HK1118452A - Regulation of mammalian keratinous tissue using personal care compositions comprising tetrahydrocurcumin - Google Patents

Description

Regulation of mammalian keratinous tissue using personal care compositions comprising tetrahydrocurcumin

Technical Field

The present invention relates to personal care compositions comprising skin and hair care actives such as tetrahydrocurcumin. The compositions are useful for regulating the condition of keratinous tissue in a mammal in need of such treatment, and are particularly useful for lightening the skin.

Background

Many personal care products currently available to consumers are aimed at improving the health and physical appearance of keratinous tissue, such as skin, hair, and nails. Most of these products are concerned with delaying, minimizing or even eliminating skin wrinkling and histological changes typically associated with skin aging or environmental damage to human skin. However, there remains a need for cosmetic agents that prevent, retard, and/or treat uneven skin color by acting as cosmetic agents that lighten the skin or reduce pigmentation.

Mammalian keratinous tissue, especially human skin and hair, is subject to attack by a number of extrinsic and intrinsic factors. Such extrinsic factors include ultraviolet radiation, environmental pollution, wind, sun, infrared radiation, low humidity, harmful surfactants, abrasives, and the like. Intrinsic factors, on the other hand, include chronological age and other biochemical changes in the skin. Whether extrinsic or intrinsic, they result in the development of significant signs of skin damage. Typical skin lesions include naturally occurring thinning of the skin with increasing age. As the skin becomes thinner, the cells and blood vessels supplying the skin decrease and, in addition, the dermal-epidermal junction becomes flatter, which results in a weaker mechanical resistance of this junction. See, for example, "The Aging of Skin" by Oikarinen: chronographing Versus Photoaging "(photomutanol. photomed., volume 7, pages 3 to 4, 1990). Other damage or changes seen on aged or damaged skin include fine lines, wrinkles, hyperpigmentation, sallowness, sagging, dark under-eye circles, puffy eyes, enlarged pores, reduced turnover rate, and abnormal desquamation or scaling. Other injuries that result from extrinsic and intrinsic factors include significant dead skin (i.e., shavings, flakes, roughness). For hair, these extrinsic and intrinsic factors can lead to hair bleaching, hair splitting, thinning, roughness, hair loss, reduced hair growth rate, among other problems. Thus, there is a need for products and methods that seek to improve the condition of these keratinous tissues.

Summary of The Invention

Applicants have discovered that topical compositions comprising certain actives are useful for providing prophylactic and therapeutic treatment of keratinous tissue conditions, particularly skin lightening.

In accordance with a preferred embodiment, there has now been provided a personal care composition comprising tetrahydrocurcumin; a safe and effective amount of at least one additional skin and/or hair care active; and a dermatologically acceptable carrier. The active substance is selected from the group consisting of: sugar amine, vitamin B₃Retinoids, hydroquinone, peptides, phytosterols, dialkanoyl hydroxyproline, hexamidine, salicylic acid, n-acyl amino acid compounds, sunscreen actives, water soluble vitamins, oil soluble vitamins, hesperetin, mustard seed extract, glycyrrhizic acid, glycyrrhetinic acid, carnosine, Butylated Hydroxytoluene (BHT) and Butylated Hydroxyanisole (BHA), menthyl anthranilate, cetylpyridinium chlorideOnium, ergothioneine, vanillin or derivatives thereof, diethylhexyl syringylidenemalonate, melanotropin, sterol ester, dehydroacetic acid, idebenone, yeast extract, β -glucan, α -glucan, salts thereof, derivatives thereof, precursors thereof, and/or combinations thereof.

In accordance with another preferred embodiment, a personal care composition has now been provided. The composition comprises at least one antioxidant compound, at least one tyrosinase inhibiting compound, at least one trypsin inhibiting compound, at least one anti-inflammatory compound, and at least one nitric oxide scavenging compound.

In accordance with another preferred embodiment, an article of commerce has now been provided. The article of commerce comprises a personal care composition; at least one of said personal care compositions; a package for the personal care composition; and advertising material associated with the personal care composition. The advertising material includes indicia and/or images that convey the following information: topical application of personal care compositions can improve the skin tone or skin color of a person. The personal care composition comprises tetrahydrocurcumin and at least one sunscreen active.

The present invention also relates to methods for regulating the condition of mammalian keratinous tissue, wherein each of said methods comprises the step of topically applying to the keratinous tissue of a mammal in need of such treatment, a safe and effective amount of a personal care composition according to the present invention.

Detailed Description

All percentages and ratios used herein are by weight of the total composition and all measurements made are at 25 ℃, unless otherwise specified.

The compositions of the present invention can comprise, consist essentially of, or consist of the essential components and optional ingredients described herein. As used herein, "consisting essentially of means that the composition or component may include additional ingredients, as long as the additional ingredients do not materially alter the basic and novel characteristics of the claimed compositions or methods.

The term "keratinous tissue" as used herein refers to stratum corneum-containing layers as the outermost protective covering for mammals, including, but not limited to, skin, hair, toenails, fingernails, cuticles, hooves, and the like.

The term "topical application" as used herein means the application or application of the composition of the present invention to the surface of keratinous tissue.

The term "dermatologically acceptable" as used herein means that the compositions or components are suitable for use in contact with human keratinous tissue without undue toxicity, incompatibility, instability, allergic response, and the like.

As used herein, the term "safe and effective amount" means an amount of a compound or composition sufficient to significantly produce a positive benefit, preferably a positive keratinous tissue appearance or feel benefit, including the benefits disclosed herein, individually or in combination, while being low enough to avoid serious side effects (i.e., to provide a reasonable benefit to risk ratio, within the scope of sound judgment of the skilled artisan).

The term "post-inflammatory hyperpigmentation" as used herein refers to the change in melanin content in response to an inflammatory event (e.g., acne, abrasion, insect sting or biting, sun exposure, etc.), which is particularly evident in subjects with dark skin.

The term "hyperpigmentation" as used herein refers to an area of the skin (e.g., an eyespot, age spot, etc.) in which the pigmentation is greater than that of the adjacent areas of the skin.

The term "desquamation, desquamation and/or renewal" as used herein refers to the removal of the outer layers of the stratum corneum, including the stratum corneum.

As used herein, the term "oily and/or shiny appearance" means that mammalian skin having a smooth appearance tends to exhibit the secretion of oil, sebum, and/or sweat from the respective glandular source.

The term "sagging" as used herein refers to the condition of the skin, such as sagging, which is caused by the loss, destruction, alteration and/or abnormality of the skin elastin.

The terms "smooth" and "softening" as used herein refer to altering the surface of keratinous tissue to improve tactile feel.

The term "sallowness" as used herein refers to the condition of ashen, yellowish skin color resulting from loss, destruction, alteration, and/or abnormality of skin components to discolor them (e.g., yellow color) due to, for example, protein glycation and lipofuscin accumulation or peripheral blood flow reduction typically associated with skin aging.

The compositions of the present invention are useful for topical application and for regulating keratinous tissue condition. Regulation of keratinous tissue condition, particularly human skin condition, is often desirable because intrinsic and/or extrinsic factors can induce or cause various conditions of the body. For example, "modulating a skin condition" includes prophylactic and/or therapeutic modulation, and may include one or more of the following benefits: thickening (i.e., constructing the epidermal and/or dermal layers and/or subcutaneous layers of the skin such as fat and muscle, and, where appropriate, the cuticle layer of the nails and hair shafts) to reduce atrophy (e.g., of the skin), increase the curling of the dermal-epidermal border, reduce non-melanin skin discoloration such as under-eye puffiness, blotches (e.g., uneven redness resulting from, e.g., rosacea) (hereinafter referred to as erythema) and sallowness (grayish or yellow), reduce discoloration resulting from telangiectasia or spider vessels, reduce discoloration resulting from melanin (e.g., eye spots, age spots, uneven pigmentation) and other chromophores in the skin (e.g., lipofuscin, protein cross-linking such as those that occur with glycation, etc.). Prophylactic modulation, as used herein, includes delaying, minimizing, and/or preventing visible and/or tactile discontinuities in the skin (e.g., visible or perceived in the skin of irregular textures, fine lines, wrinkles, sagging, stretch marks, cellulite, puffy eyes, and the like). Therapeutic modulation, as used herein, includes ameliorating (e.g., reducing, minimizing, and/or eliminating) discontinuities in the skin. Regulating skin condition includes improving skin appearance and/or feel.

The term "regulating skin condition" as used herein is intended to include regulation of the above signs, regardless of the mechanism of origin.

The term "indicia" as used herein refers to identifying indicia, including words and/or graphics.

The term "image" as used herein refers to a photograph, illustration, and/or other pictorial representation of a mammal or subject.

