Classifications

• • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
  • A61K8/0295—Liquid crystals
• • 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
• • 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
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/37—Esters of carboxylic acids
  • A61K8/375—Esters of carboxylic acids the alcohol moiety containing more than one hydroxy group
• • 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
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/38—Percompounds, e.g. peracids
• • 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
  • A61K8/60—Sugars; Derivatives thereof
• • 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
  • A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof
  • A61K8/66—Enzymes

Definitions

• the present invention relates to cosmetic compositions.
• cosmetic compositions with high moisturisation efficacy without high levels of tack.
• the compositions further display good in-use rub-in and absorption characteristics, as well as excellent skin feel, skin softness, and skin smoothness benefits.
• Skin is made up of several layers of cells which coat and protect the keratin and collagen fibrous proteins that form the skeleton of its structure.
• the outermost of these layers, referred to as the stratum corneum is known to be composed of 25nm protein bundles surrounded by 8nm thick layers.
• Anionic surfactants and organic solvents typically penetrate the stratum corneum membrane and, by delipidization (i.e. removal of the lipids from the stratum corneum), destroy its integrity. This destruction of the skin surface topography leads to a rough feel and may eventually permit the surfactant or solvent to interact with the keratin, creating irritation.
• compositions which will assist the stratum corneum in maintaining its barrier and water-retention functions at optimum performance in spite of deleterious interactions which the skin may encounter in washing, work, and recreation.
• Desirable properties of cosmetic cream and lotion compositions are good skin feel, water retention, moisturisation, abso ⁇ tion, and rub-in characteristics.
• the skin feel of a composition perceived by the consumer as skin softness or skin smoothness, is related to the emollients of a composition which form a film or layer upon application to the skin.
• the abso ⁇ tion and rub-in characteristics of a composition relate to its physical behaviour under mechanical stress which is affected by the rheological profile of the composition.
• compositions which show low levels of stickiness or tack whilst providing high levels of moisturisation, as well as providing excellent skin feel, skin softness and skin smoothness benefits.
• a composition is provided with low levels of stickiness or tack.
• the compositions also show good abso ⁇ tion and water retention properties, in addition to skin feel, skin softness and skin smoothness benefits and excellent moisturisation characteristics.
• Emulsifiers capable of forming liquid crystals in water are known for use in cosmetic compositions.
• a leave-on cosmetic composition suitable for topical application to the skin comprising:
• compositions of the invention display high moisturisation efficacy without the associated high levels of tack, as well as good rheological and abso ⁇ tion properties, in addition to skin feel, skin softness and skin smoothness benefits.
• a cosmetic method of treatment of the skin comprising applying to the skin a composition according to the present invention.
• a use of an emulsifier capable of forming liquid crystals in water for reducing tack in a skin care composition comprising from greater than about 20% to less than about 80% of a polyhydric alcohol, or mixtures thereof.
• a use of a composition comprising from greater than about 20% to less than about 80% of a polyhydric alcohol, or mixtures thereof; and an emulsifier capable of forming liquid crystals in water for a leave-on skin care application.
• compositions of the present invention comprise a polyhydric alcohol together with an essential emulsifier component, as well as various optional ingredients as indicated below. All levels and ratios are by weight of total composition, unless otherwise indicated. Chain length and degrees of ethoxylation are also specified on a weight average basis.
• tack or "tackiness”, as used herein, in relation to a leave-on composition means the ability of a composition to lightly bond to skin surfaces where the composition has been applied, upon the application of light pressure and within a short time-scale.
• sticking or "sticky” as used herein, is a term often used by consumers to describe their perception of the tack, either actual or perceived of a composition.
• the term "leave-on" in relation to skin care compositions means that it intended to be used without a rinsing step, such that after applying the composition to the skin, the leave-on composition is preferably left on the skin for a period of at least about 15 minutes, more preferably at least about 30 minutes, even more preferably at least about 1 hour, most preferably for at least several hours, e.g., up to about 12 hours or more.
• skin conditioning agent means a material which is capable of providing a cosmetic conditioning benefit to the skin such as moisturization, humectancy
• enzyme as used herein means the enzyme, wild-type or variant, either per se, or chemically modified by the conjugation of polymer moieties.
• wild-type refers to an enzyme produced by unmutated hosts.
• variable means an enzyme having an amino acid sequence which differs from that of the wild-type enzyme due to the genetic mutation of the host producing that enzyme.
• the present compositions can be used for any suitable pu ⁇ ose.
• the present compositions are suitable for topical application to the skin.
• the skin care compositions can be in the form of creams, lotions, gels, and the like.
• the cosmetic compositions herein are in the form of an emulsion of one or more oil phases in an aqueous continuous phase.
• compositions herein comprise at least one polyhydric alcohol.
• the compositions of the present invention preferably comprise from greater than about 20%) to less than about 80%, more preferably from about 22% to about 10%, and especially from about 25% to about 60% by weight of the polyhydric alcohol, or mixtures thereof.
• Suitable polyhydric alcohols for use herein include 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, erythritol, threitol, pentaerythritol, xylitol, glucitol, mannitol, hexylene glycol, butylene glycol (e.g., 1,3-butylene glycol), hexane triol (e.g., 1,2,6- hexanetriol), trimethylol propane, neopentyl glycol, glycerine, ethoxylated glycerine and propoxylated glycerine.
• alkylene polyols and their derivatives including propylene glycol, dipropylene glycol, polypropylene glyco
• Preferred polyhydric alcohols of the present invention are selected from glycerine, butylene glycol, propylene glycol, dipropylene glycol, polyethylene glycol and derivatives thereof, hexane triol, ethoxylated glycerine and propoxylated glycerine, or mixtures thereof.
