WO2013083645A2 - Composition éclaircissante pour la peau - Google Patents

Composition éclaircissante pour la peau Download PDF

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Publication number
WO2013083645A2
WO2013083645A2 PCT/EP2012/074534 EP2012074534W WO2013083645A2 WO 2013083645 A2 WO2013083645 A2 WO 2013083645A2 EP 2012074534 W EP2012074534 W EP 2012074534W WO 2013083645 A2 WO2013083645 A2 WO 2013083645A2
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WO
WIPO (PCT)
Prior art keywords
skin
climbazole
composition
lightening
composition according
Prior art date
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PCT/EP2012/074534
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English (en)
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WO2013083645A3 (fr
Inventor
Rebecca Susan Ginger
Original Assignee
Unilever Plc
Unilever N.V.
Hindustan Unilever Limited
Conopco, Inc., D/B/A Unilever
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Application filed by Unilever Plc, Unilever N.V., Hindustan Unilever Limited, Conopco, Inc., D/B/A Unilever filed Critical Unilever Plc
Publication of WO2013083645A2 publication Critical patent/WO2013083645A2/fr
Publication of WO2013083645A3 publication Critical patent/WO2013083645A3/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • A61K8/4946—Imidazoles or their condensed derivatives, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4986—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with sulfur as the only hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q15/00—Anti-perspirants or body deodorants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin

Definitions

  • Desired skin colour is a major unmet consumer need in Asia. Consumers particularly desire even skin colour, absence of age spots (solar lentigines) and lighter overall skin tone.
  • One solution is to use biological actives that reduce the activity of melanocytes in skin. These cells, present in the basal layer of the epidermis, make the darkly coloured pigment melanin and export it in small export vesicles called melanosomes to the neighbouring keratinocytes. It is well described in the literature that compounds which reduce melanin synthesis when topically applied to the skin will reduce skin darkness over time.
  • This invention relates to a composition comprising climbazole for use in skin lightening.
  • This invention is based on the fact that climbazole has been found to inhibit pigment production in B16 monolayer and MelanoDermTM cultures.
  • climbazole when applied topically over an appropriate length of time in-vivo, would be expected to cause skin lightening, or to reduce blemishes and/or hyperpigmented spots and/or solar lentigines leading to an improvement in skin tone and evenness.
  • Climbazole is a topical antifungal agent commonly used in the treatment of human fungal skin infections such as dandruff and eczema. Climbazole has shown a high in-vitro and in- vivo efficacy against Pityrosporum ovale that appears to play an important role in the pathogenesis of dandruff. Its chemical structure and properties are similar to other fungicides such as ketoconazole and miconazole.
  • WO 95/34280 discloses methods of lightening hyper-pigmented regions in mammalian skin by administering to the skin a composition comprising an effective amount of a sulfhydryl compound.
  • Preferred sulfhydryl compounds include lipoic acid.
  • WO 2010/121919 discloses a hair growth composition comprising lipoic acid as a microcirculation promoter and climbazole as an anti-dandruff agent. Summary of the invention
  • a skin lightening composition comprising:
  • Climbazole has the following structure:
  • lipoic acid has the following structure:
  • a composition according to the first aspect is provided for use in skin lightening.
  • skin lightening is preferably a skin benefit selected from the group consisting of treating freckles, treating age spots, treating uneven skin tone, treating underarm hyperpigmentation, reducing blemishes and treating hyperpigmented spots.
  • an effective amount of climbazole is provided for use in skin lightening.
  • This invention relates to a composition comprising climbazole for use in skin lightening.
  • This invention is based on the fact that climbazole has been found to inhibit pigment production in B16 monolayer and MelanoDermTM cultures.
  • climbazole when applied topically over an appropriate length of time in-vivo, would be expected to cause skin lightening, or to reduce blemishes and/or hyperpigmented spots and/or solar lentigines leading to an improvement in skin tone and evenness.
  • the invention provides an effective amount of climbazole for use in skin lightening.
  • use of an effective amount of climbazole is provided in the manufacture of a medicament for lightening skin.
  • a method of lightening the skin of a human is provided, the method comprising the step of applying an effective amount of climbazole to skin of a person in need thereof.