As used herein, the term "package" refers to a structure or material that is at least partially disposed on or around a personal care composition when the product is disclosed in the public. By "primary package" is meant any container, including its housing, pump, lid or other external item, in which the composition is in direct contact. And "secondary package" means any additional material associated with the primary package, such as a container, e.g., a box or polymeric sleeve, that at least partially surrounds, contains, or contacts the primary package.

The term "advertising material" as used herein refers to a tangible medium of expression that, by itself or with the aid of a peripheral device, provides a person with an understanding of the presence of, or indication of the quality or advantage of, an associated personal care composition.

The composition of the present invention comprising essential components and optional components thereof will be described in detail hereinafter.

Components

Tetrahydrocurcumin

The present invention comprises a safe and effective amount of Tetrahydrocurcumin (THC), its derivatives such as esters or ethers, and combinations thereof. Preferably, the composition comprises from about 0.01% to about 10%, more preferably from about 0.1% to about 5%, even more preferably from about 0.25% to about 3%, by weight of the composition, of the tetrahydrocurcumin compound.

Oxygen radicals are generated in the skin as a result of many stimuli, such as exposure to ultraviolet light and irritants. The above-mentioned radicals may also be produced as byproducts of general cellular or tissue metabolism. The oxygen radicals can stimulate pigment cells (melanocytes) to increase melanin production. Curcuminoids (such as THC) have antioxidant properties, which allow their clearance before oxygen radicals stimulate melanocytes.

Protein tyrosinases are enzymes involved in the conversion of the amino acid tyrosine into DOPA (dihydroxyphenylalanine) which is then further converted into other intermediates and polymerized into skin melanin. Partial or complete inhibition of tyrosinase delays or prevents, respectively, melanin formation, resulting in a brighter skin tone (e.g., reduced depth of hyperpigmented spots). Curcuminoids (e.g., THC) also inhibit tyrosinase.

Other curcuminoids useful in the present invention include curcumin, tetrahydrodemethoxycurcumin, tetrahydrobisdemethoxycurcumin, derivatives thereof such as esters and ethers, and combinations thereof. The curcuminoids (e.g. THC) may be of natural or synthetic origin. Preferably, in the present invention, tetrahydrocurcumin can be used alone, or in combination with tetrahydrodemethoxycurcumin, and/or in combination with tetrahydrobisdemethoxycurcumin. Preferred derivatives are esters, especially tetrahydrocurcumin diacetate, and/or combinations thereof with tetrahydrocurcumin, and/or combinations thereof with tetrahydrodemethoxycurcumin, and/or combinations thereof with tetrahydrobisdemethoxycurcumin, and/or combinations thereof with esters, especially tetrahydrodemethoxycurcumin diacetate and/or tetrahydrobisdemethoxycurcumin diacetate.

Additional skin and/or hair care actives

The present invention comprises a safe and effective amount of at least one additional skin and/or hair care active. These skin and/or hair care activesThe substance is selected from the group consisting of: sugar amine, vitamin B₃Retinoids, hydroquinone, peptides, phytosterols, dialkanoyl hydroxyproline, hexamidine, salicylic acid, n-acyl amino acid compounds, sunscreen actives, water soluble vitamins, oil soluble vitamins, hesperetin, mustard seed extract, glycyrrhizic acid, glycyrrhetinic acid, carnosine, Butylated Hydroxytoluene (BHT) and Butylated Hydroxyanisole (BHA), menthyl anthranilate, cetylpyridinium chloride, ergothioneine, vanillin or derivatives thereof, diethylhexyl syringylidenemalonate, melatoninerostatin, sterol esters, idebenone, dehydroacetic acid, yeast extracts (e.g., Pitera, beta-hydroxy-proline), and mixtures thereof^®) Beta-glucan, alpha-glucan, salts thereof, derivatives thereof, precursors thereof, and/or combinations thereof. Further description of some of these additional actives is provided below.

The skin and/or hair care actives of the present invention may be used to lighten skin. Lightening skin can occur by a variety of mechanisms, including antioxidant mechanisms, trypsin inhibition, anti-inflammatory mechanisms, nitric oxide scavenging, tyrosinase inhibition, and the like. Thus, compounds that exist in these mechanisms have the potential to lighten skin.

1. Sugar amine (amino sugar)

The compositions of the present invention optionally comprise a safe and effective amount of a sugar amine, also known as an amino sugar. Sugar amine compounds useful in the present invention are described in PCT publication WO 02/076423 and U.S. patent 6,159,485.

The composition preferably comprises from about 0.01% to about 15%, more preferably from about 0.1% to about 10%, even more preferably from about 0.5% to about 5%, by weight of the composition, of a sugar amine.

Sugar amines are synthetic or natural in origin and can be used as pure compounds or mixtures of compounds (e.g., extracts derived from natural sources or mixtures of synthetic materials). Glucosamine is commonly found in many shellfish and can also be obtained from fungal sources. The term "sugar amine" as used herein includes isomers and tautomers of the above and salts thereof (e.g., HCl salt), and is commercially available from Sigma chemical co.

Examples of sugar amines useful in the present invention include glucosamine, N-acetylglucosamine, glucosamine sulfate, mannosamine, N-acetylmannosamine, galactosamine, N-acetylgalactosamine, isomers (e.g., stereoisomers) thereof, and salts (e.g., HCl salt) thereof. Preferred for use herein are glucosamine, especially D-glucosamine and N-acetylglucosamine, especially N-acetyl-D-glucosamine.

2. Vitamin B₃

The compositions of the present invention may include a safe and effective amount of vitamin B₃A compound is provided. Vitamin B₃The compounds are particularly useful for regulating skin conditions, as described in U.S. Pat. No. 5,939,082. Preferably, the composition comprises from about 0.01% to about 50%, more preferably from about 0.1% to about 20%, even more preferably from about 0.5% to about 10%, still more preferably from about 1% to about 7%, even more preferably from about 2% to about 5%, by weight of the composition, of vitamin B₃A compound is provided.

"vitamin B" as used herein₃Compound "refers to a compound having the formula:

wherein R is-CONH₂(i.e., niacinamide), -COOH (i.e., nicotinic acid), or-CH₂OH (i.e., nicotinyl alcohol); derivatives thereof; and salts of any of the foregoing.

The aforementioned vitamin B₃Exemplary derivatives of the compounds include nicotinic acid esters, including non-vasodilating esters of nicotinic acid (e.g., tocopherol nicotinate, tetradecyl nicotinate).

Suitable vitamin B₃Examples of compounds are well known in the art and are commercially available from a variety of sources (e.g., Sigma Chemical Company, ICN Biomedicals, inc., and aldrich Chemical Company). Vitamin B preferably usable in the present invention₃The compound is niacinamide.

3. Retinoids

The compositions of the present invention may comprise a safe and effective amount of a retinoid such that the resulting compositions are safe and effective for regulating keratinous tissue condition, preferably for regulating visible and/or tactile discontinuities of the skin, and more preferably for regulating signs of skin aging. The composition preferably comprises from about 0.001% to about 10%, more preferably from about 0.005% to about 2%, even more preferably from about 0.01% to about 1%, and still more preferably from about 0.01% to about 0.5%, by weight of the composition, of a retinoid. The optimum concentration to use in the composition will depend on the particular retinoid desired, as their efficacy varies considerably.

As used herein, "retinoid" includes all natural and/or synthetic analogs of vitamin A or retinol-like compounds that possess the biological activity of vitamin A in the skin, as well as geometric isomers and stereoisomers of such compounds. The retinoid is preferably selected from retinol, retinol esters (e.g., C of retinol)₂-C₂₂Alkyl esters including retinyl palmitate, retinyl acetate, retinyl propionate), retinal and/or retinoic acid (including all-trans retinoic acid and/or 13-cis retinoic acid), or mixtures thereof. More preferably, the retinoid is a retinoid other than retinoic acid. Preferred retinoids are retinol, retinyl palmitate, retinyl acetate, retinyl propionate, retinal and combinations thereof. More preferably retinyl propionate, even more preferably in an amount of from about 0.1% to about 0.3%.

4. Peptides

The compositions of the present invention may comprise a safe and effective amount of peptides, including, but not limited to, dipeptides, tripeptides, tetrapeptides, pentapeptides, and hexapeptides, and combinations thereofAnd (3) derivatives. The composition preferably comprises about 1 x 10 by weight of the composition^-6% to about 20%, more preferably about 1X 10^-6% to about 10%, even more preferably about 1X 10^-5% to about 5% peptide.

