CN1160053C - Low viscosity niacinamide composition - Google Patents

Abstract

The present invention relates to a topical leave-on skin care composition comprising: a) from about 1% to about 10% of a vitamin _B3 compound; and b) a high spreading oil selected from: i) a branched hydrocarbon having a weight average molecular weight of from about 100 to about 1000, and ii) a liquid ester softener of formula I: wherein ^R1 is selected from H or _CH3 , ^R2 , ^R3 and R4 are independently selected from _C1 - _C20 straight or branched chain alkyl, and x is an integer from 1 to 20 and mixtures thereof, characterized in that the composition contains 0.3% to 4% of an anti-tack agent selected from poly(alpha-olefins) having a MW of 260 to 1000, preferably polydecene, and an occlusive agent selected from petrolatum, cetyl ricinoleate and lanolin. The composition of the present invention is preferably an oil-in-water emulsion containing less than 4% of anionic or amphoteric surfactants, useful for maintaining a natural skin appearance and can be applied topically without undesirable cosmetic effects such as a sticky feel on the skin. The present invention also relates to the use of polydecene or petrolatum to reduce the viscosity of leave-on skin care compositions containing from about 1% to about 10% of a vitamin _B3 compound.

Description

Low viscosity niacinamide composition

skin care composition

This invention relates to topical compositions for improving the appearance and feel of human skin. In particular, the present invention relates to leave-on skin care compositions, more particularly oil-in-water emulsions, which are effective for conditioning skin without being highly viscous.

Background technique

Various compounds have been described in the art for conditioning fine lines, wrinkles and other forms of undesirable skin surface texture. For example, vitamin _B3 compounds, particularly niacinamide, have recently been found to provide modest benefits in regulating skin condition, including the regulation of fine lines, wrinkles and other forms of uneven or rough surface texture associated with aging or photodamaged skin . However, these substances, when used in clinically effective amounts, can produce undesired short-term cosmetic effects, particularly a tacky or viscous feel upon application to the skin.

Many substances produce stickiness on the skin at high levels; glycerin is one of the commonly known substances. Therefore, there are many solutions for reducing viscosity in the prior art.

EP-A-692,242 discloses hollow, deformable particles of 1-250 [mu]m particle size for reducing the sticky feel of compositions rich in fatty substances.

WO 92/19217 describes cosmetic compositions in the form of hydrogels containing glycerin, panthenol moisturizer and polyglycerylmethacrylate (PGMA) lubricant. The composition is said to have low viscosity. Likewise, WO93/24101 describes cosmetic compositions which also contain polyols, especially glycerol, and PGMA. It tells that trimethylglycine (betaine) is valuable in providing improved skin feel and reduced stickiness.

Co-pending PCT applications PCT/US98/22483 and PCT/US99/04748 disclose that the sticky feel of vitamin _B3 compounds can be reduced by providing organic particles.

Furthermore, it is known in the art, eg WO98/52530, that emollients, including petrolatum and branched chain hydrocarbons, can be added to vitamin _B3 compositions.

Co-pending PCT application PCT/US98/21521 discloses cosmetic compositions that can provide improved moisturization, skin feel, skin softness, skin smoothness, and superior penetration and absorption. Its examples contain both isohexadecane and niacinamide.

Certain hydrocarbon emollients have now been found to be effective in reducing the stickiness and stickiness of vitamin _B3 compositions. Surprisingly, these substances are oily in nature and would be believed to increase the sticky feeling rather than reduce it.

It is an object of the present invention to provide a vitamin _B3 composition which is effective in conditioning the condition of the skin and which has low stickiness or stickiness.

Summary of the invention

The present invention relates to a topical leave-on skin care composition comprising:

a) about 1% to about 10% vitamin _B3 compound;

b) high spreading oils selected from:

i) branched chain hydrocarbons having a weight average molecular weight of from about 100 to about 1000, and

ii) liquid ester softeners of the following formula I and mixtures thereof:

Formula I

wherein R ¹ is selected from H or CH ₃ , R ² , R ³ and R 4 are independently selected from C ₁ -C ₂₀ straight chain or branched chain alkyl, and x is an integer from 1 to 20 and mixtures thereof; and

iii) mixtures thereof; and

c) a carrier for the skin,

It is characterized in that the composition contains 0.3%-4% anti-adhesive agent selected from poly(α-olefins) with MW of 260-1000 and occult agent selected from petrolatum, cetyl ricinoleate and lanolin. agent).

A second aspect of the present invention relates to the use of polydecene for reducing the viscosity of leave-on skin care compositions containing from about 1% to about 10% vitamin _B3 compound. A third aspect of the present invention relates to the use of petrolatum for reducing the viscosity of leave-on skin care compositions containing from about 1% to about 10% vitamin _B3 compound.

The composition, preferably an oil-in-water emulsion, can be used to maintain the natural skin appearance and can be applied topically without undesired cosmetic effects such as skin feeling sticky. In general, the compositions of the present invention contain less than about 4%, preferably less than about 1%, of anionic, amphoteric or zwitterionic surfactants.

Detailed description of the invention

As used herein, all percentages and ratios are by weight of the total composition and all measurements made are at 25°C, unless otherwise specified. All publications mentioned herein are incorporated herein by reference.

As used herein, the term "leave on" with respect to skin care compositions means that they are used without a cleansing step, such as after applying the composition to the skin. Preferably, the composition remains on the skin for at least about 15 minutes, more preferably at least about 15 minutes. 1 hour, preferably several hours.

Useful active and other ingredients are categorized or described herein by their cosmetic and/or therapeutic benefit or their postulated mode of action. It should be understood, however, that the active and other ingredients useful herein may in some instances provide more than one cosmetic and/or therapeutic benefit or operate via more than one mode of action. Accordingly, classifications are made herein for convenience and are not intended to limit ingredients to the applications specifically stated or listed.

The compositions of the present invention are useful in regulating the condition of the skin, including regulating visible and/or tactile discontinuities in the skin, especially discontinuities associated with skin aging, such as wrinkles. This discontinuity may be caused or caused by internal and/or external factors. External causes include ultraviolet radiation (such as exposure to the sun), environmental pollution, wind, heat, low humidity, harsh surfactants, abrasives, etc. Intrinsic causes include chronic aging and other biochemical changes within the skin.

Vitamin _B3 Compound

The first essential component of the compositions of the present invention is from about 1% to about 10%, preferably from about 2% to about 8%, more preferably from about 3% to about 7%, of a vitamin _B3 compound. This compound gives a sticky feel when used alone, especially when used in higher amounts. Herein, "vitamin _B3 compound" refers to a compound having the following formula:

wherein R is _-CONH2 (ie, nicotinamide), -COOH (ie, niacin), or _-CH2OH (ie, nicotinol); derivatives thereof and salts of any of the foregoing.

Exemplary derivatives of the aforementioned vitamin _B3 compounds include nicotinic acid esters, including nicotinic acid, nicotinyl amino acids, nicotinyl alcohol esters of carboxylic acids, non-vasodilating esters of nicotinic acid N-oxide and nicotinamide N-oxide. As used herein, "non-vasodilating" means that esters do not often produce a visible flushing response following application of the present composition to the skin (most normal people will not experience a visible flushing response, although such compounds may cause invisible flushing to the naked eye. vasodilation, i.e. the ester is non-erythrotic). Non-vasodilating esters of niacin include tocopheryl nicotinate and inositol hexanatinate; tocopheryl nicotinate is preferred.