• polyhydric alcohols for use in the present invention are glycerine, butylene glycol, or mixtures thereof.
• the compositions herein comprise an emulsifier which is capable of forming liquid crystals in water. It is not essential that the composition herein comprises liquid crystals at ambient temperature. Gel networks are commonly formed from liquid crystals as a result of cooling during the manufacturing procedure. It has been found that compositions that form gel networks at ambient temperature give excellent results.
• liquid crystals are also referred to as anisotropic fluids, a fourth state of matter, surfactant association structure or mesophases. Those terms are often used interchangeably.
• the term "lytropic" means a liquid crystalline system containing a polar solvent, such as water.
• the liquid crystals used herein are lamellar, hexagonal, or rod structures or mixtures thereof.
• liquid crystalline phase utilised in the compositions of the invention can be identified in various ways.
• a liquid crystal phase flows under shear and is characterised by a viscosity that is significantly different from the viscosity of its isotropic solution phase.
• liquid crystals or the gel networks formed at ambient temperature show identifiable birefringence, as, for example, plain lamellar birefringence, whereas when isotropic solutions and rigid gels are viewed under polarised light, both show dark fields.
• Other suitable means for identifying liquid crystals include x-ray diffraction, NMR spectroscopy and transmission electron microscopy.
• the emulsifier herein is a mixture comprising at least one emulsifier having a high HLB (hyrophilic lipophilic balance), and at least one emulsifier having a low HLB.
• HLB high lipophilic balance
• the ratio of low HLB emulsifier to high HLB emulsifier in the mixture is from about 10 : 1 to about 100 : 1.
• the emulsifier is inco ⁇ orated into the composition in an amount of from about 2% to about 45%, preferably from about 3% to about 40%, more preferably from about 3% to about 30%, by weight of the composition.
• Low HLB emulsifiers suitable for the present invention have an HLB of 1 to 8 and a melting point of at least 45°C.
• suitable low HLB emulsifiers for use in the compositions of this invention include the following: saturated C, 6 to C 30 fatty alcohols, such as cetyl, stearyl and behenyl alcohols; saturated C 16 to C 30 hydroxy fatty acids, such as palmitic, stearic, behenic and hydroxystearic acids; C 8 to C 24 mono- or polyglycerol esters, such as triglycerol stearate and triglycerol distearate; C 8 to C 24 polyol mono-, di- or tri-fatty acid esters such as sorbitan stearate, available under the trade name Arlacel 60 from ICI, Wilton, Middlesborough, U.K., sorbitan tristearate, available under the trade name Arlacel 65 from ICI, methyl glucose sequisterate, available under the trade name
• C 8 to C 30 glyceryl esters such as glyceryl monostearate or distearate (40 - 60%> mono), glyceryl monostearate, palmitate or laurate (90%> mono) and glyceryl hydroxystearate; and saturated C 16 to C 30 ethoxylated fatty alcohols containing from about 1 to about 5 moles of ethylene oxide, such as steareth 2, available under the trade name Brij 72 from ICI, ceteth 2, available under the trade name Brij 52 from ICI, and beheneth 5 available under the trade name Nikkol BB-5 from Nikko Chemical Co., Ltd, Tokyo, Japan; and mixtures thereof.
• glyceryl esters such as glyceryl monostearate or distearate (40 - 60%> mono), glyceryl monostearate, palmitate or laurate (90%> mono) and glyceryl hydroxystearate
• the low HLB emulsifiers useful herein are selected from the group consisting of saturated C l6 to C 30 fatty alcohols; saturated C 16 to C 30 ethoxylated fatty alcohols containing from about 1 to about 5 moles of ethylene oxide; C 8 to C 24 mono or polyglycerol esters; C 8 to C 24 polyol mono-, di-, or tri-fatty acid esters, wherein the polyol is preferably selected from dextrin, sugars, or sorbitan; saturated C 16 to C 30 hydroxy fatty acids; and mixtures thereof.
• Preferred low HLB emulsifiers for use herein include C 8 to C 24 polyol mono-fatty acid esters wherein the polyol is sorbitan; saturated C, 6 to C 30 fatty alcohols; saturated C, 6 to C 30 ethoxylated fatty alcohols and mixtures thereof.
• C 8 to C 24 sorbitan fatty acid esters are more preferred.
• Most preferred are glyceryl monostearate, stearyl alcohol, sorbitan stearate, cetyl alcohol, or mixtures thereof.
• a particularly preferred low HLB emulsifier is sorbitan stearate.
• High HLB emulsifiers have an HLB greater than 8.
• Suitable high HLB emulsifiers useful herein are cationic, anionic or nonionic. Preferred are nonionic.
• Suitable examples of nonionic high HLB emulsifiers include the following: alkoxylated ethers of C, - C 30 fatty alcohols, such as Steareth 10, available under the trade name Brij 76 from ICI, Wilton, Middlesborough, U.K., Steareth 20, available under the trade name Brij 78 from ICI, Steareth 21, available under the trade name Brij 721 from ICI, Steareth 100, available under the trade name Brij 700 from ICI, and Ceteareth -12, available under the trade name Emulgin BI from Henkel, La Grange, Illinois, U.S.A.; alkoxylated derivatives of C, - C 30 fatty acids, such as PEG-20-stearate, available under the trade name Myrj 49 from ICI, P
• alkyl polyoxyalkylene sugar esters such as polysorbate 60, available under the trade name Tween 60 from ICI, PEG-20-methyl glucose sesquistearate, available under the trade name Glucamate SSE 20 from Amerchol, Edison, New Jersey, U.S.A., and PEG-20-glyceryl monostearate, available under the trade name Tagat S2 from Goldschmidt, Hopewell, Virginia, U.S.A.