The term "peptide" as used herein refers to peptides comprising ten or fewer amino acids and their derivatives, isomers, and complexes with other species such as metal ions (e.g., copper, zinc, manganese, magnesium, etc.). As used herein, peptides refer to both naturally occurring and synthetic peptides. Also useful in the present invention are naturally occurring and commercially available peptide-containing compositions. More preferred peptides are the dipeptide carnosine (β -alanine-histidine), the tripeptide glycine-histidine-lysine, the pentapeptide lysine-threonine-lysine-serine, lipophilic derivatives of the peptides, and metal complexes of the above, such as copper complexes of the tripeptide histidine-glycine (also known as Iamin). A preferred dipeptide derivative is palmitoyl-lysine-threonine. A preferred commercially available composition comprising a tripeptide derivative is Biopeptide CL^®It contains 100ppm palmitoyl-glycine-histidine-lysine and is commercially available from Sederma. A preferred commercial composition comprising a pentapeptide derivative is Matrixyl^®It contains 100ppm palmitoyl-lysine-threonine-lysine-serine, and is commercially available from Sederma.

5. Plant sterol

The topical compositions of the present invention may comprise a safe and effective amount of one or more phytosterols selected from the group consisting of: beta-sitosterol, campesterol, brassicasterol, delta 5-avenasterol, lupeol, alpha-spinasterol, stigmasterol, derivatives, analogs thereof, and combinations thereof. More preferably, the phytosterol is selected from the group consisting of beta-sitosterol, campesterol, brassicasterol, stigmasterol, derivatives thereof, and combinations thereof. More preferably, the phytosterol is stigmasterol.

Phytosterols are synthetic or natural in origin and may be used as compounds, either pure per se or as mixtures of compounds (e.g., extracts from natural sources). Phytosterols are typically present in the unsaponifiable fraction of vegetable oils and fats, and they are obtained as free sterols, acetylated derivatives, sterol esters, ethoxylated or glycoside derivatives. More preferably, the phytosterol is a free sterol. The term "phytosterol" as used herein includes isomers and tautomers of the above and is commercially available from Aldrich Chemical Company, Sigma Chemical Company, and Cognis.

The phytosterols are preferably present in the compositions of the present invention at a level of from about 0.0001% to about 25%, more preferably from about 0.001% to about 15%, even more preferably from about 0.01% to about 10%, still more preferably from about 0.1% to about 5%, even more preferably from about 0.2% to about 2%, by weight of the composition.

6. Hexamidine

Hexamidine compounds useful in the present invention correspond to those having the following chemical structure:

wherein R is¹And R²Including organic acids (e.g., sulfonic acids, etc.).

Preferably, hexamidine is present in the compositions of the present invention at a level of from about 0.0001% to about 25%, more preferably from about 0.001% to about 10%, more preferably from about 0.01% to about 5%, even more preferably from about 0.02% to about 2.5%, by weight of the composition.

The topical compositions of the present invention may optionally contain a safe and effective amount of one or more hexamidine compounds, their salts and their derivatives. As used herein, hexamidine derivatives include all isomers and tautomers of hexamidine compounds, including but not limited to organic and inorganic acids, such as, for example, sulfonic acidsAcids, carboxylic acids, and the like. Preferably, the hexamidine compound comprises hexamidine dihydroxyethyl sulfonate, which is available under the trade name Elestab^®HP100 is commercially available from laboratory Serobiologiques.

7. Dialkanoyl hydroxyproline compounds

The dialkanoyl hydroxyproline compounds of the present invention correspond to those having the following chemical structure:

wherein R is¹Includes H, X, C₁-C₂₀A linear or branched alkyl group,

x comprises a metal (Na, K, Li, Mg, Ca) or an amine (DEA, TEA);

R²comprising C₁-C₂₀A linear or branched alkyl group;

R³comprising C₁-C₂₀Straight or branched chain alkyl.

The topical compositions of the present invention may contain a safe and effective amount of one or more dialkanoyl hydroxyproline compounds, as well as their salts and derivatives. In the compositions of the present invention, the dialkanoyl hydroxyproline compounds are preferably present in an amount of from about 0.01% to 10%, more preferably from about 0.1% to 5%, even more preferably from about 0.1% to 2% by weight of the composition.

Suitable derivatives include, but are not limited to, esters such as aliphatic esters, including, but not limited to, tripalmitoyl hydroxyproline and dipalmitoyl acetyl hydroxyproline. A particularly useful compound is dipalmitoyl hydroxyproline. Dipalmitoyl hydroxyproline as used herein includes all isomers and tautomers of the above and is under the tradename Sepilift DPHP^®Commercially available from Seppic, inc. Further discussion of dipalmitoyl hydroxyproline may be found inSee PCT publication WO 93/23028. The dipalmitoyl hydroxyproline is preferably the triethanolamine salt of dipalmitoyl hydroxyproline.

8. Salicylic acid compounds

The topical compositions of the present invention may contain a safe and effective amount of a salicylic acid compound, its ester, its salt, or combinations thereof. In the compositions of the present invention, the salicylic acid compound preferably comprises from about 0.0001% to about 25%, more preferably from about 0.001% to about 15%, even more preferably from about 0.01% to about 10%, still more preferably from about 0.1% to about 5%, even more preferably from about 0.2% to about 2%, by weight of the composition, of salicylic acid.

N-acylamino acid compounds

The topical compositions of the present invention may contain a safe and effective amount of one or more N-acyl amino acid compounds. The amino acid may be any amino acid known in the art. The N-acyl amino acid compounds of the present invention correspond to the following structure:

wherein R can be hydrogen, alkyl (substituted or unsubstituted, branched or straight chain), or a combination of alkyl and aryl. A list of possible side chains of amino acids known in the art is described in "Biochemistry" by Stryer published in 1981 by w.h.freeman and Company. R¹C which may be saturated or unsaturated, linear or branched, substituted or unsubstituted₁To C₃₀An alkyl group; substituted or unsubstituted aryl; or mixtures thereof.

The N-acylamino acid compound is preferably selected from the group consisting of N-acylphenylalanine, N-acyltyrosine, isomers thereof, salts thereof, and derivatives thereof. The amino acids may be D or L isomers, or mixtures thereof. The N-acylphenylalanine corresponds to the formula:

wherein R is¹May be C₁To C₃₀Saturated or unsaturated, linear or branched, substituted or unsubstituted alkyl groups of (a); a substituted or unsubstituted aromatic group; or mixtures thereof.

The N-acyl tyrosine conforms to the following structure:

wherein R is¹May be C₁To C₃₀Saturated or unsaturated, linear or branched, substituted or unsubstituted alkyl groups of (a); a substituted or unsubstituted aromatic group; or mixtures thereof.

Particularly useful as cosmetic agents for evening local skin color (lightening skin or reducing pigmentation) is N-undecylenoyl-L-phenylalanine. This reagent belongs to the broad class of N-acyl phenylalanine derivatives, the acyl of which is the C11 monounsaturated fatty acid moiety, and the amino acid is the L-isomer of phenylalanine. N-undecylenoyl-L-phenylalanine corresponds to the following structure:

N-undecylenoyl-L-phenylalanine as used herein may be sold under the trade name Sepiwhite^®Commercially available from SEPPIC.

In the compositions of the present invention, the N-acyl amino acids are preferably present at a level of from about 0.0001% to 25%, more preferably from about 0.001% to 10%, more preferably from about 0.01% to 5%, and even more preferably from about 0.02% to 2.5% by weight of the composition.

10. Sunscreen active

The subject compositions may optionally comprise a sunscreen active. As used herein, "sunscreen actives" include sunscreens and physical sunblocks. Suitable sunscreen actives may be organic or inorganic.

There are a variety of conventional sunscreen actives that are suitable for use herein. A number of suitable active substances are disclosed by Sagarin et al in chapter VIII of the "cosmetics science and Technology" (1972), starting from page 189 and onwards. Particularly suitable sunscreens are 2-ethylhexyl p-methoxycinnamate (commercially available under the trade name PARSOL MCX), 4' -tert-butyl methoxydibenzoylmethane (commercially available under the trade name PARSOL 1789), 2-hydroxy-4-methoxybenzophenone, octyldimethyl-p-aminobenzoic acid, behenyl trioleate, 2-dihydroxy-4-methoxybenzophenone, ethyl 4- (di (hydroxypropyl) aminobenzoate, 2-ethylhexyl 2-cyano-3, 3-diphenylacrylate, 2-ethylhexyl salicylate, glyceryl p-aminobenzoate, 3, 5-trimethylcyclohexylsalicylate, methyl anthranilate, p-dimethylaminobenzoic acid or aminobenzoate, 2-ethylhexyl p-dimethylaminobenzoate, ethylhexyl p-dimethylaminobenzoate, 2-phenylbenzimidazole-5-sulfonic acid, 2- (p-dimethylaminophenyl) -5-sulfonic acid benzoxazole acid, octocrylene, zinc oxide, titanium dioxide, and mixtures of these compounds.