  • a skin lightening composition is also provided, the composition comprising:
  • the composition may comprise 0.001 to 2, preferably 0.005 to 0.5 % w/w climbazole and/or 0.001 to 2, preferably 0.002 to 0.2 % w/w lipoic acid. These concentration ranges will provide about 10 ⁇ of each of climbazole and lipoic acid in the basal epidermis.
  • the lipoic acid is preferably in the form of the R-(+)-isomer, preferably exclusively in the form of the R-(+)-isomer.
  • Sunscreens include those materials commonly employed to block ultraviolet light.
  • Illustrative organic compounds are the derivatives of PABA, cinnamate and salicylate.
  • avobenzophenone Parsol 1789®
  • octyl methoxy cinnamate and 2-hydroxy-4- methoxy benzophenone also known as oxybenzone
  • Octyl methoxycinnamate and 2-hydroxy-4-methoxy benzophenone are commercially available under the trademarks, Parsol MCX and Benzophenone-3, respectively.
  • Inorganic sunscreens include oxides like titanium dioxide and zinc oxide which reflect or scatter the suns rays. The exact amount of sunscreen employed in the compositions can vary depending upon the degree of protection desired from the sun's UV radiation. However levels can be in the range 0.01 to 15, preferably 0.1 to 10, most preferably 0.5 to 7.5 % by weight of the composition.
  • the composition preferably contains an antiperspirant active.
  • Antiperspirant actives are preferably incorporated in an amount of from 0.5 to 50, particularly from 5 to 30 and especially from 10 to 26 % by weight of the composition. It is often considered that the main benefit from incorporating of up to 5 % by weight of the composition of an antiperspirant active in a stick composition is manifest in reducing body odour, and that as the proportion of antiperspirant active increases, so the efficacy of that composition at controlling perspiration increases.
  • Antiperspirant actives for use herein are often selected from astringent active salts, including in particular aluminium, zirconium and mixed aluminium/zirconium salts, including both inorganic salts, salts with organic anions and complexes.
  • astringent active salts include aluminium, zirconium and aluminium/zirconium halides and halohydrate salts, such as chlorohydrates.
  • Especially effective aluminium halohydrate salts, known as activated aluminium chlorohydrates, are described in EP 6739 A (Unilever NV et al), the contents of which specification is incorporated herein by reference.
  • Such activated aluminium chlorohydrates are made by a method in which the weight concentration of aluminium compounds in the solution is controlled within specified limits and simultaneously the temperature of that solution is controlled within a specified elevated temperature range whilst polymeric aluminium species are formed, and drying conditions are strictly controlled as described in the said EP 6739 A.
  • Some activated salts do not retain their enhanced activity in the presence of water but are useful in substantially anhydrous formulations, i.e. formulations that do not contain a distinct aqueous phase.
  • Zirconium actives can usually be represented by the empirical general formula: ZrO(OH)2n- nzBz.wH 2 0 in which z is a variable in the range of from 0.9 to 2.0 so that the value 2n-nz is zero or positive, n is the valency of B, and B is selected from the group consisting of chloride, other halide, sulphamate, sulphate and mixtures thereof. Possible hydration to a variable extent is represented by wH 2 0. Preferable is that B represents chloride and the variable z lies in the range from 1.5 to 1.87. In practice, such zirconium salts are usually not employed by themselves, but as a component of a combined aluminium and zirconium-based antiperspirant.
  • aluminium and zirconium salts may have co-ordinated and/or bound water in various quantities and/or may be present as polymeric species, mixtures or complexes.
  • zirconium hydroxy salts often represent a range of salts having various amounts of the hydroxy group.
  • Zirconium aluminium chlorohydrate may be particularly preferred.
  • Antiperspirant complexes based on the above-mentioned astringent aluminium and/or zirconium salts can be employed.
  • the complex often employs a compound with a carboxylate group, and advantageously this is an amino acid.
  • suitable amino acids include dl-tryptophan, dl-P-phenylalanine, dl-valine, dl-methionine and ⁇ -alanine, and preferably glycine which has the formula CH 2 ( H 2 )COOH.
  • ZAG actives generally contain aluminium, zirconium and chloride with an Al/Zr ratio in a range from 2 to 10, especially 2 to 6, an Al/Cl ratio from 2.1 to 0.9 and a variable amount of glycine. Actives of this preferred type are available from Westwood, from Summit and from Reheis, though with differing particle size distributions.