Other derivatives of vitamin _B3 compounds are nicotinamide derivatives resulting from substitution of one or more amido hydrogens. Examples of nicotinamides suitable for use in the present invention include nicotinyl amino acids (obtained, for example, from the reaction of an activated nicotinic acid compound (such as nicotinic acid azide or nicotinyl chloride) with an amino acid) and organic carboxylic acids (such as C1-C18) of nicotinol esters. Specific examples of such derivatives include nicotinyl glycine (C ₈ H ₈ N ₂ O ₃ ) and nicotinyl hydroxamic acid (C ₆ H ₆ N ₂ O ₂ ). Exemplary nicotinol esters include nicotinol esters of the carboxylates salicylic acid, acetic acid, glycolic acid, palmitic acid, and the like. Other non-limiting examples of vitamin _B3 compounds useful in the present invention are 2-chloronicotinamide, 6-methylnicotinamide, N-methylnicotinamide, and nicotinamide.

Vitamin _B3 compounds are well known in the art and are available from many sources such as Sigma Chemical Company (St. Louts, MO); ICN Biomedicals Company (Irvin, CA) and Aldrich Chemical Company (Milwaukee, WI).

One or more vitamin _B3 compounds may be used in the present invention. Preferred vitamin _B3 compounds are niacinamide and tocopheryl nicotinate. Niacinamide is more preferred.

Salts of vitamin _B3 compounds may also be used. Examples that can be used in the present invention include organic or inorganic salts such as inorganic salts formed with anionic inorganic substances (eg chlorides) and organic acid carboxylates. These and other salts of vitamin _B3 compounds are readily prepared by those skilled in the art, for example W. Wenner "Reaction of L-ascorbic acid and D-isoascorbic acid with niacin and its amides", Journal of Organic Chemistry, Vol. 14, 22 - as described on page 26 (1949). Wenner describes the synthesis of the ascorbate salt of nicotinamide.

In a preferred embodiment, the ring nitrogen of the vitamin _B3 compound is uncomplexed, or becomes uncomplexed after delivery to the skin. More preferably, the vitamin _B3 compound is essentially uncomplexed. Thus, if a salt or other complexed form of the vitamin _B3 compound is included in the composition, such complexing is preferably substantially reversible when the composition is applied to the skin. This complex should be substantially reversible at a pH of about 5.0 to about 6.0. Such reversibility is readily determined by one of ordinary skill in the art. Preferably, the vitamin _B3 compound contains less than about 50% of the compound in salt form.

The vitamin _B3 compound may be included as substantially pure material, or as an extract by suitable physical and/or chemical isolation from a natural (eg plant) source. The vitamin _B3 compound is preferably substantially pure, which means that it is substantially free of impurities when obtained from a natural source. These compounds may be provided in solution, optionally containing antioxidants or other stabilizers.

high spreading oil

Particularly preferred compositions of the present invention also contain from 3% to 10%, preferably from about 3% to about 8%, more preferably from about 4% to about 6%, of a high spreading oil selected from i) having a weight average molecular weight of about 100 to about 1000 branched chain hydrocarbons and ii) liquid ester softeners of formula I below:

Formula I

Wherein R ¹ is selected from H or CH ₃ , R ² , R ³ and R ⁴ are independently selected from C ₁ -C ₂₀ straight chain or branched chain alkyl, and x is an integer of 1-20.

This highly spreading oil facilitates the distribution of vitamin _B3 compounds on the skin.

Suitable examples of branched chain hydrocarbons include isododecane, isohexadecane and isoeicosane. Isohexadecane is preferred. Herein, poly(alpha-olefin) antiblocking agents also generally belong to branched chain hydrocarbons, which will be described in detail below. When using this anti-adhesive agent, it should be considered that its amount should be included in the content range of the above-mentioned high-spreading oil.

Suitable ester softener materials of formula I above include methyl isostearate, isopropyl isostearate, isostearyl neopentanoate, isononyl isononanoate, isodecyl octanoate, isononyl Isodecyl Isononanoate, Tridecyl Isononanoate, Myristyl Caprylate, Octyl Nonanoate, Octyl Isononanoate, Myristyl Myristate, Myristyl Neopentanoate, Isostearyl Neopentanoate esters, myristyl caprylate, myristyl propionate, isopropyl myristate and mixtures thereof.

Preferred ester softeners for use in the present invention are isononyl isononanoate, isostearyl neopentanoate, methyl isostearate, isopropyl isostearate, isopropyl stearate, meat Isopropyl myristate and mixtures thereof.

Particularly preferred high spreading oils for use herein are isohexadecane, isononyl isononanoate, methyl isostearate, isopropyl isostearate or mixtures thereof.

More preferred for use herein are mixtures of high spreading oils containing isohexadecane and isopropyl isostearate. The use of such mixtures is particularly preferred when the compositions of the invention contain high levels of glycerol.

Ester softener materials are preferably present in the compositions at a level of from about 0.1% to about 10%, preferably from about 0.1% to about 8%, especially from about 0.5% to about 5%, by weight of the composition.

Antisticking agent

Another essential component of the compositions of the present invention is from about 0.3% to about 4%, preferably from about 0.5% to about 2.5%, more preferably from about 1% to about 2%, of an anti-adhesive agent selected from Poly(alpha-olefins) and occlusion agents having a MW of from about 260 to about 1000, wherein said occlusion agent is selected from the group consisting of petrolatum, cetyl ricinoleate and lanolin. Although not fully understood, it appears that poly(alpha-olefin) antiadhesives and occluded antiadhesives work by different mechanisms. Nonetheless, both are effective in reducing the sticky skin sensation associated with high levels of vitamin _B3 compounds. Although mixtures of anti-sticking agents are not excluded, the best results are obtained when the anti-sticking agent is selected from only one of these two types.

Suitable poly(alpha-olefins) as described above can be obtained from 1-alkene monomers having from about 6 to about 14 carbon atoms, preferably from about 6 to about 12 carbon atoms, especially from about 8 to about 12 carbon atoms. The poly(alpha-olefin)s useful in the present invention are preferably hydrogenated poly(alpha-olefin) oligomers. The 1-alkene monomers useful in preparing the poly(alpha-olefin) oligomers of the present invention include 1-hexene, 1-octene, 1-decene, 1-dodecene, 1-tetradecene Alkenes, such as branched isomers of 4-methyl-1-pentene, and combinations thereof. Preferred are oligomers of 1-octene to 1-dodecene or combinations thereof. Polydecene is particularly preferred. Suitable polydecene oils are available from Mobil Chemical Company (P.O. Box 3140, Edison, NJ 08818, USA) under the tradename Puresyn 4 and from BP Amoco (200 E. Randolph Drive, Chicago, IL 60601-7125) under the tradename Silkflo(R) 364 NF is commercially available.

The preferred anti-sticking agent is petrolatum.

carrier

The compositions of the present invention comprise a dermatologically acceptable carrier suitable for topical application to the skin, wherein the essential materials and optional other materials are incorporated into the carrier so that the essential materials and optional components can be delivered to the skin in suitable concentrations. on the skin. The carrier can thus act as a diluent, dispersant, solvent, etc. for the particulate material and active, ensuring their uniform application or distribution at the proper concentration throughout the chosen target.

The topical compositions of the present invention may be formulated in a variety of product forms known in the art. These forms include, but are not limited to, lotions, creams, gels, sprays, ointments and mousses. Particularly preferred carriers are liquid or semi-solid. Preferably the carrier is in the form of a lotion, cream or gel, more preferably of sufficient consistency or yield point to resist deposition of particles. The carrier itself can be inert, or it can have dermatological benefits of its own. The carrier should also be one that is physically and chemically compatible with the essential components described herein, and should not unduly impair stability, efficacy or other use benefits associated with the compositions of the invention.