Preferred organic sunscreen actives for use in the compositions of the present invention are 2-ethylhexyl p-methoxycinnamate, butyl methoxydibenzoylmethane, 2-hydroxy-4-methoxybenzophenone, 2-phenylbenzimidazole-5-sulfonic acid, octyl dimethyl p-aminobenzoic acid, octocrylene, zinc oxide, titanium dioxide, and mixtures thereof. Particularly preferred sunscreen actives include 4, 4' -t-butyl methoxydibenzoylmethane, 2-ethylhexyl p-methoxycinnamate, phenylbenzimidazole sulfonic acid, octocrylene, zinc oxide and titanium dioxide, and mixtures thereof.

The sunscreen actives are preferably present at levels of from about 1% to about 20%, more preferably from about 2% to about 10%, by weight of the composition. The exact amount will depend on the sunscreen selected and the desired Sun Protection Factor (SPF).

11. Water-soluble vitamins

The compositions of the present invention may contain a safe and effective amount of one or more water-soluble vitamins. Examples of water-soluble vitamins include, but are not limited to, water-soluble forms of vitamin B (e.g., vitamin B5 and vitamin B6 (e.g., pyridoxine)), vitamin B derivatives, vitamin C (e.g., ascorbyl glucoside), vitamin C derivatives (e.g., magnesium ascorbyl phosphate, sodium ascorbyl phosphate, and ascorbyl palmitate), vitamin K derivatives, provitamins thereof such as panthenol, and mixtures thereof. When a vitamin compound is present in the compositions of the present invention, the compositions preferably comprise from about 0.0001% to about 50%, more preferably from about 0.001% to about 10%, still more preferably from about 0.01% to about 8%, still more preferably from about 0.1% to about 5%, by weight of the composition, of the vitamin compound.

12. Oil-soluble vitamins

The compositions of the present invention may contain a safe and effective amount of one or more oil-soluble vitamins. Examples of oil soluble vitamins include, but are not limited to, oil soluble forms of vitamin D, vitamin D derivatives, vitamin E (e.g., vitamin E acetate), vitamin E derivatives, their provitamins such as panthenol, and mixtures thereof. When an oil-soluble vitamin compound is included in the compositions of the present invention, the compositions preferably comprise from about 0.0001% to about 50%, more preferably from about 0.001% to about 10%, still more preferably from about 0.01% to about 8%, and still more preferably from about 0.1% to about 5%, by weight of the composition, of the oil-soluble vitamin compound.

13. OrangePepsin

The compositions of the present invention may contain a safe and effective amount of hesperetin. The hesperetin in the composition is preferably glucosyl hesperetin which is a derivative thereof. Preferably, the composition comprises from about 0.01% to about 10%, more preferably from about 0.1% to about 5%, even more preferably from about 0.5% to about 3%, by weight of the composition, of the hesperetin compound.

Hesperetin and glucosyl hesperetin are flavonoids. Oxygen radicals are generated in the skin as a result of many stimuli, such as exposure to ultraviolet light and irritants. The above-mentioned radicals may also be produced as byproducts of general cellular or tissue metabolism. The oxygen radicals can stimulate pigment cells (melanocytes) to increase melanin production. Hesperetin and glucosyl hesperetin have antioxidant properties so that they can be eliminated before oxygen radicals stimulate melanocytes.

Protein tyrosinases are enzymes involved in the conversion of the amino acid tyrosine into DOPA (dihydroxyphenylalanine) which is then further converted into other intermediates and polymerized into skin melanin. Partial or complete inhibition of tyrosinase delays or prevents, respectively, melanin formation, resulting in a brighter skin tone (e.g., reduced depth of hyperpigmented spots). Hesperetin and glucosyl hesperetin also inhibit tyrosinase.

14. Glycyrrhizic acid

The compositions of the present invention may comprise a safe and effective amount of glycyrrhizic acid and/or its salts. Preferably, the composition comprises from about 0.01% to about 10%, more preferably from about 0.05% to about 5%, even more preferably from about 0.1% to about 3%, by weight of the composition, of the glycyrrhizic acid compound. Glycyrrhizic acid is a component of licorice extract.

Glycyrrhizic acid is an anti-inflammatory agent. Inflammatory mediators or cytokines can stimulate pigment cells (melanocytes) to produce melanin. Thus, inflammatory conditions such as ultraviolet injury, acne, ingrown hair, insect bites, abrasions, and the like will provoke so-called post-inflammatory hyperpigmentation. Although ultraviolet light is the primary inducer of all types of skin pigmentation, in particular, the pigments produced by other inflammatory stimuli (acne, etc.) will promote pigmentation in the skin of dark-skinned individuals (e.g., spain, asian). Inhibition of inflammation with anti-inflammatory agents will reduce pigmentation.

Glycyrrhizic acid is also believed to be a scavenger of nitric oxide. Nitric Oxide (NO) is a stimulant of pigmentation. Use of nitric oxide scavengers (substances that react with nitric oxide to prevent it from stimulating pigmented cells) will reduce pigmentation.

Glycyrrhizic acid is also known as glycyrrhizin, glycyrrhizin or glycyrrhizin.

15. Glycyrrhetinic acid

The composition of the present invention may contain a safe and effective amount of glycyrrhetinic acid and/or its salts. Preferably, the composition comprises from about 0.01% to about 10%, more preferably from about 0.05% to about 5%, even more preferably from about 0.1% to about 3%, by weight of the composition, of the glycyrrhetinic acid compound. Glycyrrhetinic acid is a component of licorice extract.

Glycyrrhetinic acid is also an anti-inflammatory agent, discussed above in the glycyrrhizic acid section. Glycyrrhetinic acid is structurally different from glycyrrhizic acid in that glycyrrhetinic acid does not have a linked sugar residue (glycoside). Glycyrrhetinic acid is also known as carbenoxolone, glycyrrhetinic acid, or ursolic acid.

16. Carnosine

The compositions of the present invention may comprise a safe and effective amount of carnosine. Preferably, the composition comprises from about 0.01% to about 20%, more preferably from about 0.1% to about 15%, even more preferably from about 1% to about 10%, by weight of the composition, of carnosine compound.

Carnosine is a dipeptide and can be used as an antioxidant. The antioxidant mechanism is the same as described in the hesperetin section above. Carnosine occurs naturally in the human body. It is called an anti-aging agent because it is present at high levels in tissues with a long life span and at low levels in problematic tissues (such as cataracts). Structurally and functionally analogous substances to carnosine include β -alanyl histamine, anserine, homocarnosine and snake carnosine.

17. Cetyl pyridinium chloride

The compositions of the present invention may contain a safe and effective amount of cetylpyridinium chloride. Substituted forms of cetylpyridinium chloride include those in which one or two of the substituents on the quaternary nitrogen have a carbon chain length (typically alkyl) of from about 8 to about 20, typically from about 10 to about 18 carbon atoms, while the remaining substituents (typically alkyl or benzyl) have a lower number of carbon atoms, such as from about 1 to about 7 carbon atoms (typically methyl or ethyl). Examples of typical quaternary ammonium agents are dodecyltrimethylammonium bromide, tetradecylpyridinium chloride, domiphen bromide, N-tetradecyl-4-ethylpyridinium chloride, dodecyldimethyl (2-phenoxyethyl) ammonium bromide, benzyldimethylstearylammonium chloride, quaternized 5-amino-1, 3-bis (2-ethylhexyl) -5-methylhexahydropyrimidine, alkylbenzyldimethylammonium chloride, benzethonium chloride and benzethonium chloride. Other compounds are bis-4- (R-amino) -1-pyridinium alkanes, which are disclosed in U.S. Pat. No. 4,206,215.

Cetyl pyridinium chloride is present in an amount of from about 0.005% to about 10%, more preferably from about 0.01% to about 5%, more preferably from about 0.05% to about 2%, by weight of the composition. Cetyl pyridinium chloride is an inhibitor of tyrosinase, the mechanism of which is described above.

18. Ergothioneine

The compositions of the present invention may contain a safe and effective amount of ergothioneine. Ergothioneine is present at a level of from about 0.01% to about 20%, more preferably from about 0.1% to about 15%, even more preferably from about 1% to about 10%, by weight of the composition. The preferred ergothioneine is Thiotaine^®Which is a commercial solution of the chemical ergothioneine, available from Barnet Products. Ergothioneine has been shown to have antioxidant propertiesThe mechanism is as described above.