• mono-, di- or tri- sucrose fatty acid esters preferably sucrose mono-fatty acid esters, such as sucrose cocoate, available under the trade name Crodesta SL-40 from Croda Surfactants, Goole, England, sucrose palmitate, available under the trade name Ryoto Sugar Ester P-1570 from Mitsubishi-Kasei, Tokyo, Japan, and sucrose stearate, available under the trade name Crodesta F-160 from Croda Surfactants; poly
• Suitable anionic high HLB emulsifiers useful herein include lactates, such as sodium stearoyl lactylate, available from Nikko Chemical Co., Ltd; phosphonic acid esters and salts, such as diethanolamine cetyl phosphate, available under the trade name Amphisol from Givaudan-Roure, Clifton, New Jersey, U.S.A., and potassium cetyl phosphate, available under the trade name Amphisol K from Nikko Chemical Co., Ltd; and sulphuric acid esters, such as sodium cocomonoglyceride sulphate, available from Nikko Chemical Co., Ltd; and mixtures thereof.
• lactates such as sodium stearoyl lactylate, available from Nikko Chemical Co., Ltd
• phosphonic acid esters and salts such as diethanolamine cetyl phosphate, available under the trade name Amphisol from Givaudan-Roure, Clifton, New Jersey, U.S.A., and potassium cet
• Suitable cationic high HLB emulsifiers useful herein include tetra-alkyl ammonium salts, such as dicetyl or distearyl dimethyl ammonium chloride, available from Witco, Greenwich, Connecticut, U.S.A.; and fatty acid amides, such as steapyrium chloride, available from Witco; and mixtures thereof.
• Preferred high HLB emulsifiers for use herein are C,-C 30 ethers of polyols; alkoxylated ethers of C,-C 30 fatty alcohols; or mono-, di- or tri- sucrose fatty acid esters; or mixtures thereof.
• the monoester preferably comprises at least 70%, more preferably 80%, by weight of total sucrose ester mixture.
• Most preferred high HLB emulsifiers are mono-, di- or tri-sucrose fatty acid esters.
• a particularly preferred high HLB emulsifier is sucrose cocoate.
• An emulsifier for use herein is most preferably a fatty acid ester blend based on a mixture of sorbitan fatty acid ester and sucrose fatty acid ester, especially a blend of sorbiton stearate and sucrose cocoate. This is commercially available from ICI under the trade name Arlatone 2121.
• the concentration of the combined polyhydric alcohol and emulsifier is in the range of from about 10%> to about 99%>, preferably about 15% to about 95%> and especially about 20%> to about 90%> by weight of the composition.
• the cosmetic compositions herein are in the form of an emulsion of one or more oil phases in an aqueous continuous phase, each oil phase comprises a single oily component or a mixture of oily components in miscible or homogeneous form. Different oil phases contain different materials or combinations of materials from each other.
• the total level of oil phase components in the compositions of the invention is typically from about 0.1%) to about 60%, preferably from about 1% to about 30%>, more preferably from about 1% to about 10%.
• the oil phase components of the compositions herein comprise an emollient material or mixtures thereof, and a silicone oil, or mixtures thereof.
• the oil phase preferably comprises additional oily components such as a natural or synthetic oils selected from mineral, vegetable, and animal oils, fats and waxes, and mixtures thereof. These oily components are present in an amount of from about 0.1 % to about 15%, more preferably from about 1% to about 10%> by weight of composition.
• additional oily components such as a natural or synthetic oils selected from mineral, vegetable, and animal oils, fats and waxes, and mixtures thereof.
• these oily components are present in an amount of from about 0.1 % to about 15%, more preferably from about 1% to about 10%> by weight of composition.
• Preferred for use herein are for example, hydrocarbons such as mineral oils or petrolatum. Further examples suitable for use herein are disclosed in WO98/22085.
• compositions of the present invention can comprise emollient materials selected from branched chain hydrocarbons having an weight average molecular weight of from about 100 to about 15,000, preferably from about 100 to 1000; compounds of formula I:
• R 3 OR 4 Formula I wherein Ri is selected from H or CH3, R ⁇ , R3 and R 4 are independently selected from C1 -C20 straight chain or branched chain alkyl, and x is an integer of from 1-20; and compounds having the formula (II):
• R ⁇ is selected from optionally hydroxy or C1-C4 alkyl substituted benzyl and Rg is selected from C1-C20 branched or straight chain alkyl; and mixtures thereof.
• Suitable branched chain hydrocarbons for use herein are selected from isododecane, isohexadecane, isoeicosane, isooctahexacontane, isohexapentacontahectane, isopentacontaoctactane, petrolatum, and mixtures thereof.
• Suitable for use herein are branched chain aliphatic hydrocarbons sold under the trade name Permethyl (RTM) and commercially available from Presperse Inc., P.O. Box 735, South Plainfield, NJ. 07080, U.S.A.
• Suitable ester emollient materials of Formula I above include, but are not limited to, methyl isostearate, isopropyl isostearate, isostearyl neopentanoate. isononyl isononanoate, isodecyl octanoate, isodecyl isononanoate, tridecyl isononanoate, myristyl octanoate, octyl pelargonate, octyl isononanoate, myristyl myristate, myristyl neopentanoate, myristyl octanoate, myristyl propionate, isopropyl myristate and mixtures thereof.