A preferred carrier contains a dermally acceptable hydrophilic diluent. Suitable hydrophilic diluents include water, organic hydrophilic diluents such as C ₁ -C ₄ monohydric alcohols and low molecular weight diols and polyols, including propylene glycol, polyethylene glycol (e.g., molecular weight 200-600), polypropylene glycol (e.g. molecular weight 425-2025), glycerol, butanediol, 1,2,4-butanetriol, sorbitol, 1,2,6-hexanetriol, ethanol, isopropanol, sorbitol esters, Ethoxylated ethers, propoxylated ethers and mixtures thereof. The diluent is preferably a liquid. Water is a particularly preferred diluent. The compositions preferably comprise at least about 60% hydrophilic diluent.

Preferred carriers are emulsions containing a hydrophilic phase, especially an aqueous phase, and a hydrophobic phase, such as lipids, oils or oily substances. As is well known to those skilled in the art, the hydrophilic phase is dispersed in the hydrophobic phase, or vice versa, forming a hydrophilic or hydrophobic dispersed continuous phase, respectively, depending on the ingredients of the composition. In emulsion technology, the term "dispersed phase" is a well-known term for those skilled in the art and means that the phase exists in the form of small particles or droplets suspended in and surrounded by the continuous phase. The dispersed phase is also called the internal or discontinuous phase. The emulsion can be or comprise (for example in a three-phase or other multi-phase emulsion) an oil-in-water emulsion or a water-in-oil emulsion, such as a water-in-silicone emulsion. A typical oil-in-water emulsion contains about 1% to about 5% (preferably about 1% to about 30%) of a dispersed hydrophobic phase and about 1% to about 99% (preferably about 40% to about 90%) of a continuous hydrophilic phase. Aqueous phase; a typical water-in-oil emulsion contains from about 1% to about 98% (preferably from about 40% to about 90%) of the dispersed hydrophilic phase and from about 1% to about 50% (preferably from 1% to about 30%) continuous hydrophobic phase. Emulsions can also include gel networks, such as G.M. Eccleston, Application of Emulsion Stability Theories to Mobile and Semisolid O/W Emulsions, Cosmetics and Toiletries ( Cosmetics & Toiletries), Vol. 101, Nov. 1996, pp. 73-92, which is incorporated herein by reference. Preferred compositions of the present invention are oil-in-water emulsions.

Preferred compositions have an apparent viscosity of from about 5,000 to about 200,000 mPa.s (centipoise). For example, preferred lotions have an apparent viscosity of from about 10,000 to about 40,000 mPa.s; preferred creams have an apparent viscosity of from about 60,000 to about 160,000 mPa.s. Apparent viscosity may be measured with a Brookfield DV11 RV viscometer, spindle TD, at 5 rpm, or using its equivalent. After the prepared composition is stabilized (generally, the composition is stabilized at 25°C±1°C and ambient pressure for 24 hours after preparation), the composition is subjected to a viscosity measurement. Viscosity measurements were performed on the compositions after 30 seconds of spindle rotation at 25°C ± 1°C.

Generally, the compositions of the present invention are formulated to have a pH of 9.5 or lower, and typically have a pH in the range of from about 4.5 to about 9, more preferably from about 5 to about 8.5.

Some compositions, particularly those containing additional actives such as salicylic acid, require a lower pH for the additional active to be fully effective. Typically, these compositions are formulated to have a pH of from about 2.5 to about 5, more preferably from about 2.7 to about 4.

optional components

The topical compositions of the present invention may contain a variety of optional ingredients so long as these optional ingredients are physically and chemically compatible with the essential components described herein and do not unduly impair compatibility with the compositions of the present invention. Relevant stability, efficacy or other benefits of use. Optional components can be dispersed or dissolved in the vehicle of the composition.

Optional components include emollients, oil absorbers, antimicrobials, binders, buffers, denaturants, cosmetic astringents, external analgesics, film formers, humectants, opacifiers, fragrances, pigments, Skin penetration enhancers, solvents, suspending agents, emulsifiers, detergents, thickeners, solubilizers, waxes, sunscreens, non-sun tanning agents, antioxidants and/or free radical scavengers, chelating agents, Anti-inflammatory agents, peeling/peeling agents, organic hydroxy acids, vitamins, and natural extracts. Non-exclusive examples of these substances are described in Harry's Cosmetology , 7th Edition, Harry and Wilkinson (Hill Publisher, London, 1982); Pharmaceutical Formulations - Dispersion Systems ; Lieberman, Rieger and Banker, Vol. 1 (1988) and Vol. 2 volumes (1989), Marcel Decker Ltd; Chemistry and Manufacture of Cosmetics , 2nd ed., de Navarre (yan Nostrand 962-1965) and Handbook of Cosmetic Science and Technology , 1st ed., Knowlton and Pearce (Elsevier 1993). They can also be used in the present invention.

organic particulate matter

Preferred compositions of the present invention contain organic particulate material having a refractive index of 1.3-1.7 dispersed in the composition and having a volume average particle size in the range of about 5 to about 30 microns, preferably about 8 to 25 microns. Without wishing to be bound by theory, it is believed that the organic particulate particles, having a diameter at least equal to the oil layer produced by the composition of the present invention on the skin, act as a non-greasy emollient, thereby improving overall skin feel and are also effective in counteracting stickiness .

The volume average particle size is determined when the particulate material is in the form of a powder in neat (ie essentially pure) form prior to association with the carrier of the present invention. However, specific methods of measuring particle size may require that the particulate material be dispersed in an inert carrier such as pure oil in order to determine the particle size distribution. Particle size may be determined by any suitable method known in the art, for example by using a Coulter counter or ASTM designation E20-85" Particle Size Analysis Standard for Particulate Matter from 0.2 to 75 microns by Light Microscopy Method (Standard Practice for Particulate Size Analysis of particulate Substances in the Range of 0.2 to 75 Micrometers by Optical Microscopy)", ASTM Volume 14.02, 1993.

The refractive index can be measured by a conventional method. For example, a method for determining the refractive index suitable for use in the present invention is described in J.A. Dean, edited, Lange's Handbook of Chemistry, 14th Edition, McGraw Hill, New York, 1992 Section 9, Refractive Methods. The refractive index is preferably from about 1.35 to about 1.6, a range that closely matches the refractive index of skin.

The compositions of the present invention preferably contain from about 0.1% to about 10%, more preferably from about 0.3% to about 5%, especially from about 0.5% to about 2%, of organic particulate material.

Preferred granular materials are free-flowing, porous materials, especially particles having a spherical shape. Suitable organic particulate materials include polymethylsilsesquioxane (mentioned in the above reference), polyamide, polyethylene, polyacrylonitrile, polyacrylic acid, polymethacrylic acid, polystyrene, polytetrahydroethylene (PTFE) and poly(vinylidene chloride) particles. Copolymers produced from monomers of the aforementioned substances can also be used. Polyamides are preferred, especially nylon. Particularly preferred herein are porous nylon particles having a volume average particle size in the range of about 15 to about 25 microns. Suitable nylon particles are commercially available from Elf Atochem SA (Paris, France) under the trade name Orgasol(R).