19. Diethylhexylidene malonate

The compositions of the present invention may comprise a safe and effective amount of diethylhexyl syringylidenemalonate. Diethylhexylsyrinylidene malonate is present at a level of from about 0.01% to about 20%, more preferably from about 0.1% to about 15%, even more preferably from about 0.5% to about 10%, by weight of the composition.

A preferred diethylhexyl syringylidenemalonate is Oxynex^®It shows antioxidant properties. It is available from Rona/Merck.

20. Melanocyte-stimulating hormone inhibin

The composition of the present invention may contain a safe and effective amount of melatonin. The melanostatin is present in an amount from about 0.01% to about 20%, more preferably from about 0.1% to about 15%, even more preferably from about 0.5% to about 10% by weight of the composition. Since melatonin is a commercial solution of peptides, where there is a mass of about 50ppm of peptides, the exact amount of peptides contained in a product containing 5% melatonin is actually about 2.5ppm of peptides.

Preferred melanotropins are available from Vincience, france. Melanotropin is a hexapeptide and, mechanistically, it acts by inhibiting the binding of alpha-MSH (melanocyte stimulating hormone) to its cellular receptors, thereby inhibiting the initiation of pigmentation.

21. Sterol esters

The compositions of the present invention may contain a safe and effective amount of a sterol ester. The sterol ester is present in an amount from about 0.01% to about 20%, more preferably from about 0.1% to about 15%, even more preferably from about 0.5% to about 10% by weight of the composition.

When sterol esters are used in the present invention, the formulation of the composition should be such that hydrolysis of the ester does not occur. Thus, the pH of the composition comprising sterol ester desirably ranges from about 3 to about 8, preferably from about 4 to about 7.

Sterol esters useful in the present invention include sterols or sterol mixtures (in particular, sitosterol, campesterol, stigmasterol, brassicasterol, and other sterols) esterified with fatty acids or fatty acid mixtures having from 8 to 30 carbon atoms (preferably from 16 to 22 carbon atoms), which may be linear or branched, saturated or unsaturated. Sterol esters are available from P & gcchemicals.

22. Idebenone

The compositions of the present invention may contain a safe and effective amount of idebenone. Preferably, the composition comprises from about 0.001% to about 10%, more preferably from about 0.005% to about 5%, even more preferably from about 0.01% to about 1%, by weight of the composition, of idebenone compound. Alternatively, the composition may comprise from about 0.1% to about 0.5% of the idebenone compound, by weight of the composition.

As used herein, "idebenone" refers to the following compounds, esters and other derivatives, salts, isomers, tautomers, and combinations thereof:

one technical name of idebenone of the present invention is 6- (10-hydroxydecyl) -2, 3-dimethoxy-5-methyl-1, 4-benzoquinone.

23. Dehydroacetic acid

The compositions of the present invention comprise dehydroacetic acid having the structure:

or a pharmaceutically acceptable salt, derivative or tautomer thereof. As used herein, "pharmaceutically acceptable" means that the dehydroacetates are suitable for use in contact with the tissues of the mammal in which they will be used without undue toxicity, incompatibility, instability, irritation, allergic response, and the like. The technical name of dehydroacetic acid is 3-acetyl-6-methyl-2H-pyran-2, 4(3H) -dione, and is available from Lonza.

Pharmaceutically acceptable salts include alkali metal salts, such as sodium and potassium salts; alkaline earth metal salts, such as calcium and magnesium salts; non-toxic heavy metal salts; an ammonium salt; and trialkylammonium salts such as trimethylammonium salts and triethylammonium salts. Sodium, potassium and ammonium salts of dehydroacetic acid are preferred. Highly preferred is sodium dehydroacetate available from Tri-K under the tradename Tristat SDHA. Derivatives of dehydroacetic acid include, but are not limited to, any of the compounds in which CH is present₃Compounds in which groups are replaced by amides, esters, amino groups, alkyl groups and alcohol esters, alone or in combination. Tautomers of dehydroacetic acid are dehydroacetic acid isomers that can be more readily interconverted, and thus they are usually present in equilibrium. Thus, tautomers of dehydroacetic acid can be described as having formula C₈H₈O₄And generally has the structure described above.

In one embodiment, the compositions of the present invention may comprise from about 0.001% to about 25%, preferably from about 0.01% to about 10%, more preferably from about 0.05% to about 5%, and even more preferably from about 0.1% to about 1%, by weight of the composition, of dehydroacetic acid, or a pharmaceutically acceptable salt, derivative, or tautomer thereof.

24. Other active substances

The compositions of the present invention may contain a safe and effective amount of one or more of the following other actives or ingredients: fatty acids (especially polyunsaturated fatty acids), glucosamine, 1-oxo-2-mercaptopyridine Zinc (ZPT), fungicides, thiol compounds (such as N-acetyl cysteine, glutathione, thioglycolate), other vitamins (vitamin B12), beta-carotene, ubiquinone, amino acids, and the like.

Dermatologically acceptable carrier

The topical compositions of the present invention may also comprise a dermatologically acceptable carrier for the active. The phrase "dermatologically acceptable carrier" as used herein means that the carrier is suitable for topical application to keratinous tissue, has good aesthetic properties, is compatible with the active agents of the present invention as well as any other components, and does not pose any safety or toxicity problems. A safe and effective amount of carrier comprises from about 50% to about 99.99%, preferably from about 60% to about 99.9%, more preferably from about 70% to about 98%, even more preferably from about 80% to about 95% of the composition.

The carrier may take a variety of forms. For example, emulsion carriers including, but not limited to, oil-in-water emulsions, water-in-oil emulsions, silicone-in-water emulsions, water-in-silicone emulsions, water-in-oil-in-water emulsions, and oil-in-water-in-silicone emulsions may be used in the present invention.

Preferred carriers include emulsions, such as oil-in-water emulsions and water-in-oil emulsions, for example silicone-in-water emulsions or water-in-silicone emulsions. As will be appreciated by the skilled person, a given component will partition predominantly into either the aqueous or oil phase, depending on the water solubility/dispensability of that component in the composition. Oil-in-water emulsions are particularly preferred.

The emulsions according to the invention generally comprise a solution as described above and a lipid or oil. The lipids and oils may be derived from animals, plants, or petroleum, and may be natural or synthetic (i.e., manufactured artificially). Preferred emulsions also contain a humectant, such as glycerin. The emulsion preferably further comprises from about 0.1% to about 10%, more preferably from about 0.2% to about 5%, by weight of the composition, of an emulsifier. The emulsifier may be nonionic, anionic or cationic. Suitable Emulsifiers are disclosed, for example, in U.S. Pat. No. 3,755,560, U.S. Pat. No. 4,421,769, and McCut cheon, North American edition 317 to 324 (1986).

Suitable emulsions can have a wide range of viscosities, depending on the type of product desired. Preferred exemplary low viscosity emulsions have about 5E-5m²(ii) s (50 centistokes) or less, more preferably about 1E-5m²(ii) s (10 centistokes) or less, even more preferably about 5E-6m²(ii) a viscosity of 5 centistokes or less.

The compositions of the present invention may also comprise other dermatologically acceptable topical carriers, and may also comprise oral carriers. For example, another topical carrier can be a surfactant-containing cleanser (e.g., bar soap, shampoo, foaming cleanser, liquid cleanser, body wash, cleaning wipe, etc.). In the above carriers, the surfactant may be anionic, cationic, zwitterionic, nonionic, or a mixture thereof. Another topical carrier is a color cosmetic (lipstick, blusher, eyeliner, mascara, foundation, nail polish, etc.). An oral carrier is a beverage, food, pill, capsule, powder, caplet, etc.

Optional Components

The compositions of the present invention may contain other ingredients commonly used in a variety of given product types, provided that they do not unacceptably alter the benefits of the present invention.

When incorporated into compositions, the optional ingredients should be suitable for use in contact with human keratinous tissue without undue toxicity, incompatibility, instability, allergic response, and the like, within the scope of sound judgment. The second edition of "CTFA Cosmetic Ingredient Handbook" (1992) describes a variety of non-limiting Cosmetic and pharmaceutical ingredients commonly used in the skin care field, which are suitable for use in the compositions of the present invention. Examples of these composition classes include: abrasives, absorbents, aesthetic components such as fragrances, pigments, colorants/colorants, essential oils, skin sensates, astringents, and the like (e.g., clove oil, menthol, camphor, eucalyptus oil, eugenol, menthyl lactate, witch hazel distillate), anti-acne agents, anti-caking agents, anti-foaming agents, antimicrobial agents (e.g., iodopropyl butylcarbamate), antioxidants, binders, biological additives, buffering agents, extenders, chelating agents, chemical additives, colorants, cosmetic astringents, cosmetic insecticides, denaturants, medicinal astringents, external analgesics, film formers or film forming materials such as polymers that contribute to the film forming properties and film substantivity of the composition (e.g., copolymers of eicosene and vinyl pyrrolidone), opacifiers, pH adjusters, propellants, reducing agents, sequestering agents, skin lightening agents, and skin lightening agents, skin conditioning agents, skin soothing and/or healing agents and derivatives, skin treatment agents, thickeners, and vitamins, and derivatives thereof.