• Suitable ester emollient materials of Formula (II) include but are not limited to C12-15 alkyl benzoates.
• Preferred emollients for use herein are isohexadecane, isooctacontane, petrolatum, isononyl isononanoate, isodecyl octanoate, isodecyl isononanoate, tridecyl isononanoate, myristyl octanoate, octyl isononanoate, myristyl myristate, methyl isostearate, isopropyl isostearate, C12-15 alkyl benzoates and mixtures thereof.
• emollients for use herein are isohexadecane, isononyl isononanoate, methyl isostearate, isopropyl isostearate, petrolatum, or mixtures thereof.
• the emollient material is preferably present in the compositions at a level of from about 0.1%) to about 10%, preferably from about 0.1% to about 8%, especially from about 0.5%> to about 5% by weight of composition.
• compositions of the present invention may further comprise as an additional emollient, a polyol carboxylic acid ester.
• compositions of the present invention preferably comprise from about 0.01% to about 20%), more preferably from about 0.1 % to about 15%>, and especially from about 0.1%) to about 10% by weight of the polyol ester.
• the level of polyol ester by weight of the oil in the composition is preferably from about 1% to about 30%, more preferably from about 5% to about 20%.
• the weight ratio of the carboxylic acid polyol ester to the emollient material is preferably in the range of from about 5: 1 to about 1:5, more preferably in the range of from 2: 1 to about 1:2.
• the preferred polyol polyesters useful in this invention are C1 -C30 mono- and polyesters of sugars and related materials.
• esters are derived from a sugar or polyol moiety and one or more carboxylic acid moieties. Depending on the constituent acid and sugar, these esters can be in either liquid or solid form at room temperature. Examples include: glucose tetraoleate, the galactose tetraesters of oleic acid, the sorbitol tetraoleate, sucrose tetraoleate.
• Other materials include cottonseed oil or soybean oil fatty acid esters of sucrose. Other examples of such materials are described in WO 96/16636, inco ⁇ orated by reference herein. A particularly preferred material is known by the NCI name sucrose polycottonseedate.
• compositions may comprise at least one silicone oil phase.
• Silicone oil phase(s) generally comprises from about 0.1 %> to about 20%>, preferably from about 0.5% to about 10%), more preferably from about 0.5% to about 5%, of the composition.
• The, or each, silicone oil phase preferably comprises one or more silicone components.
• Silicone components can be fluids, including straight chain, branched and cyclic silicones.
• Suitable silicone fluids useful herein include silicones inclusive of polyalkyl siloxane fluids, polyaryl siloxane fluids, cyclic and linear polyalkylsiloxanes, poly- alkoxylated silicones, amino and quaternary ammonium modified silicones, polyalkylaryl siloxanes or a polyether siloxane copolymer and mixtures thereof.
• the silicone fluids can be volatile or non-volatile.
• Silicone fluids generally have a weight average molecular weight of less than about 200,000. Suitable silicone fluids have a molecular weight of about 100,000 or less, preferably about 50,000 or less, most preferably about 10,000 or less.
• the silicone fluid is selected from silicone fluids having a weight average molecular weight in the range from about 100 to about 50,000 and preferably from about 200 to about 40,000.
• silicone fluids have a viscosity ranging from about 0.65 to about 600,000 mm 2 ⁇ " 1 , preferably from about 0.65 to about 10,000 mrn 2 ⁇ ' 1 at 25°C. The viscosity can be measured by means of a glass capillary viscometer as set forth in Dow Corning Co ⁇ orate Test Method CTM0004, July 29, 1970.
• Suitable polydimethyl siloxanes that can be used herein include those available, for example, from the General Electric Company as the SF and Viscasil (RTM) series and from Dow Corning as the Dow Corning 200 series. Also useful are essentially non-volatile polyalkylarylsiloxanes, for example, polymethylphenylsiloxanes, having viscosities of about 0.65 to 30,000 mm ⁇ .s'l at 25°C. These siloxanes are available, for example, from the General Electric Company as SF 1075 methyl phenyl fluid or from Dow Corning as 556 Cosmetic Grade Fluid. Cyclic polydimethylsiloxanes suitable for use herein are those having a ring structure inco ⁇ orating from about 3 to about 7 (CH3)2SiO moieties.
• the silicone fluid is selected from dimethicone, decamethylcyclopentasiloxane, octamethylcyclotetrasiloxane, phenyl methicone, and mixtures thereof.
• Silicone gums can also be used herein.
• the term "silicone gum” herein means high molecular weight silicones having a weight average molecular weight in excess of about 200,000 and preferably from about 200,000 to about 4,000,000. Iincluded are non- volatile polyalkyl and polyaryl siloxane gums.
• a silicone oil phase comprises a silicone gum or a mixture of silicones including the silicone gum.
• silicone gums typically have a viscosity at 25°C in excess of about 1,000,000 mm ⁇ s'l.
• the silicone gums include dimethicones as described by Petrarch and others including US-A-4, 152,416, May 1, 1979 to Spitzer, et al, and Noll, Walter, Chemistry and Technology of Silicones. New York: Academic Press 1968. Also describing silicone gums are General Electric Silicone Rubber Product Data Sheets SE 30, SE 33, SE 54 and SE 76.
• silicone gums include polydimethylsiloxane, (polydimethylsiloxane)(methylvinylsiloxane) copolymer, poly(dimethylsiloxane)- (diphenyl)(methylvinylsiloxane) copolymer and mixtures thereof.
• Preferred silicone gums for use herein are silicone gums having a molecular weight of from about 200,000 to about 4,000,000 selected from dimethiconol, and dimethicone and mixtures thereof.