The composition may contain other inorganic or organic particulate materials. However, it is preferred that the organic particulate material in the composition of the invention consists essentially of the particulate material described in the section entitled "Organic Particulate Material".

interference pigment

Another preferred component in the compositions of the present invention is a green, platelet-shaped interference pigment substance having a _TiO2 layer thickness of about 120 nm to about 160 nm or an integer multiple thereof. Preferably, the interfering pigment substance contains platelet-shaped mica coated with TiO ₂ . The color of the reflected light differs depending on the thickness of the layer. The interfering pigment material used in the present invention contains at least a portion of the pigment material having a _TiO2 layer thickness of about 120 nm to about 160 nm or integer multiples thereof, so that the pigment itself has an overall green color when applied to the skin due to light reflection of the pigment platelets appearance. Without wishing to be backed by theory, it is believed that the inclusion of low levels of green interference pigments will help counteract red areas in the skin without giving it an unnatural green appearance. In this way, it helps to provide an overall even tone. Interfering pigment substances preferably used in the compositions according to the invention have a TiO ₂ layer thickness of about 150 nm to about 250 nm, preferably about 150 nm. Suitable examples are supplied by Merck under the tradename Timiron(R), especially Timiron(R) Silk Green, or by Mearl under the tradename Flamenco(R), especially Flamenco(R) Satin Green.

Typically, interference pigments are present in an amount from about 0.05% to about 1.5%, preferably from about 0.1% to about 1%, more preferably from about 0.2% to about 0.5%.

Inorganic matting agent

Inorganic matting agents, such as titanium oxide or zinc oxide, are also useful in the compositions of the present invention. When present, matting agents are used at no more than 3% to avoid undesired skin whitening or an unnatural "masked" appearance. Preferred for use in the present invention is titanium dioxide, especially anatase titanium dioxide.

Anatase titanium oxide has a density of about 3.90 g/cm ³ and a tetragonal, cubic close-packed structure. The refractive index of anatase titanium oxide is 2.55. Anatase titanium dioxide is commercially available from Kobo Products, Inc. under the tradename Kobo BTD 11 S2, from Whittaker (Clark, Daniels, South Plainfield, New Jersey, USA) under the product name TiO ₂ 9729, and from Cardre Corporation ( South Plainfield, New Jersey, USA) is commercially available under the tradename Carde 70429.

Matting agents preferred for use in the present invention are coated pigments in view of skin feel, skin appearance and emulsion compatibility. Pigments can be treated with compounds such as amino acids such as lysine, polysiloxanes, lauroyl compounds, collagen, polyethylene, lecithin and ester oils. Preferred matting agents are silicone (silicone) treated pigments such as silicone treated titanium dioxide. First choice, silicone-treated anatase titanium dioxide. The effect of the surface treatment is to modify the anticipation of hydrophobicity so that they are "wettable" in the oil phase of the oil-in-water emulsion.

The total concentration of inorganic matting agents may be from about 0% to about 3%, and preferably from about 0.1% to about 2.5%, preferably from about 0.25% to 2%.

panthenol

A particularly preferred, but optional ingredient in the compositions of the present invention is panthenol. Panthenol is also useful for conditioning the skin, but may additionally provide short-term benefits such as moisturizing properties. Panthenol is preferably used in an amount of 0.1 to about 5%, more preferably about 0.5 to about 3%.

retinoid

Retinoids may optionally be included in the compositions of the present invention. Retinoids are also useful in regulating skin condition.

As used herein, "retinoids" include all natural and/or synthetic analogues of vitamin A or retinol analog compounds having the biological activity of vitamin A in the skin, as well as geometric and stereoisomers of these compounds. things. The retinoid is preferably retinol, retinyl esters (e.g. _C2 - _C22 alkyl esters of retinol, including retinyl palmitate, retinyl acetate, retinyl propionate), retinal and/or retinoic acid (including all trans-retinoic acid and/or 13-cis-retinoic acid) or esters thereof, such as tocopheryl retinoate, preferably retinoids other than retinoic acid. These compounds are well known in the art and are commercially available from a number of sources such as Sigma Chemical Company (St. Louts, MO) and Boerhinger Mannheim (Indianapolis, IN). Other retinoids useful in the present invention are described in US Patent 4,677,120 (issued June 30, 1987 to Parish et al); US Patent 4,885,311 (issued December 5, 1989 to Parish et al); issued to Purcell et al. on June 23, 1992); US Patent 5,124,356 (issued to Purcell et al. on June 23, 1992) and US Patent 34,075 (issued to Purcell et al. on September 22, 1992). Preferred retinoids are retinyl esters such as retinyl palmitate, retinyl acetate and retinyl propionate. Retinyl propionate and retinyl palmitate are preferred.

The compositions preferably contain from about 0.005% to about 2%, more preferably from 0.01% to about 2%, of a retinoid. Retinol is preferably used at about 0.01% - or about 0.15%; retinol esters are preferably used at about 0.01% - about 2% (eg, about 1%); retinoic acid is preferably used at about 0.01% % to about 0.25%; tocopheryl retinoate is preferably used in an amount of about 0.01 to about 2%.

softener

The topical compositions of the present invention comprise from about 1% to about 50%, preferably from about 3% to about 15%, of a dermatologically acceptable emollient. Emollients tend to lubricate the skin, increase the smoothness and suppleness of the skin, prevent or relieve dryness of the skin and/or protect the skin. Softeners are generally oily or waxy substances that are immiscible with water. The high spreading oils and antitack agents of the present invention also function as softeners. Various other suitable softeners are known and can be used in the present invention. Sagarin, Cosmetics , Science and Technology 2nd Edition, Vol. 1, pp. 32-43 (1972) describes many examples of materials suitable as softeners. Illustrative examples of softeners include:

i) straight and branched chain hydrocarbons having from about 7 to about 40 carbon atoms, such as dodecane, squalane, cholesterol, hydrogenated polyisobutene, isohexadecane, and C ₇ -C ₄₀ isoparaffins, which are C ₇ -C ₄₀ branched chain hydrocarbons.

ii) C ₁ -C ₃₀ alcohol esters of C ₁ -C ₃₀ carboxylic acids and C ₂ -C ₃₀ dicarboxylic acids, such as isononyl isononanoate, isopropyl myristate, myristyl propionate, stearyl isopropyl behenate, behenyl behenate, dioctyl maleate, diisopropyl adipate and diisopropyl dilinoleate. These include the aforementioned ester softeners.

iii) Mono-, di- and triglycerides of C ₁ -C ₃₀ carboxylic acids and their ethoxylated derivatives, eg tricaprylic/capric glyceride, PEG-6 tricaprylic/capric glyceride.

iv) Alkylene glycol esters of C ₁ -C ₃₀ carboxylic acids, such as ethylene glycol mono- and propylene glycol mono- and diesters of C ₁ -C ₃₀ carboxylic acids, for example ethylene glycol distearate.

v) C ₁ -C ₃₀ mono- or polyesters of sugars and related substances. These esters consist of a sugar or polyol moiety and one or more carboxylic acid moieties. Depending on the constituent acids and sugars, these esters can be in liquid or solid form at room temperature. Examples thereof include: glucose tetraoleate, galactose tetraoleate of oleic acid, sorbitol tetraoleate, sucrose tetraoleate, sucrose pentaoleate, sucrose hexaoleate, sucrose heptaoleate, Sucrose octaoleate, sorbitan hexaester in which the carboxylate moieties are in a 1:2 molar ratio of palmitoleate and arachidic acid esters and in which the carboxylic acid moieties used for esterification are in a 1:3:4 molar ratio of lauryl Sucrose octaesters of linoleate, linoleate and behenate. Other materials include cottonseed oil or soybean oil fatty acid esters of sucrose. Further examples of such materials can be found in WO 96/16636. A particularly preferred material is the INCI name sucrose polycotton oilate.