Other optional components that may be used in the compositions of the present invention include those described in U.S. publication 2004-0175347a1, including desquamation actives such as salicylic acid and zwitterionic surfactants; anti-acne actives such as resorcinol, sulfur, erythromycin, zinc, dehydroacetic acid; anti-wrinkle actives/anti-atrophy actives; antioxidants/radical scavengers, such as tocopherol; chelating agents, such as furildioxime and its derivatives; a flavonoid; an anti-inflammatory agent; anti-cellulite agents; tanning actives, such as dihydroxyacetone; a skin lightening agent; antimicrobial and antifungal actives; a sunscreen active; conditioning agents such as glycerin, urea, petrolatum, sucrose polyesters, and combinations thereof; thickeners such as carboxylic acid polymers, crosslinked polyacrylate polymers, polyacrylamide polymers, polysaccharides, gums; and a particulate material.

Composition form

Topical compositions of the subject invention include, but are not limited to, lotions, emulsions, mousses, slurries, sprays, aerosols, foams, sticks, pencils, gels, creams, and ointments, which may comprise dermatologically acceptable emollients. The above compositions preferably comprise from about 2% to about 50% of an emollient. As used herein, "emollient" refers to a substance used to prevent or reduce dryness, as well as to protect the skin. A variety of suitable emollients are known and may be used herein. Examples of materials suitable for use as emollients are contained in Sagarin "Cosmetics, Science and Technology" Vol.2, Vol.1, pages 32-43 (1972). The preferred emollient is glycerin. Glycerol is preferably used in amounts of about 0.001 to about 20%, more preferably about 0.01 to about 15%, even more preferably about 0.1 to about 10%, by weight of the composition.

The compositions of the present invention useful for cleansing ("cleansers") are formulated with a suitable carrier (e.g., a carrier as described above, and comprising from about 1% to about 90%, by weight of the composition, of a dermatologically acceptable surfactant).

The physical form of the cleaning composition is not critical. The composition may be formulated, for example, as a toilet bar, liquid, shampoo, shower gel, conditioner, hair tonic, paste, or mousse. Toilet bar soaps are preferred because this is the most common form of cleanser used to wash the skin. Rinse-off cleansing compositions, such as shampoos, require a delivery system suitable for depositing sufficient amounts of active onto the skin and scalp. The preferred delivery system involves the use of insoluble complexes. A more complete disclosure of the above delivery system can be found in U.S. patent 4,835,148.

The compositions of the present invention may also be in the form of a cosmetic product. Suitable cosmetic forms include, but are not limited to, foundations, lipsticks, blushers, mascaras, and the like. The cosmetic products may include conventional ingredients such as oils, colorants, pigments, emollients, fragrances, waxes, stabilizers and the like. Exemplary carriers and other ingredients described above suitable for use herein are described, for example, in U.S. Pat. No. 6,060,547.

The compositions of the present invention may also be in the form of shave preparation products including, for example, gels, foams, lotions, and creams; and include aerosol and non-aerosol types.

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. The above-described methods typically involve mixing the ingredients in one or more steps to a relatively uniform state, with or without the need for heating, cooling, the use of vacuum, and the like. The composition is preferably prepared to optimize the stability (physical stability, chemical stability, photostability) and/or delivery of the active substance. Such optimization may include appropriate pH (e.g., less than 7), exclusion of materials that may complex with the active and thus negatively affect stability or delivery (e.g., exclusion of iron impurities), use of methods to prevent complex formation (e.g., appropriate dispersion or dual chamber packaging), use of appropriate photostability methods (e.g., addition of sunscreen/sunblock, use of opaque packaging), and the like.

Method for regulating the condition of keratinous tissue

The compositions of the present invention are useful for regulating the condition of keratinous tissue in a wide variety of mammals. Such regulation of keratinous tissue condition includes both prophylactic and therapeutic regulation. More particularly, the above-described methods of modulation relate to, but are not limited to, thickening keratinous tissue (i.e., constructing the epidermal and/or dermal and/or subcutaneous layers of the skin, and, where appropriate, the stratum corneum of the nails and hair shafts); preventing, retarding and/or treating uneven skin tone by use as a cosmetic agent to lighten skin or reduce pigmentation; preventing, retarding and/or treating atrophy of the skin of a mammal, softening and/or smoothing lips, hair and nails of a mammal; preventing, delaying and/or treating itch of skin in mammals; preventing, delaying and/or treating the appearance of dark under-eye circles and/or puffy eyes; preventing, retarding and/or treating sallowness of mammalian skin; preventing, retarding and/or treating sagging (i.e., glycation) of mammalian skin; preventing and/or delaying tanning, desquamation, scaling and/or increasing turnover in the skin of a mammal; reducing pore size in mammalian skin; regulating the appearance of oily/shiny mammalian skin; preventing, delaying and/or treating hyperpigmentation such as post-inflammatory hyperpigmentation; preventing, delaying and/or treating the appearance of spider vessels and/or erythema on the skin of a mammal; preventing, retarding and/or treating fine lines and wrinkles of mammalian skin; preventing, retarding and/or treating dry skin (i.e., rough, flaky); and preventing, delaying and/or treating the appearance of cellulite in the skin of a mammal. The compositions of the present invention may also be used to inhibit hair growth, reduce shaving frequency, improve ease of shaving, reduce shaving frequency, make hair softer and/or finer, make hair less visible, slow hair regrowth, reduce erythema and skin inflammation, make skin smoother and/or softer, and improve hair removal patterns. Regulating keratinous tissue condition involves topically applying to the keratinous tissue a safe and effective amount of a composition of the present invention. The amount of composition applied, the frequency of application, and the period of use will vary widely depending upon the level of skin and/or hair care active and/or other components in a given composition and the degree of adjustment desired.

In a preferred embodiment, the composition is applied to the skin for an extended period of time. By "chronic topical administration" is meant the topical administration of the composition for a prolonged period of time, preferably for a period of at least about one week, more preferably at least about one month, even more preferably at least about three months, even more preferably at least about six months, and yet even more preferably at least about one year, over the life of the subject. Although beneficial effects may still be obtained after various maximum periods of use (e.g., five, ten, or twenty years), it is preferred that the administration be continued for a long period throughout the subject's lifetime. During the extended period, administration is typically on a regular basis of about once a day, however the frequency of administration may vary from about once a week to about three or more times a day.

Various amounts of the compositions of the present invention can be used to provide skin appearance and/or skin feel benefits. In mg composition/cm²The amount of the composition of the present invention per typical application is about 0.1mg/cm on a dermometer basis²To about 20mg/cm². A particularly useful coating amount is about 0.5mg/cm²To about 10mg/cm²。

The conditioning of keratinous tissue conditions is preferably carried out by applying the composition in the form of a skin lotion, cleansing lotion, milky lotion, cream, gel, foam, salve, paste, emulsion, spray, conditioner, tonic, cosmetic, lipstick, foundation, nail polish, aftershave, or the like. The compositions are intended to remain on the skin or other keratinous tissue for certain aesthetic, prophylactic, therapeutic, or other benefits (i.e., "leave-on" compositions). After application of the composition to keratinous tissue (e.g., skin), it remains on the skin for preferably at least about 15 minutes, more preferably at least about 30 minutes, even more preferably at least about 1 hour, even more preferably at least several hours, such as up to about 12 hours. Any surface area of the face, hair and/or nails may be treated such as the face, lips, under-eye areas, eyelids, scalp, neck, torso, arms, hands, legs, fingernails, toenails, scalp hair, eyelashes, eyebrows, and the like. Application of the compositions of the present invention is carried out by using, for example, the palm and/or fingers, an implement (e.g., a cotton ball, swab, wipe, pad, etc.).

Another way to ensure that at least a minimum level of skin and/or hair care actives is continuously applied to keratinous tissue is by applying the compounds using a patch that is applied, for example, to the face. The above method is particularly useful for areas of skin with problems that require more intensive treatment (e.g., areas of facial crow's feet, eyebrow ridges, under-eye areas, etc.). The patch may be occlusive, semi-occlusive or non-occlusive. The composition may be contained in a patch or applied to the skin prior to use of the patch. The patch also contains an additional active substance, such as a chemical initiator for the exothermic reaction, such as those described in PCT application WO 9701313. The patch also includes a source of electrical energy (e.g., a battery) to, for example, enhance delivery of skin and/or hair care actives and other actives (e.g., iontophoresis). The residence time of the patch when applied to keratinous tissue is preferably at least about 5 minutes, more preferably at least about 15 minutes, even more preferably at least about 30 minutes, even more preferably at least about 1 hour, and even more preferably at night, as a form of nighttime treatment.