• a silicone phase herein preferably comprises a silicone gum inco ⁇ orated into the composition as part of a silicone gum- fluid blend.
• the silicone gum when the silicone gum is inco ⁇ orated as part of a silicone gum-fluid blend, the silicone gum preferably constitutes from about 5% to about 40%>, especially from about 10% to 20% by weight of the silicone gum- fluid blend.
• Suitable silicone gum-fluid blends herein are mixtures consisting essentially of:
• a carrier which is a silicone fluid, the carrier having a viscosity from about 0.65 mm ⁇ .s"! to about 100 mm ⁇ .s'l,
• the ratio of i) to ii) is from about 10:90 to about 20:80 and wherein said silicone gum-based component has a final viscosity of from about 100 mm ⁇ .s"' to about 100,000 mm ⁇ .s"!, preferably from 500 mm ⁇ .s ' l to about 10,000 mm ⁇ .s'l.
• An especially preferred silicone-gum fluid blend based component for use in the compositions herein is a dimethiconol gum having a molecular weight of from about 200,000 to about 4,000,000 along with a silicone fluid carrier with a viscosity of about
• crosslinked polyorganosiloxane polymers are crosslinked polyorganosiloxane polymers, optionally dispersed in a fluid carrier.
• the crosslinked polyorganosiloxane polymers together with its carrier (if present) comprises 0.1% to about 20%>, preferably from about 0.5%> to about 10%, more preferably from about 0.5%> to about 5% of the composition.
• Such polymers comprise polyorganosiloxane polymers crosslinked by a crosslinking agent. Suitable crosslinking agents are disclosed in WO98/22085. Examples of suitable polyorganosiloxane polymers for use herein include methyl vinyl dimethicone, methyl vinyl diphenyl dimethicone and methyl vinyl phenyl methyl diphenyl dimethicone.
• crosslinked polyorganosiloxane polymers for use herein are silicone vinyl crosspolymer mixtures available under the tradename KSG supplied by Shinetsu Chemical Co., Ltd, for example KSG- 15, KSG-16, KSG-17, KSG-18. These materials contain a combination of crosslinked polyorganosiloxane polymer and silicone fluid. Particularly preferred for use herein especially in combination with the organic amphiphilic emulsifier material is KSG-18.
• the assigned NCI names for KSG- 15, KSG- 16, KSG-17 and KSG-18 are cyclomethicone dimethicone/vinyl dimethicone crosspolymer, dimethicone dimethicone/vinyl dimethicone crosspolymer, cyclomethicone dimethicone/vinyl dimethicone crosspolymer and phenyl trimethicone dimethicone/phenyl vinyl dimethicone crosspolymer, respectively.
• silicone components suitable for use in a silicone oil phase herein includes polydiorganosiloxane-polyoxyalkylene copolymers containing at least one polydiorganosiloxane segment and at least one polyoxyalkylene segment.
• Suitable polydiorganosiloxane segments and copolymers thereof are disclosed in WO98/22085.
• Suitable polydiorganosiloxane-polyalkylene copolymers are available commercially under the tradenames Belsil (RTM) from Wacker-Chemie GmbH, Geschafts Symposium S,
• a particularly preferred copolymer fluid blend for use herein includes Dow Corning DC3225C which has the CTFA designation Dimethicone/Dimethicone copolyol.
• compositions of the present invention can comprise at least one polymeric thickening agent.
• the polymeric thickening agents useful herein preferably have a number average molecular weight of greater than 20,000, more preferably greater than 50,000 and especially greater than 100,000.
• compositions of the present invention may comprise from about 0.01% to about 10%), preferably from about 0.1 % to about 8%> and most preferably from about 0.5% to about 5%> by weight of the composition of the polymeric thickening agent, or mixtures thereof.
• compositions comprising polyol like humectants and polymeric thickening agents
• a physical association of the polyol like humectant with any polymeric thickening agents present in the composition may occur.
• This physical association between the polyol like humectant and the polymeric thickening agents may further exacerbate the stickiness already displayed in compositions comprising high levels of polyol like humectants alone.
• Preferred polymer thickening agents for use herein include non-ionic thickening agents and anionic thickening agents, or mixtures thereof.
• Suitable non-ionic thickening agents include polyacrylamide polymers, crosslinked poly(N-vinylpyrrolidones), polysaccharides, natural or synthetic gums, polyvinylpyrrolidone, and polyvinylalcohol.
• Suitable anionic thickening agents include acrylic acid/ethyl acrylate copolymers, carboxyvinyl polymers and crosslinked copolymers of alkyl vinyl ethers and maleic anhydride.
• Particularly preferred thickening agents for use herein are the non-ionic polyacrylamide polymers such as polyacrylamide and isoparaffin and laureth-7, available under the trade name Sepigel 305 from Seppic Co ⁇ oration, and acrylic acid/ethyl acrylate copolymers and the carboxyvinyl polymers sold by the B.F. Goodrich Company under the trade mark of Carbopol resins, or mixtures thereof.
• Suitable Carbopol resins may be hydrophobically modified, and other suitable resins are described in WO98/22085, or mixtures thereof.
• compositions of the present invention may comprise additional humectants which are preferably present at a level of from about 0.01% to about 20%>, more preferably from about 0.1%> to about 15%> and especially from about 0.5% to about 15%).