vi) Organopolysiloxane oils. The organopolysiloxane oil can be a volatile, nonvolatile or a mixture of volatile and nonvolatile silicones. "Non-volatile" herein means that the polysiloxane is liquid at ambient conditions and has a flash point (at one atmosphere) of greater than about 100°C. Herein, the term "volatile" refers to all other silicone oils. Suitable organopolysiloxanes can be selected from a wide variety of polysiloxanes, covering various volatility and viscosity ranges. Non-volatile polysiloxanes are preferred. Suitable polysiloxanes are disclosed in US Patent 5,069,897 (issued December 3, 1991). Preferred organopolysiloxanes for use in the present invention are selected from the group consisting of polyalkylsiloxanes, alkyl-substituted polydimethylsiloxanes, dimethiconols, polyalkylarylsiloxanes and its mixture. More preferred for use herein are polyalkylsiloxanes and cyclomethicones. Polydimethylsiloxane is preferred among the polyalkylsiloxanes.

vii) Vegetable oils and hydrogenated vegetable oils. Examples of vegetable oils and hydrogenated vegetable oils include safflower oil, castor oil, coconut oil, cottonseed oil, menhaden oil, palm kernel oil, palm oil, peanut oil, soybean oil, rapeseed oil, linseed oil, rice bran oil, pine oil, sesame oil, Sunflower seed oil, partially or fully hydrogenated oils from the aforementioned sources and mixtures thereof.

viii) Animal fats or oils such as cod liver oil, lanolin and their derivatives such as acetylated lanolin and lanolin isopropyl ester. Lanolin oil is preferred.

ix) C ₄ -C ₂₀ alkyl esters of polypropylene glycol, C ₁ -C ₂₀ carboxylic acid esters and di-C ₈ -C ₃₀ alkyl esters of polypropylene glycol can also be used, examples of which include PPG-14 butyl ether, PPG-15 stearyl ether, dioctyl ether, dodecyl octyl ether and mixtures thereof.

moisturizer

A highly preferred optional component is a humectant, especially of the polyol type. Typical polyols include polyalkylene glycols, more preferably alkylene glycols and their derivatives, including propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol and its derivatives, sorbitol, hydroxypropyl sorbitol Sugar alcohol, erythritol, threitol, pentaerythritol, xylitol, glucitol, mannitol, hexanediol, butylene glycol (such as 1,3-butanediol), hexanetriol (such as 1,2,6-hexanetriol), glycerin, ethoxylated glycerin and propoxylated glycerin.

The present invention can also use sodium 2-pyrrolidone-5-carboxylate, guanidine; glycolic acid and glycolate (such as ammonium and quaternary alkyl ammonium); lactic acid and lactate (such as ammonium and quaternary alkyl ammonium); forms of Aloe vera (such as Aloe vera gel); hyaluronic acid and its derivatives (such as salt derivatives, such as sodium hyaluronate); lactamide monoethanolamine; acetamide monoethanolamine; urea; Alcohols; sodium pyroglutamate (NaPCA), water-soluble glyceryl poly(meth)acrylate lubricants (such as Hispagel(R)) and mixtures thereof.

The above-mentioned compounds may be added alone or in combination. Preferred humectants are selected from glycerin, glyceryl polyacrylate, urea and mixtures thereof. Glycerin is preferred and may be used in an amount from about 1% to about 15%, preferably from about 4% to about 14%. It is known in the art that glycerin at these levels can also contribute to a sticky feel. It has been found that the viscosity-reducing benefits of vitamin _B3 compounds achieved by the anti-adhesive agents of the present invention can also be extended to reduce the stickiness or viscosity of glycerin. For lotions or creams intended for use on the body or face, glycerin levels are suitably from about 7% to about 15%, preferably from about 9% to about 14%. For hand lotions or creams, about 4% to about 8% is preferred, and about 5% to about 7% is more preferred.

Particularly preferred preparations of the present invention contain both nicotinamide and glycerin, the total content of nicotinamide and glycerin is about 7% to about 16%, preferably about 9% to about 15%, and for hand-used preparations, the content of nicotinamide and glycerin The total level is preferably from about 8% to about 12%, and for facial and/or body formulations, preferably from about 12% to about 15%.

Emulsifier/Surfactant

The compositions of the present invention preferably contain emulsifiers and/or surfactants to assist in dispersing and suspending the discontinuous phase within the continuous phase. Surfactants are also useful if the product is intended for skin cleansing. For convenience below, emulsifiers are included within the term "surfactant" herein, and "surfactant" is therefore used to broadly refer to surfactants that function as emulsifiers or other surfactants such as skin cleansers. Known or conventional surfactants may be used in the composition provided that the agent is selected to be chemically and physically compatible with the essential components of the composition and to provide the desired dispersion characteristics. Suitable agents include silicone materials, non-silicone materials and mixtures thereof.

The compositions of the present invention preferably contain from about 0.05% to about 15% of a surfactant or mixture of surfactants. The exact surfactant or mixture of surfactants will be selected based on the pH of the composition and the other components present.

Preferred hydrophilic surfactants are nonionic surfactants. Nonionic surfactants useful in the present invention are those that can be broadly defined as condensation products _of long chain alcohols (eg _C8-30 alcohols) with sugar or starch polymers (ie glycosides). These compounds can be represented by the formula (S)nOR, wherein S is a sugar moiety such as glucose, fructose, mannose, and galactose; n is an integer from about 1 to about 1000 and R is a C8-30 alkyl group. Examples of long chain alcohols from which the alkyl group may be provided include decyl alcohol, cetyl alcohol, stearyl alcohol, lauryl alcohol, myristyl alcohol, oleyl alcohol, and the like. Preferred examples of _these surfactants include those wherein S is a glucose moiety, R is a _C8-20 alkyl group, and n is an integer from about 1 to about 9. Commercially available examples of these surfactants include decyl polyglucoside (available as APG 325 CS from Henkel), lauryl polyglucoside (available as APG 600 CS and 625 CS from Henkel), and cetyl-stearyl polyglucoside (available as APG 600 CS and 625 CS from Henkel). Cetearyl polyglucoside (available as Montanov 68 from Seppic).

Other useful nonionic surfactants include condensation products of alkylene oxides with fatty acids (ie, alkylene oxide esters of fatty acids). These substances have the general formula RCO(X)nOH, where R is a C _10-30 alkyl group and X is -OCH ₂ CH ₂ - (ie hexanediol or ethylene oxide) or -OCH ₂ CHCH ₃ - (ie derived from propylene glycol or propylene oxide), n is an integer from about 6 to about 200. Other nonionic surfactants are condensation products of alkylene oxides with 2 moles of fatty acids (ie, alkylene oxide diesters of fatty acids). These materials have the general formula RCO(X)nOOCR, where R is a C _10-30 alkyl group, X is -OCH ₂ CH ₂ - (ie, hexanediol or ethylene oxide) or -OCH ₂ CHCH ₃ - (ie, derived from propylene glycol or propylene oxide), and n is an integer from about 6 to about 100. Other nonionic surfactants are condensation products of alkylene oxides with fatty alcohols (ie, alkylene oxide ethers of fatty alcohols). These substances have the general formula R(X)nOR', where R is a C10-30 alkyl group and X is -OCH ₂ CH ₂ - (ie hexanediol or ethylene oxide) or -OCH ₂ CHCH ₃ - (ie derived from propylene glycol or propylene oxide), and n is an integer from about 6 to about 100, and R' is H or C _10-30 alkyl. Still other non-ionic surfactants are condensation products of alkylene oxides with both fatty acids and fatty alcohols [i.e. where the polyalkylene oxide moiety is esterified at one end with a fatty acid and at the other end with a fatty alcohol etherified (via ether linkage)]. These materials have the general formula RCO(X)nOR', where R and R' are C _10-30 alkyl, and X is -OCH ₂ CH ₂ - (ie, hexanediol or ethylene oxide) or -OCH ₂ CHCH ₃ - (i.e. derived from propylene glycol or propylene oxide), and n is an integer from about 6 to about 100, examples of which include ceteth-6, ceteth-10, ceteth-10, Hexaalkyl polyoxyethylene ether-12, ceteareth-6, ceteareth-10, ceteareth-12, steareth-6, steareth-10, steareth-12, PEG-6 stearate, PEG-10 stearate, PEG-100 Stearate, PEG-12 Stearate, PEG-20 Glyceryl Stearate, PEG-80 Glyceryl Butoleate, PEG-10 Glyceryl Stearate, PEG-30 Glyceryl Cocoate Esters, PEG-80 Glyceryl Cocoate, PEG-200 Glyceryl Butanoate, PEG-8 Dilaurate, PEG-10 Distearate, and mixtures thereof.