  • aluminium and/or zirconium-containing astringent antiperspirant salts employed herein have metal: chloride mole ratio in the range of 1.3 : 1 to 1.5: 1. Others having a lower metal: chloride mole ratio, such as from 1 : 1 to 1.25: 1 tend to generate lower pHs when applied to skin and thus tend to be more irritating.
  • the proportion of solid antiperspirant salt in a suspension composition normally includes the weight of any water of hydration and any complexing agent that may also be present in the solid active.
  • RI refractive index
  • Actives which are free from zirconium tend to have an RI of from 1.49 to 1.54, depending on their formula and at least partly on their residual water content.
  • actives which contain zirconium tend to have an RI of from 1.52 to 1.57.
  • the selection of the antiperspirant active material desirably takes into account the type of applicator from which it is dispensed.
  • the antiperspirant active comprises an aluminium-zirconium active, such as AZAG.
  • the antiperspirant active is highly desirably an aluminium chlorohydrate (ACH) and in others an activated aluminium chlorohydrate (AACH).
  • At least 90, preferably at least 95 and especially at least 99 % by weight of the particles have a diameter in the range of from 0.1 up to 100 ⁇ , and usually have an average particle diameter of at least 1 ⁇ and especially below 20 ⁇ .
  • the particles by weight have a weight average particle size of at least 2 ⁇ and particularly below 10 ⁇ , such as in the range of from 3 to 8 ⁇ .
  • Suitable deodorant actives can comprise deodorant effective concentrations of antiperspirant metal salts, deoperfumes, and/or microbiocides, including particularly bactericides, such as chlorinated aromatics, including biguanide derivatives, of which triclosan (e.g. Irgasan DP300 or Triclorban), and chlorhexidine warrant specific mention.
  • bactericides such as chlorinated aromatics, including biguanide derivatives, of which triclosan (e.g. Irgasan DP300 or Triclorban), and chlorhexidine warrant specific mention.
  • Another class of effective deodorants comprises polyaminopropyl biguanide salts such as are available under the trade mark Cosmosil. Such materials commonly act as bactericides.
  • a still further class of materials that can inhibit malodour formation comprise chelators that can sequester iron, and thereby retard bacterial growth, including aminopolycarboxylates such as ethylenediamine tetraacetic acid (EDTA) or higher homologues such as diethylenetriamine pentaacetic acid (DTP A).
  • chelators that can sequester iron, and thereby retard bacterial growth, including aminopolycarboxylates such as ethylenediamine tetraacetic acid (EDTA) or higher homologues such as diethylenetriamine pentaacetic acid (DTP A).
  • EDTA ethylenediamine tetraacetic acid
  • DTP A diethylenetriamine pentaacetic acid
  • Deodorant actives other than astringent metal antiperspirant salts are commonly employed at a concentration of from 0.1 to 5, and particularly 0.1 to 2 % by weight.
  • cosmetically acceptable vehicle suitable for use in this invention may be aqueous-based, anhydrous or an emulsion whereby a water-in-oil or oil-in-water emulsion is generally preferred. If the use of water is desired, water typically makes up the balance of the composition, and preferably makes up from 5 to 99 %, and most preferably from 40 to 80 % by weight of the topical composition, including all ranges subsumed therein.
  • organic solvents may be optionally included to act as carriers or to assist carriers within the compositions of the present invention.
  • organic solvents suitable for use in the present invention include alkanols like ethyl and isopropyl alcohol, mixtures thereof or the like.
  • ester oils like isopropyl myristate, cetyl myristate, 2-octyldodecyl myristate, avocado oil, almond oil, olive oil, neopentylglycol dicaprate, mixtures thereof or the like.
  • ester oils assist in emulsifying the composition of this invention, and an effective amount is often used to yield a stable, and most preferably, water-in-oil emulsion.
  • Emollients may also be used, if desired, as carriers within the composition of the present invention. Alcohols like 1-hexadecanol (i.e. cetyl alcohol) are often desired as are the emollients generally classified as silicone oils and synthetic esters.
  • Silicone oils suitable for use include cyclic or linear polydimethylsiloxanes containing from 3 to 9, preferably from 4 to 5, silicon atoms.
  • Non-volatile silicone oils useful as an emollient material in the inventive composition described herein include polyalkyl siloxanes, polyalkylaryl siloxanes and polyether siloxane copolymers.