Another way to enhance the beneficial effects of actives is to use a kit or embodiment having 2 or 3 or 4 or more products and/or treatment steps (e.g., desquamation, followed by topical treatment with one or more actives of the present invention, hair loss, followed by topical treatment with one or more actives of the present invention, etc.). The various components of the embodiments may be used over a short period of time (e.g., over an hour), or over a longer period of time throughout the day (e.g., morning and evening), or even longer periods of time (e.g., one step of the embodiments is performed weekly or monthly, and other steps of the embodiments are performed on a more regular basis (e.g., daily)). The kit or embodiment further comprises a combination of the above carriers and/or product forms such as two or more cleansers, topical leave-on treatments, and oral supplements.

The present invention also contemplates the delivery of energy to keratinous tissue via a device, which can be simultaneous and/or sequential with the application of the topical composition. The energy delivery device can deliver a variety of forms of energy, including but not limited to the following forms of energy: light, heat, sound (including ultrasonic waves), magnetic energy, electromagnetic energy (including radio frequency waves and microwaves), and combinations thereof. The delivery of energy may be continuous, pulsed, modulated, non-modulated, and combinations thereof. In one embodiment, the energy delivery device is handheld. Alternatively, the energy delivery device is wireless.

Energy is applied by maintaining the device within a single area of keratinous tissue, and then moving the device to another area of tissue (or "punch"). Alternatively, the energy may be applied while the device is continuously moved or scanned across the tissue surface. The device will remain in substantially continuous contact with the keratinous tissue surface when a laser device is used, or a short distance from the keratinous tissue while the energy is directed at the surface when a flash lamp is used.

In keratinous tissue or alternatively, in compounds applied to the surface of the tissue, a temperature change may be produced simultaneously. This temperature change is in addition to any temperature change resulting from the delivered energy itself. For example, the keratinous tissue may be slightly heated prior to energy delivery, or alternatively, the keratinous tissue may be cooled after energy delivery.

For energy derived from an ultraviolet light source, the wavelength is typically in the UV-A range of about 315-400nm, where "nm" refers to 1X 10-9 meters. For energy derived from visible light sources, the wavelength is typically in the range of about 400nm to about 700 nm. For energy derived from Infrared (IR) light sources, the wavelength is typically in the range of about 700nm to about 3000 nm. The amount of energy delivered or "output flow" may be about 1J/cm²To about 100J/cm²Wherein "J" refers to Joule. For a pulsed light source, the pulse width is in the range of about 0.001 seconds to about 3 seconds, and the average pulse duration is about 0.001 seconds to about 1 second. The surface area of the keratinous tissue to be covered will vary depending on the application. These and other parameters related to energy delivery depend on the type of treatment and the type of tissue to be treated and may be appropriately selected by those skilled in the art.

Article of commerce

The present invention also provides an article of commerce comprising a personal care composition, and indicia (and/or images) associated with at least one package for the personal care composition, and advertising material associated with the personal care composition, the advertising material conveying the following information: topical application of personal care compositions can improve the skin tone or skin color of a person.

In an exemplary embodiment, a package for a personal care composition includes indicia and/or images. The package may be a primary package, a secondary package, and/or an additional package. The type of packaging associated with the present invention is not limiting. The package can be made from a variety of materials, can be made in a variety of configurations, and can be made using any manufacturing technique known to the skilled artisan. Exemplary package embodiments include boxes, bags, pouches, cardboard cans, bottles, tottles, jars, thermoformed blisters, clamshell, and combinations thereof. Other packaging embodiments are equally suitable.

In another exemplary embodiment, the advertising material and/or device associated with the personal care composition includes indicia and/or images. Exemplary advertising materials/devices include, but are not limited to, point-of-sale devices and/or materials, samples and related information, coupons, mailed advertising prints, periodic advertising documents, product manuals, product inserts, product displays, shelf cards, billings, posters, buses, outdoor recreational facilities, and any other advertising medium available to potential buyers. For example, the advertising material and/or device may be (permanently or removably) affixed to or contained within the package.

Examples

The following are non-limiting examples of compositions of the present invention. The examples are given solely for the purpose of illustration and are not to be construed as limitations of the present invention, as many variations thereof are possible without departing from the spirit and scope of the invention, which will be recognized by those of ordinary skill in the art. In the examples, all concentrations are listed in weight percent and exclude minor materials such as diluents, fillers, etc., unless otherwise indicated. Thus, the listed formulations include the listed components and any trace materials associated with the components. It will be apparent to those of ordinary skill in the art that the selection of these minor components will vary depending on the physical and chemical characteristics of the particular ingredients selected to make the invention described herein.

The content of the preparation (grams of the components in each 100g of the preparation)
							Components	A	B	C	D	E	F
Ethylenediaminetetraacetic acid disodium salt	0.100	0.100	0.100	0.100	0.100	0.100
							Carnosine	5.000	0	0	0	0	0
Vanillin acetate	0	2.000	0	0	0	0
							Tetrahydrocurcumin	0.500	0.500	0.500	1.000	0.250	0.500
Glycyrrhetinic acid	0	0	0	0.300	0	0
							Thiotaine®	0	0	0	0	5.000	0
Sinablanca®	0	0	0	0	0	2.500
							Nicotinamide	4.000	4.000	4.000	4.000	4.000	4.000
Citric acid	1.500	0	0	0	0	0
							Isohexadecane	3.000	3.000	0	0	3.000	3.000
Isostearic acid isopropyl ester	1.330	1.330	0	0	1.330	1.330
							N-lauroylsarcosine isopropyl ester	0	0	5.000	6.000	0	0
Sucrose Polyraffinate	0.670	0.670	0	0	0.670	0.670
							Polymethylsilsesquioxane	0.250	0.250	0.250	0.250	0.250	0.250
Cetearyl glucoside + cetostearyl alcohol	0.200	0.200	0.200	0.200	0.200	0.200
							Behenyl alcohol	0.400	0.400	0.400	0.400	0.400	0.400
P-hydroxybenzoic acid ethyl ester	0.200	0.200	0.200	0.200	0.200	0.200
							Propyl p-hydroxybenzoate	0.100	0.100	0.100	0.100	0.100	0.100
Cetyl alcohol	0.320	0.320	0.320	0.320	0.320	0.320
							Stearyl alcohol	0.480	0.480	0.480	0.480	0.480	0.480
Tocopherol acetate	0.500	0.500	0.500	0.500	0.500	0.500
							PEG-100 stearate	0.100	0.100	0.100	0.100	0.100	0.100
Glycerol	7.000	7.000	7.000	7.000	7.000	7.000
							Titanium dioxide	0.604	0.604	0.604	0.604	0.604	0.604
Polyacrylamide, C13-14 isoparaffin, lauryl polyoxyethylene ether-7	3.000	2.000	2.000	2.000	2.000	2.000
							Panthenol	1.000	1.000	1.000	1.000	1.000	1.000
Benzyl alcohol	0.400	0.400	0.400	0.400	0.400	0.400
							Polydimethylsiloxane + dimethiconol	2.000	2.000	2.000	2.000	2.000	2.000
Water (to 100g)	To 100	To 100	To 100	To 100	To 100	To 100
							Total of	100	100	100	100	100	100