Still other useful nonionic surfactants include the polyhydroxy fatty acid amide surfactants which are described in detail in WO 98/04241.

Preferred nonionic surfactants are selected from steareth-2, steareth-21, ceteareth-20, ceteareth-12, sucrose cocoate, steareth-100, PEG-100 stearate and mixtures thereof.

Other nonionic surfactants suitable for use herein include sugar esters and polyesters, alkoxylated sugar esters and polyesters, C ₁ -C ₃₀ fatty acid esters of C ₁ -C ₃₀ fatty alcohols, C ₁ -C ₃₀ Alkoxylated derivatives of C ₁ -C ₃₀ fatty acid esters of fatty alcohols, alkoxylated ethers of C ₁ -C ₃₀ fatty acids, polyglycerol esters of C ₁ -C ₃₀ fatty acids, C ₁ -C of polyols ₃₀ esters, C ₁ -C ₃₀ ethers of polyols, alkyl phosphates, polyoxyalkylene fatty ether phosphates, fatty acid amides, acyl lactylates and mixtures thereof. Non-limiting examples of these silicon-free surfactants include: Polysorbate 20, Macrogol 5 Soy Sterol, Steareth-20, Ceteareth-20, PPG-2 Methyl Glucose Distearate, Cetyl polyoxyethylene ether-10, polysorbate 80, polysorbate 60, glyceryl stearate, sorbitan monolaurate, polyoxyethylene 4 lauryl ether sodium stearate, Polyglyceryl-4-isostearate, Hexyl Laurate, PPG-2 Methylgluconate Distearate, PEG-100 Stearate, and mixtures thereof.

Another class of emulsifiers suitable for use in the present invention are fatty acid ester blends based on a mixture of sorbitan or sorbitol fatty acid esters and sucrose fatty acid esters, the fatty acids in each case being preferably C ₈ -C ₂₄ , More preferably C ₁₀ -C ₂₀ . A preferred fatty acid ester emulsifier is a blend of sorbitan or sorbitol C ₁₆ -C ₂₀ fatty acid esters with sucrose C ₁₀ -C ₁₆ fatty acid esters, especially sorbitan stearate and sucrose Cocoate blend. It is commercially available from ICI under the tradename Arlatone 2121.

Hydrophilic surfactants useful in the present invention may alternatively or additionally include any of a variety of cationic, anionic, zwitterionic and amphoteric surfactants known in the art. See, eg, McCutcheon, Detergents and Emulsifiers , North American Edition (1986), published by Allured Publishing Company; US Patent 5,011,681 (issued April 30, 1991 to Ciotti et al); US Patent 4,421,769 (issued December 20, 1983 to Dixon et al) and US Patent 3,755,560 (issued Aug. 28, 1973 to Dickert et al).

Anionic, amphoteric and zwitterionic surfactants can be used herein, although generally they are more suitable for rinse-off cleansing compositions. Their content is kept below 4%, preferably below 1%. Exemplary anionic surfactants include alkanoyl isethionates (eg, C ₁₂ -C ₃₀ ), alkyl and alkyl ether sulfates and salts thereof, alkyl and alkyl ether phosphates and salts thereof, alkane methyl taurates (eg C ₁₂ -C ₂₀ ) and soaps of fatty acids (eg alkali metal salts, eg sodium or potassium salts). Exemplary amphoteric and zwitterionic surfactants useful in the compositions of the present invention include alkyliminoacetates, iminodialkanoates and aminoalkanoates, imidazolinium salts and ammonium derivatives. Other suitable amphoteric and diionic surfactants are selected from the group consisting of betaines, sultaines, hydroxysultaines, alkyl sarcosinates (eg C ₁₂ -C ₃₀ ) and alkanoyl sarcosinates.

Preferred emulsions of the present invention include silicone-containing emulsifiers or surfactants. A variety of silicone emulsifiers are useful herein. These silicone emulsifiers are typically organically modified organopolysiloxanes, also known to those skilled in the art as silicone surfactants. Useful silicone emulsifiers include dimethicone copolyols. These materials are polydimethylsiloxanes modified to include polyether side chains such as polyethylene oxide chains, polypropylene oxide chains, mixtures of these chains, and polyether chains containing Polyether chains derived from portions of ethylene oxide and propylene oxide. Other examples include alkyl-modified dimethicone copolyols, ie compounds containing _C2 - _C30 pendant side chains. Other useful dimethicone copolyols include those having various cationic, anionic, amphoteric, and zwitterionic side chain moieties.

Thickeners (including thickeners and gelling agents)

The compositions of the present invention may also contain a thickening agent, preferably from about 0.1% to about 5%, more preferably from about 0.1% to about 3%, and most preferably from about 0.25% to about 2%.

Suitable thickeners include cellulose and derivatives such as cellulose, carboxymethyl hydroxyethyl cellulose, cellulose acetate propionate carboxylate, hydroxyethyl cellulose, hydroxyethyl ethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethylcellulose, methylhydroxyethylcellulose, microcrystalline cellulose, sodium cellulose sulfate, and mixtures thereof. Alkyl substituted celluloses are also suitable for use in the present invention. In these polymers, the hydroxyl groups of the cellulose polymer are hydroxyalkylated (preferably hydroxyethylated or hydroxypropylated) to form hydroxyalkylated cellulose, which is then substituted with C10-C30 linear or Branched alkyl groups further modify the cellulose. These polymers are typically ethers of C10-C30 linear or branched chain alcohols and hydroxyalkylcelluloses. Examples of alkyl groups useful in the present invention are selected from the group consisting of stearyl, isostearyl, lauryl, myristyl, cetyl, isocetyl, cocoyl (i.e. the alcohol derived from coconut oil). Alkyl), palmityl, oleyl, linoleyl, linolenic, castoryl, behenyl, and mixtures thereof.

Other useful thickeners include gum arabic, agar, algin, alginic acid, ammonium alginate, pullulan, calcium alginate, calcium carrageenan, carnitine, carrageenan, dextrin, gelatin, Cold Gum, Guar Gum, Guar Hydroxypropyltrimonium Chloride, Hectorite, Hyaluronic Acid, Hydrated Silica, Hydroxypropyl Chitosan, Hydroxypropyl Guar Gum, Karaya gum, seaweed, locust bean gum, natto gum, potassium alginate, potassium carrageenan, propylene glycol alginate, sclerotin gum, sodium carboxymethyl dextran, sodium carrageenan , tragacanth gum, xanthan gum and mixtures thereof. Acrylic acid/ethyl acrylate copolymers and carboxyvinyl polymers commercially available under the tradename Carbopol resins from B.F. Goodrich Company are also useful. Suitable Carbopol resins are described in WO98/22085.