  • the essentially non-volatile polyalkyl siloxanes useful herein include, for example, polydimethylsiloxanes.
  • ester emollients that may optionally be used are:
  • Alkenyl or alkyl esters of fatty acids having 10 to 20 carbon atoms examples thereof include isoarachidyl neopentanoate, isononyl isonanonoate, oleyl myristate, oleyl stearate, and oleyl oleate.
  • Ether-esters such as fatty acid esters of ethoxylated fatty alcohols.
  • Ethylene glycol mono and di-fatty acid esters diethylene glycol mono- and di-fatty acid esters, polyethylene glycol (200-6000) mono- and di- fatty acid esters, propylene glycol mono- and di-fatty acid esters, polypropylene glycol 2000 monooleate, polypropylene glycol 2000 monostearate, ethoxylated propylene glycol monostearate, glyceryl mono- and di-fatty acid esters, polyglycerol poly-fatty esters, ethoxylated glyceryl mono-stearate, 1,3-butylene glycol monostearate, 1,3-butylene glycol distearate, polyoxyethylene polyol fatty acid ester, sorbitan fatty acid esters, and polyoxyethylene sorbitan fatty acid esters are satisfactory polyhydric alcohol esters.
  • Wax esters such as beeswax, spermaceti, stearyl stearate and arachidyl behenate.
  • Sterols esters of which cholesterol fatty acid esters are examples.
  • Emollients when used typically make up from 0.1 to 50 % by weight of the composition, including all ranges subsumed therein.
  • Fatty acids having from 10 to 30 carbon atoms may also be included as acceptable carriers within the composition of the present invention.
  • Illustrative examples of such fatty acids include pelargonic, lauric, myristic, palmitic, stearic, isostearic, oleic, linoleic, arachidic, behenic or erucic acid, and mixtures thereof.
  • Compounds that are believed to enhance skin penetration, like dimethyl sulfoxide, may also be used as an optional carrier.
  • Humectants of the polyhydric alcohol type may also be employed in the compositions of this invention.
  • the humectant often aids in increasing the effectiveness of the emollient, reduces scaling, stimulates removal of built-up scale and improves skin feel.
  • Typical polyhydric alcohols include glycerol, polyalkylene glycols and more preferably alkylene polyols and their derivatives, including propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol and derivatives thereof, sorbitol, hydroxypropyl sorbitol, hexylene glycol, 1,3-butylene glycol, 1,2,6-hexanetriol, ethoxylated glycerol, propoxylated glycerol and mixtures thereof.
  • the humectant is preferably propylene glycol or sodium hyaluronate.
  • the amount of humectant may range anywhere from 0.2 to 25%, and preferably, from 0.5 to 15 % by weight of the composition, based on total weight of the composition and including all ranges subsumed therein.
  • Thickeners may also be utilized as part of the acceptable carrier in the compositions of the present invention.
  • Typical thickeners include cross-linked acrylates (e.g. Carbopol 982), hydrophobically-modified acrylates (e.g. Carbopol 1382), cellulosic derivatives and natural gums.
  • useful cellulosic derivatives are sodium carboxymethylcellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, ethyl cellulose and hydroxymethyl cellulose.
  • Natural gums suitable for the present invention include guar, xanthan, sclerotium, carrageenan, pectin and combinations of these gums.
  • Amounts of the thickener may range from 0.0 to 5, usually from 0.001 to 1, optimally from 0.01 to 0.5 % by weight of the composition.
  • the water, solvents, silicones, esters, fatty acids, humectants and/or thickeners will constitute the acceptable carrier in amounts from 1 to 99.9, preferably from 80 to 99 % by weight of the composition.
  • Surfactants may also be present in compositions of the present invention. Total concentration of the surfactant will range from about 0 to about 40%, and preferably from about 0 to about 20%, optimally from about 0 to about 5% by weight of the composition.
  • the surfactant may be selected from the group consisting of anionic, nonionic, cationic and amphoteric actives.
  • nonionic surfactants are those with a C10-C20 fatty alcohol or acid hydrophobe condensed with from 2 to 100 moles of ethylene oxide or propylene oxide per mole of hydrophobe; mono- and di- fatty acid esters of ethylene glycol; fatty acid monoglyceride; sorbitan, mono- and di- C8-C20 fatty acids; block copolymers (ethylene oxide/propylene oxide); and polyoxyethylene sorbitan as well as combinations thereof.