• Suitable additional humectants useful herein are sodium 2-pyrrolidone-5-carboxylate (NaPCA), guanidine; glycolic acid and glycolate salts (e.g. ammonium and quaternary alkyl ammonium); lactic acid and lactate salts (e.g. ammonium and quaternary alkyl ammonium); aloe vera in any of its variety of forms (e.g., aloe vera gel); hyaluronic acid and derivatives thereof (e.g., salt derivatives such as sodium hyaluronate); lactamide monoethanolamme; acetamide monoethanolamme; urea; panthenol and derivatives thereof; and mixtures thereof.
• NaPCA sodium 2-pyrrolidone-5-carboxylate
• guanidine glycolic acid and glycolate salts
• lactic acid and lactate salts e.g. ammonium and quaternary alkyl ammonium
• aloe vera in
• At least part (up to about 5% by weight of composition) of an additional humectant can be inco ⁇ orated in the form of an admixture with a particulate cross-linked hydrophobic acrylate or methacrylate copolymer, itself preferably present in an amount of from about 0.1% to about 10%), which can be added either to the aqueous or disperse phase.
• This copolymer is particularly valuable for reducing shine and controlling oil while helping to provide effective moisturization benefits and is described in further detail by WO96/03964, inco ⁇ orated herein by reference.
• Preferred additional humectants are selected from urea, panthenol and mixtures thereof.
• the compositions of the present invention comprise one or more enzymes selected from proteases, lipases, phospholipases, glycosidases, lactoperoxidases, cellulases, and mixtures thereof, especially proteases.
• the enzymes are preferably present at a level of from about 0.0001%) to about 5%, more preferably from about 0.0005% to about 1 %, and especially about 0.001 % to about 0.1 %>, by weight of the composition.
• Protease enzymes are classified under the Enzyme Classification number E.C. 3.4 (Carboxylic Ester Hydrolases) in accordance with the Recommendations (1992) of the International Union of Biochemistry and Molecular Biology (IUBMB).
• proteases are also described in PCT publications: WO 95/30010 published November 9, 1995 by The Procter & Gamble Company; WO 95/30011 published November 9, 1995 by The Procter & Gamble Company; WO 95/29979 published November 9, 1995 by The Procter & Gamble Company.
• Preferred protease enzymes for use herein are subtilisin, chymotrypsin and elastase-type protease enzymes.
• subtilisin-type protease enzymes are naturally produced by Bacillus alcalophilus, Bacillus amyloliquefaciens, Bacillus amylosaccharicus, Bacillus licheniformis, Bacillus lentus and Bacillus subtilis microorganisms.
• a particularly preferred substilisin-type enzyme is bacterial serine protease enzyme, and variants thereof, obtained from Bacillus amyloliquefaciens, Bacillus licheniformis and/or
• Bacillus subtilis including Novo Industries A/S Alcalase®, Esperase® , Savinase®
• protease enzymes and variants thereof, obtained from Bacillus amyloliquefaciens.
• Bacillus amyloliquefaciens One known enzyme is BPN'.
• the wild-type BPN' from Bacillus amyloliquefaciens is characterized by the amino acid sequence:
• protease D Another preferred BPN' variant protease, hereafter referred to as "Protease D", is described in WO 95/10615 published April 20, 1995 by Genencor International as characterized by the wild-type BPN' amino acid with mutation to position Asn76, in combination with mutations in one or more other amino acid positions selected from the group consisting of Asp99, SerlOl, Glnl03, Tyrl04, Serl05, Ilel07, Asnl09, Asnl23, Leul26, Glyl27, Glyl28, Leul35, Glul56, Glyl66, Glul95, Aspl97, Ser204, Gln206, Pro210, Ala216, Tyr217, Asn218, Met222, Ser260, Lys265, and/or Ala274.
• Protease F Another preferred BPN' variant protease, hereafter referred to as "Protease F", is described in U.S. Patent Number 4,760,025, issued to Estell, et al. on July 26, 1988 as characterized by the wild-type BPN' amino acid with mutation to one or more amino acid positions selected from the group consisting of Asp32, Ser33, His64, Tyrl04, Asnl55, Glu 156, Gly 166, Gly 169, Phe 189, Tyr217, and Met222.
• Preferred proteolytic enzymes are selected from the group consisting of Alcalase®, BPN', Protease A, Protease B, Protease D, and Protease F, and mixtures thereof. Protease F is most preferred.
• proteases which are designed to maintain high levels of activity whilst at the same time diminish potential allergenic responses.
• proteases include chemically modified proteases such as those described in WO99/06071 wherein protease molecules are modified with a plurality of twin polymer moieties conjugated to the protease, and those described in co-pending US Application No. 09/088912 filed on June 8, 1998 by The Procter and Gamble Company.
• proteases designed to display reduced allergenicity, yet maintain high activity are protease molecules whose epitope regions have been mapped and subsequently altered by removing, changing, or masking regions of the epitope amino acid sequence.
• Epitope regions are those active amino acid regions of the protease which are believed to invoke an allergic response. Suitable examples of such protease variants useful herein include those described in copending US Application Nos. 60/079447, filed March 26, 1998 and 60/079397, filed March 26, 1998 by The Procter and Gamble Company, herein both inco ⁇ orated by reference.
• compositions of the present invention may also comprise a salt selected from alkali metal and alkaline earth metal salts, and mixtures thereof, preferably sodium, calcium and magnesium salts and mixtures thereof. Especially preferred for use herein are calcium and magnesium salts.
• the compositions herein preferably comprise from about 50 ppm to about 400 ppm of the salt, based on the amount of metal ion.
• a wide variety of optional ingredients such as additional thickening agents, neutralising agents, perfumes and colouring agents can also be added to the skin compositions herein.