Preferred compositions of the present invention contain a thickener selected from the group consisting of carboxylic acid polymers, cross-linked polyacrylates, polyacrylamides, xanthan gum and mixtures thereof, more preferably selected from polyacrylamide polymers, xanthan Glues and their mixtures. The preferred polyacrylamide is predispersed in a water-immiscible solvent such as mineral oil or the like, which contains a surfactant (HLB about 7 to about 10) to help promote the water dispersibility of the polyacrylamide. Preferred for use in the present invention are nonionic polymers with the CTFA designation polyacrylamide and isoparaffin and lauryl ether-7, which are available from Seppic Corporation under the tradename Sepigel 305.

anti-inflammatory agent

A safe and effective amount of anti-inflammatory agent may be added to the composition of the present invention, preferably about 0.1% to about 5%, more preferably about 0.1% to about 2% of the composition. Anti-inflammatory agents can enhance the skin appearance benefits of the present invention, for example, such agents contribute to a more even and acceptable skin tone or color. The exact amount of anti-inflammatory agent used in the composition will depend on the particular anti-inflammatory agent used, since such agents vary widely in potency.

Anti-inflammatory agents useful in the present invention include steroidal anti-inflammatory agents, such as hydrocortisone; non-steroidal anti-inflammatory drugs (NSAIDS), such as ibuprofen; panthenol and its ether and ester derivatives, such as panthenol Panthenyl ether, panthenyl triacetate; pantothenic acid and its salt and ester derivatives, especially calcium pantothenate; aloe barbadensis, bisabolol, allantoin and compounds of the Glycyrrhizae family (Glycyrrhiza genus/species), Included are glycyrrhetinic acid, glycyrrhizinic acid and derivatives thereof such as salts (eg, ammonium glycyrrhizinate) and esters (stearyl glycyrrhetinate).

Panthenol, pantothenic acid and their ether, ester or salt derivatives and their mixtures are particularly preferred in the present invention; the suitable content is about 0.1-about 5%, preferably about 0.5-about 3%. Panthenol is particularly preferred.

Sunscreens and Sunblocks

The compositions of the present invention may contain a sunscreen. Suitable sunscreens may be organic or inorganic. Particularly preferred sunscreens include butylmethoxydibenzoylmethane, 2-ethylhexyl-p-methoxycinnamate, phenylbenzimidazole sulfonic acid and octocrylene. Inorganic sunscreens include zinc oxide and titanium dioxide. Sunscreens are typically used at levels of from about 1% to about 20%, more typically from about 2% to about 10%. The exact amount will vary depending on the sunscreen chosen and the desired Sun Protection Factor (SPF). An agent may also be added to any of the compositions useful in the present invention to improve the skin substantivity of the compositions, in particular to increase their resistance to water wash-off or rub-off. A preferred agent that provides this benefit is a copolymer of ethylene and acrylic acid. Compositions containing such copolymers are disclosed in US Patent 4,663,157 (Brock, issued May 5, 1987).

Antioxidant/Free Radical Scavenger

Antioxidants/radical scavengers may also be present in the compositions of the present invention. Antioxidants/radical scavengers are particularly useful for providing protection from UV radiation (which can lead to increased desquamation or texture changes of the stratum corneum) and from other environmental agents that cause skin damage. Suitable amounts are from about 0.1% to about 10%, more preferably from about 1% to about 5%, of the composition.

Antioxidants/radical scavengers that can be used are, for example, ascorbic acid (vitamin C) and its salts, ascorbic acid esters of fatty acids, ascorbic acid derivatives (e.g. magnesium ascorbyl phosphate), beta-carotene, tocopherol (vitamin E), tocopherol Sorbate, tocopheryl acetate, other esters of tocopherol, butylated hydroxybenzoic acid and its salts, gallic acid and its alkyl esters, especially propyl gallate, uric acid and its salts and alkyl esters, Sorbic acid and its salts, amines (such as N,N-diethylhydroxylamine, amino-guanidine), sulfhydryl compounds (such as glutathione), dihydroxyfumaric acid and its salts, bioflavonoids, Lysine, Methionine, Proline, SOD, Silymarin, Tea Extract, Grape Skin/Seed Extract, Melanin, and Rosemary Extract. Preferred antioxidants/radical scavengers are selected from tocopheryl acetate, tocopheryl sorbate and other esters of tocopherol, more preferably tocopheryl acetate.

Chelating agent

The inclusion of chelating agents is particularly useful for providing protection from UV radiation (which causes excessive peeling or changes in skin texture) and from other environmental agents that cause skin damage (which can cause skin damage). Suitable amounts are from 0.01% to about 1%, more preferably from about 0.05% to about 5%, of the composition. Examples of chelating agents useful in the present invention are those disclosed in US Patent 5,487,884. Preferred chelating agents for use in the compositions of the present invention are ethylenediaminetetraacetic acid (EDTA), furildioxime and derivatives thereof.

Desquamation agent / peeling agent

A safe and effective amount of desquamation agent can be added in the composition of the present invention, more preferably about 0.1% to about 10%, more preferably about 0.2% to about 5%, and more preferably about 0.5% to about 4% of the composition. %. Desquamation agents can enhance the skin appearance benefits of the present invention. For example, desquamation agents tend to improve the texture (eg, smoothness) of the skin. Various desquamation agents are known in the art and are suitable for use in the present invention, including organic hydroxy acids such as salicylic acid, glycolic acid, lactic acid, 5-octanoyl salicylic acid, hydroxycaprylic acid, hydroxycaprylic acid, and lanolin fatty acids. One suitable desquamation system for use in the present invention comprises a sulfhydryl compound and a zwitterionic surfactant and is described in WO 96/01101. Another desquamation system suitable for use in the present invention comprises salicylic acid and a zwitterionic surfactant and is described in WO95/13048. Salicylic acid is preferred.

skin lightening agent

The compositions of the present invention may also contain a skin lightening agent. When used, the compositions preferably contain from about 0.1% to about 10%, more preferably from about 0.2% to about 5%, still preferably from about 0.5% to about 2%, of a skin lightening agent. Suitable skin lightening agents include those known in the art, including kojic acid, arbutin, ascorbic acid and derivatives thereof, such as magnesium ascorbyl phosphate. Other skin lightening agents suitable for use in the present invention include those described in WO 95/34280 and WO 95/23780.

Preparation of the composition

The compositions of the present invention are generally prepared by conventional methods, such as those known in the art for preparing topical compositions. These methods generally involve mixing the ingredients until the ingredients are brought to a relatively homogeneous state in one or more steps, with or without heating, cooling, vacuuming, and the like.

Conditioning methods for skin conditions

The compositions of the present invention are effective in conditioning mammalian skin conditions, particularly human skin, more particularly hands or other body non-facial skin, including conditioning visible and/or tactile discontinuities in the skin, such as skin texture Visible and/or tactile discontinuities in aspects, especially those associated with skin aging. Conditioning the condition of the skin comprises topically applying to the skin a safe and effective amount of a composition of the present invention. The amount, number of applications and timing of application of the compositions will vary widely depending on the active level of a given composition and the degree of conditioning desired, for example, depending on the degree of aging of the subject's skin and the rate of further aging of the skin.

Compositions of the present invention may be used in various amounts to provide skin appearance and/or sensory benefits. The amount of the composition of the present invention per application is typically from about 0.1 mg/m ² to about 10 mg/m ² in mg composition/cm ² skin. A particularly effective application rate is about 2 mg/m ² . Typical administration is on the order of about once per day, but the frequency of administration can vary from once per week up to three or more per day.