  • Alkyl polyglycosides and saccharide fatty amides are also suitable nonionic surfactants.
  • Preferred anionic surfactants include soap, alkyl ether sulfate and sulfonates, alkyl sulfates and sulfonates, alkylbenzene sulfonates, alkyl and dialkyl sulfo succinates, C8-C20 acyl isethionates, acyl glutamates, C8-C20 alkyl ether phosphates and combinations thereof.
  • Perfumes may be used in the composition of this invention.
  • Illustrative non-limiting examples of the types of perfumes that may be used include those comprising terpenes and terpene derivatives like those described in Bauer, K., et al, Common Fragrance and Flavor Materials, VCH Publishers (1990).
  • the amount of fragrance employed in the composition of this invention is in the range from 0.0 to 10, more preferably 0.00001 to 5, most preferably 0.0001 to 2 % by weight of the compound.
  • Various types of optional additional active ingredients may be used in the compositions of the present invention. Actives are defined as skin benefit agents other than emollients and other than ingredients that merely improve the physical characteristics of the composition. Although not limited to this category, general examples include talcs and silicas, as well as alpha-hydroxy acids, beta-hydroxy acids and zinc salts.
  • Beta-hydroxy acids include salicylic acid, for example.
  • Zinc pyrithione is an example of the zinc salts useful in the composition of the present invention.
  • compositions especially those containing water, should be protected against the growth of potentially harmful microorganisms.
  • Anti-microbial compounds such as triclosan, and preservatives are, therefore, typically necessary.
  • Suitable preservatives include alkyl esters of p-hydroxybenzoic acid, hydantoin derivatives, propionate salts, and a variety of quaternary ammonium compounds.
  • Particularly preferred preservatives of this invention are methyl paraben, propyl paraben, phenoxyethanol and benzyl alcohol.
  • Preservatives will usually be employed in amounts ranging from 0.1 to 2 % by weight of the composition.
  • composition of this invention includes dioic acids (e.g. malonic acid and sebacic acid), antioxidants like vitamin E, retinoids, including retinoic acid, retinal, retinol and retinyl esters, conjugated linoleic acid, petroselinic acid and mixtures thereof, as well as any other conventional ingredients well known for wrinkle-reducing, anti-acne effects and reducing the impact of sebum.
  • dioic acids e.g. malonic acid and sebacic acid
  • antioxidants like vitamin E
  • retinoids including retinoic acid, retinal, retinol and retinyl esters, conjugated linoleic acid, petroselinic acid and mixtures thereof, as well as any other conventional ingredients well known for wrinkle-reducing, anti-acne effects and reducing the impact of sebum.
  • the desired ingredients are mixed in no particular order and usually at temperatures from 70 to 80 °C and under atmospheric pressure.
  • the packaging for the composition of this invention can be a patch, bottle, tube, roll-ball applicator, propellant driven aerosol device, squeeze container or lidded jar.
  • the composition according to the invention may be used as a medicament, more specifically for skin lightening.
  • use of climbazole and lipoic acid in the manufacture of a composition of the invention is provided for lightening skin.
  • use of a composition according to the invention is provided for lightening skin.
  • a method of lightening the skin of a human is provided, the method comprising the step of applying the composition of the invention to skin of a person in need thereof.
  • MatTek MelanoDermTM cultures (a pigmented 3D-Living Skin Equivalent (LSE) model) purchased from the MatTek Corporation. Dark cultures (MEL-300-B), for evaluation of skin lightening potential, were prepared in a long life maintenance medium (EPI-IOO-LLMM available from the MatTek Corporation) for good pigment production whilst preserving acceptable histology.
  • LSE Skin Equivalent
  • Test actives were applied to the samples by addition to the growth medium. Fresh growth medium containing dimethyl sulphoxide (DMSO) alone or test actives was replaced every 2-3 days and the cultures were grown in this way for 14 days prior to harvesting and analysis. Prior to extraction or fixation cultures were assayed using the WST-1 cell proliferation assay. 1.1.2 B 16 monolay er culture s
  • B16 mouse melanoma cells were cultured in Eagle's minimal essential medium (EMEM) supplemented with 10% foetal calf serum (FCS) and 2mM L-glutamine at 37 °C, 5 % C02 in T175 tissue culture flasks and were sub-cultured twice weekly using trypsin in EDTA.
