysiloxane, the particulate mineral gelling agent is a bentonite gelling agent in a proportion of about 5.0 to 13.0 percent, the gelling agent of metallic soap is an alkaline earth or an aluminum alkanoate of 6 to 20 carbon atoms, in a proportion of 1.0 to 5.0 percent, and the cosmetic wax material is selected from the group consisting of esters of glyceryl wax, ceresin waxes, microcrystalline waxes, equivalents thereof, and mixtures of the above cosmetic wax ingredients, these proportions being by weight, based on the weight of the composition.

23. An eye shadow or eye shadow base which is a cosmetic composition according to claim 16, and which has skin moisture improving properties.

24. A locally applied cosmetic composition, which comprises: a) an effective amount of a dermatologically active hydrophilic agent; b) a vehicle in porous particles for the active hydrophilic agent, this vehicle having an average particle size in the range of 10 to 50 microns, the active agent being loaded into the pores of the vehicle; c) a vehicle in hydrophobic phase, the vehicle loaded with active agent being dispersed in this vehicle in the hydrophobic phase; and d) a hydrophilic viscous solvent for the active agent, this hydrophilic solvent being substantially immiscible with the vehicle in hydrophobic phase, the active agent being dissolved in the viscous solvent to provide a viscous solution of the active agent, the viscous solution being retained in the pores of the vehicle; whereby, the local application of the cosmetic composition puts the viscous solution in contact with the skin for the release of the viscous solution from the vehicle by the moisture of the skin, and the application of the active agent to the stratum corneum.

25. A locally applied cosmetic composition according to claim 24, wherein the dermatologically active hydrophilic agent is an alpha-hydroxy acid, selected from a list that includes mixed fruit acids, lactic acid, glycolic acid, citric acid , and malic acid, and is present from 0.5 to 8.0 weight percent.

26. A locally applied cosmetic composition according to claim 24, wherein the porous particulate carrier for the active hydrophilic agent is a pre-eyed organic polymeric microsphere from 5.0 to

20. 0 percent.

27. A locally applied cosmetic composition according to claim 24, wherein the hydrophobic phase vehicle is a volatile polysiloxane.

28. A locally applied cosmetic composition according to claim 24, wherein the hydrophilic viscous solvent is glycerol.

29. A low-wax cosmetic film forming system suitable for incorporation into cosmetic eye enhancing compositions, this film-forming composition comprising, in percent by weight, based on the weight of the composition: a) at least 5.0 by weight percent of a particulate mineral gelling agent for a volatile cosmetic solvent; b) at least the l.O percent of a metal soap gelling agent; and c) from 0.0 to 5.0 percent of a cosmetic wax material; dispersed in the volatile cosmetic solvent.

30. A film-forming system according to claim 23, which comprises from about 8.0 to 20.0 percent of synthetic polymeric organic microspheres improving the se- quenation.

31. A film-forming system according to claim 24, wherein: a) the particulate mineral gelling agent comprises a bentonite gelling agent in a proportion of about 5.0 to 13.0 percent, - b) the gelling agent of Metallic soap is an alkaline earth alkanoate of 6 to 20 carbon atoms, in a proportion of 1.0 to 5.0 percent, - c) the cosmetic wax material is selected from the group consisting of esters of glyceryl wax, waxes of ceresin, microcrystalline waxes, equivalents thereof and mixtures of the above cosmetic wax ingredients, and wherein the volatile cosmetic solvent is a cyclomethicone in a proportion of 30.0 to 70.0 percent.

32. A film-forming system according to claim 31, which comprises from about 8.0 to 20.0 percent synthetic organic polymeric enhancing sensing microspheres.

33. A cream-to-powder cosmetic composition comprising a major proportion of a low-wax film-forming system according to claim 32.

34. A process for the preparation of a locally applied cosmetic composition according to claim 1, which comprises: a) mixing the dermatologically active agent or a solution thereof with the vehicle in absorbent particles, until this active agent is completely absorbed by the vehicle; and b) adding the dermatologically active vehicle and agent complex to the hydrophobic cosmetic base.