• Neutralizing agents suitable for use in neutralizing acidic group containing hydrophilic gelling agents herein include sodium hydroxide, potassium hydroxide, ammonium hydroxide, monoethanolamine, diethanolamine, amino methyl propanol, tris-buffer and triethanolamine.
• compositions of the invention are generally in emulsion form and are preferably formulated so as to have a product viscosity of at least about 4,000 mPa.s and preferably in the range from about 4,000 to about 1,000,000 mPa.s, more preferably from about 8,000 to about 350,000 mPa.s and especially from about 10,000 to about 250,000 mPa.s and even more especially from about 10,000 to about 150,000 mPa.s (25°C, neat, Brookfield RVT, T Spindle at 5 ⁇ ms and Heliopath Stand).
• the compositions of the invention can also contain from about 0.01% to about 10%, preferably from about 0.1 %> to about 5% of a panthenol moisturizer.
• the panthenol moisturizer can be selected from D-panthenol ([R]-2,4-dihydroxy-N-[3-hydroxypropyl)]- 3,3-dimethylbutamide), DL-panthenol, calcium pantothenate, royal jelly, panthetine, pantotheine, panthenyl ethyl ether, pangamic acid, pyridoxin, pantoyl lactose and Vitamin B complex.
• keratolytic agents/desquamation agents such as salicylic acid
• water-soluble or solubilizable preservatives preferably at a level of from about 0.1 %> to about 5%o, such as Germall 115, methyl, ethyl, propyl and butyl esters of hydroxybenzoic acid, benzyl alcohol, DMDM hydantoin iodopropanyl butylcarbanate available under the trade name Glydant Plus from Lonza, EDTA, Euxyl (RTM) K400, Bromopol (2-bromo-2-nitropropane-l,3-diol) and phenoxypropanol; anti-bacterials such as Irgasan (RTM) and phenoxyethanol (preferably at levels of from 0.1 %> to about 5%); soluble or colloidally-soluble moisturising agents such as hylaronic acid and starch- grafted sodium polyacrylates such as Sanwet
• sunscreening agents are also useful herein.
• a wide variety of sunscreening agents are described in U.S. Patent No. 5,087,445, to Haffey et al., issued February 1 1, 1992; U.S. Patent No. 5,073,372, to Turner et al., issued December 17, 1991; U.S. Patent No. 5,073,371, to Turner et al. issued December 17, 1991; and Segarin, et al., at Chapter VIII, pages 189 et seq., of Cosmetics Science and Technology.
• sunscreens which are useful in the compositions of the invention are those selected from 2-ethylhexyl p-methoxycinnamate, 2-ethylhexyl N,N-dimethyl-p-aminobenzoate, p- aminobenzoic acid, 2-phenylbenzimidazole-5-sulfonic acid, octocrylene, oxybenzone, homomenthyl salicylate, octyl salicylate, 4,4'-methoxy-t-butyldibenzoylmethane, 4- isopropyl dibenzoylmethane, 3-benzyl ⁇ dene camphor, 3-(4-methylbenzyhdene) camphor, titanium dioxide, zinc oxide, silica, iron oxide, Parsol MCX, Eusolex 6300, Octocrylene, Parsol 1789, and mixtures thereof. Still other useful sunscreens are those disclosed in U.S. Patent No 4,937,370, to Sabatelh, issued
• the sunscreens can comp ⁇ se from about 0 5%> to about 20%> of the compositions useful herein. Exact amounts will vary depending upon the sunscreen chosen and the desired Sun Protection Factor (SPF). SPF is a commonly used measure of photoprotection of a sunscreen against erythema. See Federal Register, Vol 43. No. 166, pp. 38206-38269, August 25, 1978.
• compositions of the present invention can additionally comp ⁇ se from about 0.1% to about 5% by weight of aluminium starch octenylsuccinate.
• Aluminium starch octenylsuccinate is the aluminium salt of the reaction product of octenylsuccmic anhydride with starch and is commercially available under the trade name from Dry Flo National Starch & Chemical Ltd. Dry Flo is useful herein from the viewpoint of skin feel and application characteristics.
• compositions of the present invention comprise particulate materials having a refractive index of from about 1.3 to about 1 7, the particulate mate ⁇ als being dispersed m the composition and having a median particle size of from about 2 to about 30 ⁇ m.
• the particulates useful herein have relatively narrow distributions, by which is meant that more than 50%o of the particles fall within 3 ⁇ m either side of the respective median value.
• Suitable particulate mate ⁇ als are organic or organosihcone and preferably organosihcone polymers.
• Preferred particles are free-flowing, solid, materials.
• solid is meant that the particles are not hollow. The void at the centre of hollow particles can have an adverse effect on refractive index and therefore the visual effects of the particles on either skin or the composition.
• Suitable organic particulate materials include those made of polymethylsilsesquioxane, referenced above, polyamide, polythene, polyacrylonitrile, polyacrylic acid, polymethacrylic acid, polystyrene, polytetrafluoroethylene (PTFE) and poly(vinylidene chloride). Copolymers derived from monomers of the aforementioned materials can also be used. Inorganic materials include silica and boron nitride.
• Tospearl® 145 which has a median particle size of about 4.5 ⁇ m and EA-209® from Kobo which is an ethylene / acrylic acid copolymer having a median particle size of about 10 ⁇ m, Nylon- 12 available under the trade name Orgasol 2002 from Elf Atochem, France, or mixtures thereof.
• suitable pigments are titanium dioxide, predispersed titanium dioxide from Kobo e.g. Kobo GWL75CAP, iron oxides, acyglutamate iron oxides, ultramarine blue, D&C dyes, carmine, and mixtures thereof. Depending upon the type of composition, a mixture of pigments will normally be used.