  • EMEM Eagle's minimal essential medium
  • FCS foetal calf serum
  • L-glutamine 2mM L-glutamine
  • EDTA ethylenediaminetetraacetic acid
  • DPBS Dulbecco's Phosphate Buffered Saline
  • Table 1 Normalised melanin ⁇ g per mg protein) from B16 monolayer cultures for a number of azoles (the first DMSO control relates to the climbazole results only and the second DMSO control relates to the remaining results).
  • Table 2 Normalised melanin ⁇ g per mg protein) from B16 monolayer cultures for climbazole.
  • Table 3 Normalised melanin (per mg protein) for climbazole from MelanoDermTM cultures.
  • Climbazole very effectively inhibits melanin production in B16 monolayer cultures and MelanoDermTM cultures at concentrations of 20 and 50 ⁇ . Furthermore there is no detectable effect on the viability of epidermal cultures at this dose. Surprisingly other azoles and in particular fluconazole, imidazole, oxazole and thiazole did not effectively inhibit melanin production in B16 monolayer cultures at 20 ⁇ .
  • B16 F10 cells (mouse melanoma cell line) were obtained from ATCC and grown in Lonza Biowhittaker BE12-662F media. Trypsin in ethylenediaminetetraacetic acid (EDTA) (Sigma T3924) and Dulbecco's Phosphate Buffered Saline (DPBS) (Sigma D8537) were used to split the cells. Plates were set up at a concentration of 2.5 x 10 4 cells per well in 48 well plates in Phenol Red free media (Sigma Dl 145).
  • EDTA ethylenediaminetetraacetic acid
  • DPBS Dulbecco's Phosphate Buffered Saline
  • lipoic acid LipoecTM from Cognis which is 99 % lipoic acid itself comprises a racemic mixture of R- and S- lipoic acids
  • lipoic acid LipoecTM from Cognis which is 99 % lipoic acid itself comprises a racemic mixture of R- and S- lipoic acids
  • Table 4 Melanin ⁇ g) per mg protein from B16 monolayer cultures for the combination of climbazole and lipoic acid.

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Abstract

Obtenir une couleur de peau souhaitée est un besoin majeur non satisfait des consommateurs en Asie. Les consommateurs souhaitent particulièrement une couleur de peau uniforme, l'absence de taches de vieillesse (lentigo solaire) et un teint d'ensemble plus clair. Une solution consiste à utiliser des agents actifs biologiques qui réduisent l'activité des mélanocytes dans la peau. Ces cellules, présentes dans la couche basale de l'épiderme, fabriquent la mélanine (pigment foncé) et l'exportent dans de petits vésicules d'export appelés mélanosomes vers les kératinocytes voisins. Il est bien décrit dans la littérature que, lorsqu'ils sont appliqués de façon topique sur la peau, les composés qui réduisent la synthèse de la mélanine réduisent la tendance à foncer de la peau avec le temps. La présente invention concerne une composition comprenant du climbazole destiné à être utilisé dans l'éclaircissement de la peau. La présente invention est fondée sur le fait que le climbazole inhibe la production de pigment dans des cultures de monocouches B16 et MelanoDerm™. Ainsi le climbazole, lorsqu'il est appliqué de façon topique sur une période de temps appropriée in-vivo, devrait provoquer l'éclaircissement de la peau, ou réduire les défauts et/ou les taches hyperpigmentées et/ou le lentigo solaire, conduisant à une amélioration du teint et de l'uniformité.
PCT/EP2012/074534 2011-12-07 2012-12-05 Composition éclaircissante pour la peau WO2013083645A2 (fr)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108348783A (zh) * 2015-11-17 2018-07-31 荷兰联合利华有限公司 氯咪巴唑微囊和包含表面活性剂和氯咪巴唑的毛发护理组合物

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WO1995034280A1 (fr) 1994-06-15 1995-12-21 The Procter & Gamble Company Procedes permettant d'eclaircir des regions hyperpigmentees de la peau d'un mammifere
WO2010121919A1 (fr) 2009-04-23 2010-10-28 Unilever Plc Composition de soin capillaire comprenant un complexe trichogénique et un azole

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