The content of the preparation (grams of the components in each 100g of the preparation)
							Components	G	H	I	J	K	L
Ethylenediaminetetraacetic acid disodium salt	0.100	0.100	0.100	0.100	0.100	0.100
							Glucosyl hesperidin	1.000	0	0	0	0	0
Glycyrrhizic acid, ammonium salts	0	0.300	0	0	0	0
							Cetyl pyridinium chloride	0	0	0.200	0	0	0
Menthyl anthranilate	0	0	0	5.000	0	0
							Oxynex®	0	0	0	0	2.000	0
Butylated hydroxytoluene	0	0	0	0	0	1.000
							Tetrahydrocurcumin	0.500	0.500	0.500	1.000	0.500	1.000
Nicotinamide	4.000	4.000	4.000	4.000	4.000	4.000
							Polyquaternary ammonium salt 37	0	0	1.500	0	0	0
Isohexadecane	3.000	3.000	3.000	3.000	3.000	3.000
							Isostearic acid isopropyl ester	1.330	1.330	1.330	1.330	1.330	1.330
Sucrose Polyraffinate	0.670	0.670	0.670	0.670	0.670	0.670
							Polymethylsilsesquioxane	0.250	0.250	0.250	0.250	0.250	0.250
Spermaceti hard capsuleLipoglucoside + Hexadecyl/Octadecanol	0.200	0.200	0.200	0.200	0.200	0.200
							Behenyl alcohol	0.400	0.400	0.400	0.400	0.400	0.400
P-hydroxybenzoic acid ethyl ester	0.200	0.200	0.200	0.200	0.200	0.200
							Propyl p-hydroxybenzoate	0.100	0.100	0.100	0.100	0.100	0.100
Cetyl alcohol	0.320	0.320	0.320	0.320	0.320	0.320
							Stearyl alcohol	0.480	0.480	0.480	0.480	0.480	0.480
Tocopherol acetate	0.500	0.500	0.500	0.500	0.500	0.500
							PEG-100 stearate	0.100	0.100	0.100	0.100	0.100	0.100
Glycerol	7.000	7.000	7.000	7.000	7.000	7.000
							Titanium dioxide	0.604	0.604	0.604	0.604	0.604	0.604
Polyacrylamide, C13-14 isoparaffin, lauryl polyoxyethylene ether-7	2.000	2.000	0	2.000	2.000	2.000
							Panthenol	1.000	1.000	1.000	1.000	1.000	1.000
Benzyl alcohol	0.400	0.400	0.400	0.400	0.400	0.400
							Polydimethylsiloxane + dimethiconol	2.000	2.000	2.000	2.000	2.000	2.000
Water (to 100g)	To 100	To 100	To 100	To 100	To 100	To 100
							Total of	100	100	100	100	100	100

Components	M	N	O	P
					Ethylenediaminetetraacetic acid disodium salt	0.1	0.1	0.1	0.1
Nicotinamide	4.0	4.0	4.0	0
					Tetrahydrocurcumin	0.5	1.0	1.0	0.5
Ethanesulfonic acid hexyloxy ether	0.1	1.0	1.0	0.1
					N-undecylenoyl-L-phenylalanine	0.0	0.0	0.2	0
Sodium dehydroacetate	0.0	0.0	0.2	0.5
					Isohexadecane	0	3.0	3.0	3.0
Isostearic acid isopropyl ester	0	1.33	1.33	1.33
					N-lauroylsarcosine isopropyl ester	6.0	0	0	0
Sucrose Polyraffinate	0.67	0.67	0.67	0.67
					Polymethylsilsesquioxane	0.25	0.25	0.25	0.25
Cetearyl glucoside + cetearyl glucosideOctadecanol	0.2	0.2	0.2	0.2
					Behenyl alcohol	0.4	0.4	0.4	0.4
P-hydroxybenzoic acid ethyl ester	0.2	0.2	0.2	0.2
					Propyl p-hydroxybenzoate	0.1	0.1	0.1	0.1
Cetyl alcohol	0.32	0.32	0.32	0.32
					Stearyl alcohol	0.48	0.48	0.48	0.48
Tocopherol acetate	0.5	0.5	0.5	0.5
					PEG-100 stearate	0.1	0.1	0.1	0.1
Glycerol	7.0	7.0	7.0	7.0
					Titanium dioxide	0.604	0.604	0.604	0.604
Polyacrylamide, C13-14 isoparaffin, lauryl polyoxyethylene ether-7	2.0	2.0	2.0	2.0
					Panthenol	1.0	1.0	1.0	1.0
Benzyl alcohol	0.4	0.4	0.4	0.4
					Polydimethylsiloxane + dimethiconol	2.0	2.0	2.0	2.0
Water (to 100g)	To 100	To 100	To 100	To 100
					Total of	100	100	100	100

Components	Q	R
			Ethylenediaminetetraacetic acid disodium salt	0.100	0.100
Hydroquinone	2.000	0
			Tetrahydrocurcumin	0.500	1.000
Retinyl propionate	0	0.300
			Nicotinamide	4.000	4.000
Isohexadecane	3.000	3.000
			Isostearic acid isopropyl ester	1.330	1.330
Sucrose Polyraffinate	0.670	0.670
			Polymethylsilsesquioxane	0.250	0.250
Cetearyl glucoside + cetostearyl alcohol	0.200	0.200
			Behenyl alcohol	0.400	0.400
P-hydroxybenzoic acid ethyl ester	0.200	0.200
			Propyl p-hydroxybenzoate	0.100	0.100
Cetyl alcohol	0.320	0.320
			Stearyl alcohol	0.480	0.480
Tocopherol acetate	0.500	0.500
			PEG-100 stearate	0.100	0.100
Glycerol	7.000	7.000
			Titanium dioxide	0.604	0.604
Polyacrylamide, C13-14 isoparaffin, lauryl polyoxyethylene ether-7	2.000	2.000
			Panthenol	1.000	1.000
Benzyl alcohol	0.400	0.400
			Polydimethylsiloxane + dimethiconol	2.000	2.000
Water (to 100g)	To 100	To 100

While particular embodiments of the present invention have been illustrated and described, it would be obvious to those skilled in the art that various other changes and modifications can be made without departing from the spirit and scope of the invention. It is therefore intended to cover in the appended claims all such changes and modifications that are within the scope of this invention.

All documents cited in the background of the invention, summary of the invention and detailed description of the invention are, in relevant part, incorporated herein by reference. The citation of any document is not to be construed as an admission that it is prior art with respect to the present invention.

Claims (12)

1. A personal care composition, the composition comprising:

a) tetrahydrocurcumin; and

b) at least one additional skin and/or hair care active selected from the group consisting of: sugar amine, vitamin B₃Retinoids, hydroquinone, peptides, phytosterols, dialkanoyl hydroxyproline, hexamidine, salicylic acid, n-acyl amino acid compounds, sunscreen actives, water soluble vitamins, oil soluble vitamins, hesperetin, mustard seed extract, glycerolsOxalic acid, glycyrrhetinic acid, carnosine, Butylated Hydroxytoluene (BHT) and Butylated Hydroxyanisole (BHA), menthyl anthranilate, cetylpyridinium chloride, ergothioneine, vanillin and derivatives thereof, diethylhexyl syringylidenemalonate, melanostatin, sterol esters, idebenone, dehydroacetic acid, yeast extract, β -glucan, α -glucan, salts thereof, derivatives thereof, precursors thereof, and/or combinations thereof; and

c) a dermatologically acceptable carrier.

2. The personal care composition of claim 1, wherein the tetrahydrocurcumin can be used in combination with tetrahydrodemethoxycurcumin and/or tetrahydrobisdemethoxycurcumin.

3. The personal care composition of claim 1 or 2, wherein the at least one additional skin and/or hair care active is vitamin B₃。

4. The personal care composition of any one of claims 1 to 3, wherein said at least one additional skin and/or hair care active comprises niacinamide, panthenol, and vitamin E acetate.

5. The personal care composition of any one of claims 1 to 4, wherein the at least one additional skin and/or hair care active comprises yeast extract and ascorbyl glucoside.

6. The personal care composition of any one of claims 1 to 5, further comprising from 0.001% to 10% by weight of an additional component selected from the group consisting of: desquamation actives, anti-acne actives, wrinkle repair actives, antioxidants, free radical scavengers, chelators, flavonoids, anti-inflammatory agents, anti-cellulite agents, skin lightening agents, antimicrobial actives, antifungal actives, conditioning agents, thickening agents, water soluble vitamins, oil soluble vitamins, particulate materials, local anesthetics, and combinations thereof.

7. A personal care composition comprising at least one antioxidant compound, at least one tyrosinase inhibiting compound, at least one trypsin inhibiting compound, at least one anti-inflammatory compound, and at least one nitric oxide scavenging compound.

8. An article of commerce, comprising:

a) a personal care composition comprising tetrahydrocurcumin and at least one sunscreen active; and

b) at least one of the personal care compositions, packaging for the personal care compositions, and advertising material associated with the personal care compositions, the advertising material comprising indicia and/or images that convey the following information: topical application of the personal care composition can improve skin tone or skin color in a person.

9. A method of regulating the condition of mammalian keratinous tissue comprising the step of topically applying to the skin of a mammal in need of such treatment a composition according to any one of claims 1 to 7.

10. A method of improving skin tone or skin color comprising the step of topically applying to the skin of a mammal in need of such treatment a composition according to any one of claims 1 to 7.

11. A method of lightening skin comprising the step of topically applying the composition of any one of claims 1 to 7 to the skin of a mammal in need of such treatment.

12. A method of inhibiting hair growth comprising the step of topically applying to the skin of a mammal in need of such treatment a composition according to any one of claims 1 to 7.