• the preferred pigments for use herein from the viewpoint of moisturisation, skin feel, skin appearance and emulsion compatibility are treated pigments.
• the pigments can be treated with compounds such as amino acids, silicones, lecithin and ester oils.
• compositions of the present invention can also comprise a safe and effective amount of a vitamin B3 compound.
• the compositions of the present invention preferably comprise 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%>, and still more preferably from about 1%) to about 8%>, most preferably from about 1.5% to about 6%>, of the vitamin B3 compound.
• vitamin B3 compound means a compound having the formula:
• 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.
• exemplary derivatives of the foregoing vitamin B3 compounds include nicotinic acid esters, including non-vasodilating esters of nicotinic acid, nicotinyl amino acids, nicotinyl alcohol esters of carboxylic acids, nicotinic acid N-oxide and niacinamide N-oxide.
• Suitable esters of nicotinic acid include nicotinic acid esters of C ⁇ -C22 > preferably C ⁇ - Ci6, more preferably C ⁇ -Cg alcohols.
• the alcohols are suitably straight-chain or branched chain, cyclic or acyclic, saturated or unsaturated (including aromatic), and substituted or unsubstituted.
• the esters are preferably non-vasodilating. As used herein, "non-vasodilating" means that the ester does not commonly yield a visible flushing response after application to the skin in the subject compositions (the majority of the general population would not experience a visible flushing response, although such compounds may cause vasodilation not visible to the naked eye).
• Non-vasodilating esters of nicotinic acid include tocopherol nicotinate and inositol hexanicotinate; tocopherol nicotinate is preferred.
• a more complete description of vitamin B3 compounds is given in WO 98/22085.
• vitamin B3 compounds are well known in the art and are commercially available from a number of sources, e.g., the Sigma Chemical Company (St. Louis, MO); ICN Biomedicals, Inc. (Irvin, CA) and Aldrich Chemical Company (Milwaukee, WI).
• One or more vitamin B3 compounds may be used herein.
• Preferred vitamin B3 compounds are niacinamide and tocopherol nicotinate. Niacinamide is more preferred.
• the compositions of the present invention also contain a retinoid.
• the vitamin B3 compound and retinoid provide unexpected benefits in regulating skin condition, especially in therapeutically regulating signs of skin aging, more especially wrinkles, lines, and pores. Without intending to be bound or otherwise limited by theory, it is believed that the vitamin B3 compound increases the conversion of certain retinoids to trans-retinoic acid, which is believed to be the biologically active form of the retinoid, to provide synergistic regulation of skin condition (namely, increased conversion for retinol, retinol esters, and retinal).
• the vitamin B3 compound unexpectedly mitigates redness, inflammation, dermatitis and the like which may otherwise be associated with topical application of retinoid (often referred to, and hereinafter alternatively referred to as "retinoid dermatitis").
• retinoid dermatitis also referred to, and hereinafter alternatively referred to as "retinoid dermatitis"
• the combined vitamin B3 compound and retinoid tend to increase the amount and activity of thioredoxin, which tends to increase collagen expression levels via the protein AP-1. Therefore, the present invention enables reduced active levels, and therefore reduced potential for retinoid dermatitis, while retaining significant positive skin conditioning benefits.
• higher levels of retinoid may still be used to obtain greater skin conditioning efficacy, without undesirable retinoid dermatitis occurring.
• retinoid includes all natural and/or synthetic analogs of Vitamin A or retinol-like compounds which possess the biological activity of Vitamin A in the skin as well as the geometric isomers and stereoisomers of these compounds.
• the retinoid is preferably retinol, retinol esters (e.g., C2 - C22 alkyl esters of retinol, including retinyl palmitate, retinyl acetate, retinyl proprionate), retinal, and/or retinoic acid (including all- trans retinoic acid and/or 13-cis-retinoic acid), more preferably retinoids other than retinoic acid.
• retinol retinol esters
• retinyl esters e.g., C2 - C22 alkyl esters of retinol, including retinyl palmitate, retinyl acetate, retinyl proprionate
• retinal and
• retinoids are retinol, retinyl palmitate, retinyl acetate, retinyl proprionate, retinal and combinations thereof. More preferred are retinol and retinyl palmitate.
• the retinoid may be included as the substantially pure material, or as an extract obtained by suitable physical and/or chemical isolation from natural (e.g., plant) sources.
• compositions preferably contain from or about 0.005%> to or about 2%, more preferably 0.01% to about 2%> retinoid.
• Retinol is most preferably used in an amount of from or about 0.01%> to or about 0.15%; retinol esters are most preferably used in an amount of from about 0.01% to about 2%> (e.g., about 1%>).
• the pH of the compositions herein is greater than 5, preferably greater than 5.25 and more preferably greater than 5.40, also preferably less than 9, more preferably less than 8 and even more preferably less than 7.
• compositions of the invention are preferably in the form of a moisturising cream or lotion, which can be applied to the skin as a leave-on product.
• the invention is illustrated by the following examples.
• Example I II III IV V VI Ingredient %_ %_ %_ %_ %- %_ %_ w/w w/w w/w w/w w/w w/w w/w w/w w/w w/w w/w
• compositions are made as follows:
• compositions of Examples VII and VIII are prepared according to the procedure described above with the additional final step of blending the enzyme (Protease F) solution at 30°C or below to the batch.
• enzyme Protease F
• compositions display high moisturisation efficacy without the associated high levels of tack, as well as good rheological and abso ⁇ tion properties, in addition to skin feel, skin softness and skin smoothness benefits.

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