The compositions of the present invention provide a visible improvement in skin condition substantially immediately after application of the composition to the skin. Such immediate improvement includes covering or masking of skin imperfections such as textural discontinuities, including those associated with skin aging such as enlarged pores, and/or providing a more even skin tone or color.

Compositions of the present invention containing actives for chronic regulation of skin condition may also provide visible improvement in skin condition after chronic topical application of the composition. "Chronic topical administration" and the like include continuous topical administration of a composition over an extended period of time during the life of the subject, preferably a period of at least about one week, more preferably a period of at least about one month. Typical administration is on the order of about once a day for the extended period in question, however, the number of administrations may vary from about once a week up to about three or more times a day.

Example

The following examples further describe and demonstrate embodiments within the scope of the present invention. They are given for the purpose of illustration and should not be construed as limiting the invention. Ingredients are given by CTFA designation when applicable. All examples are oil-in-water emulsions prepared by applying conventional formulation techniques. The coated titanium dioxide is incorporated through the oil phase ingredients, while the nylon particles and interference pigments are added through the water phase.

Examples 1-8 are representative hand and body lotions of the present invention Example 1 2 3 4 ingredients %w/w %w/w %w/w %w/w Nicotinamide 2.0 4.0 6.0 2.0 retinyl propionate - 0.2 - - panthenol 1.0 2.0 0.5 0.5 Polyacrylamide & Isoparaffin & Laureth-7 2.0 2.25 2.25 2.0 glycerin 5.0 3.0 7.0 12.0 Allantoin 0.2 0.05 0.1 - Curacao Aloe Vera Gel 0.05 0.075 0.05 - tocopheryl acetate 0.75 0.5 0.5 0.5 cetyl alcohol 2.0 1.0 1.25 0.3 stearyl alcohol 2.0 1.0 1.25 0.5 Docosanol 1.0 1.0 1.25 0.4 Cyclomethicone & Dimethiconol 0.75 0.5 0.50 2.0 Steareth-21 0.6 0.4 0.5 - Steareth-2 0.1 0.08 0.03 - Cetyl-Stearyl Glucoside - - - 0.5 PPG-15 stearyl ether 3.0 2.0 1.00 1.00 Isohexadecane - 7.0 5.0 5.4 Isononyl isononanoate 5.0 - - - SEFA Cottonseed Oleate - - - 1.2 Polydimethylsiloxane (350mm ² s ^-1 ) 0.5 0.0 0.60 -0.60 Disodium EDTA 0.10 0.10 0.10 0.10 Nylon-12 ¹ 1.5 1.0 1.1 2.0 Titanium Dioxide (and) Mica ² 0.75 1.5 1.25 0.25 Polydecene ³ 0 0 0 0 Petrolatum 1.00 4.00 2.00 2.00 Deionized water, flavors, preservatives to 100% to 100% to 100% to 100% Example 5 6 7 8 ingredients %w/w %w/w %w/w %w/w Nicotinamide 2.0 3.0 5.0 3.5 retinyl propionate 0.28 0.10 0.28 0.28 panthenol 1.0 1.5 0.5 0.5 Polyacrylamide & Isoparaffin & Laureth-7 2.0 2.25 2.25 2.0 glycerin 6.0 4.0 7.0 10.0 Allantoin 0.10 0.10 0.10 - Aloe vera 0 0.03 0.07 - tocopheryl acetate 0.50 1.25 0.50 0.50 cetyl alcohol 0.75 1.0 1.25 0.5 stearyl alcohol 1.0 1.5 1.20 0.3 Docosanol 1.00 1.50 1.25 0.4 Steareth-2 0.05 0.05 0.05 - Steareth-21 0.40 0.45 0.50 - Cetyl-Stearyl Glucoside - - - 0.5 PPG-15 stearyl ether 3.0 2.0 1.00 1.00 Isohexadecane 5.0 7.0 - 5.4 Isopropyl isostearate - - 5.0 2.4 Isononyl isononanoate 1.0 - - - SEFA Cottonseed Oleate - - - 1.2 Disodium EDTA 0.10 0.10 0.10 0.10 Nylon-12 ¹ 1.5 1.0 1.1 2.0 Titanium Dioxide (and) Mica ² 0.75 1.5 1.25 - Polydecene ³ 1.00 2.00 1.10 - Petrolatum - - - 2.0 Deionized water, flavors, preservatives to 100% to 100% to 100% to 100%

When applied to the hands of a subject at a rate of 2 mg/ ^cm2 of skin, the above-described embodiments provided substantially immediate improvements in skin appearance, such as reduced visibility of pores and a more even skin tone. Continuous application at the same rate once or twice daily for 3-6 months not only improves substantially immediate appearance, but also improves skin surface texture, including the reduction of fine lines and wrinkles.

Prepare a cream for facial skin according to the following ingredients Example 7 8 ingredients %w/w %w/w Nicotinamide 2.0 3.5 panthenol 1.0 2.0 Polyacrylamide & Isoparaffin & Laureth-7 2.25 2.75 glycerin 10.0 9.0 tocopheryl acetate 0.50 0.75 cetyl alcohol 0.8 1.5 stearyl alcohol 0.6 1.0 PEG-100 stearate 0.1 0.1 stearic acid 0.1 0.1 Sucrose Cocoate and Sorbitan ^Stearate4 1.0 1.0 Dimethicone and Dimethiconol 2.0 4.0 Isohexadecane 3.0 2.0 Isopropyl isostearate 1.5 1.0 SEFA Cottonseed Oleate 0.5 1.0 Disodium EDTA 0.10 0.10 Polymethylsilsesquioxane ⁵ 0.5 1.0 Titanium dioxide 0.2 0.6 Polydecene ³ 1.0 -0 Petrolatum - 3.0 Deionized water, flavors, preservatives to 100% to 100%

¹ Orgasol®2002 EXD NAT COS.

² green interference pigments

³ Silkflo 364 NF by BP Amoco

⁴ Arlatone 2121, produced by ICI

⁵ Tospearl 145a by GE Silicones

Claims (10)

1. A topical leave-on skin care composition comprising: a) 1%-10% vitamin _B3 compound; b) 3%-10% of high spreading oil, selected from: i) branched chain hydrocarbons with a weight average molecular weight of 100-1000, and ii) the liquid ester softener of the following formula I: Formula I wherein R ¹ is selected from H or CH ₃ , R ² , R ³ and R ⁴ are independently selected from C ₁ -C ₂₀ straight chain or branched chain alkyl, and x is an integer from 1 to 20; and iii) mixtures thereof; and c) a dermatologically acceptable carrier, It is characterized in that the composition contains 0.3%-4% anti-tack agent selected from poly(alpha-olefin) and petrolatum with molecular weight of 260-1000. 2. The composition of claim 1, wherein the vitamin _B3 compound is niacinamide. 3. The composition of claim 1, wherein the branched chain hydrocarbon is isohexadecane. 4. The composition of claim 1, wherein the anti-tack agent is polydecene. 5. The composition of claim 1, wherein the anti-tack agent is petrolatum. 6. The composition of any one of claims 1-5, further comprising 4% to 14% glycerol. 7. The composition of claim 1, further comprising 0.1%-10% of organic particulate matter having a refractive index of 1.3-1.7, said organic particulate matter being dispersed in the composition and having a volume average particle size in the range of 5-30 μm. 8. The composition of claim 7, wherein the organic particulate material particles are porous nylon particles having a volume average particle size in the range of 15-25 [mu]m. 9. Use of polydecene for reducing the viscosity of a leave-on skin care composition as claimed in claim 1. 10. Use of petrolatum for reducing the viscosity of a leave-on skin care composition according to claim 1.