EP1227790A1 - Compositions cosmetiques - Google Patents

Compositions cosmetiques

Info

Publication number
EP1227790A1
EP1227790A1 EP00961833A EP00961833A EP1227790A1 EP 1227790 A1 EP1227790 A1 EP 1227790A1 EP 00961833 A EP00961833 A EP 00961833A EP 00961833 A EP00961833 A EP 00961833A EP 1227790 A1 EP1227790 A1 EP 1227790A1
Authority
EP
European Patent Office
Prior art keywords
emulsifier
mixtures
skin
protease
composition according
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP00961833A
Other languages
German (de)
English (en)
Inventor
Robert Francis Date
Lisa Catherine Duffy
Christopher John Bullion
Emma Kate Brown
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Procter and Gamble Co
Original Assignee
Procter and Gamble Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Procter and Gamble Co filed Critical Procter and Gamble Co
Publication of EP1227790A1 publication Critical patent/EP1227790A1/fr
Withdrawn legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/0295Liquid crystals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/345Alcohols containing more than one hydroxy group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • A61K8/602Glycosides, e.g. rutin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/64Proteins; Peptides; Derivatives or degradation products thereof
    • A61K8/66Enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/86Polyethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair

Definitions

  • the present invention relates to cosmetic compositions.
  • cosmetic compositions In particular it relates to stable cosmetic compositions comprising a protease enzyme, or mixtures thereof; and to cosmetic products comprising the compositions.
  • the compositions display good enzyme stability while the cosmetic products have excellent 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.
  • Dry, itchy or flaky skin may also result from the failure to maintain a proper water gradient across the stratum corneum.
  • Most of the water needed to maintain the water gradient which is sometimes considered to be the stratum corneum's plasticizer, comes from inside the body. If the humidity is too low, such as in a cold climate, insufficient water remains in the outer layers of the stratum corneum to properly plasticize the tissue, and the skin begins to scale and becomes itchy.
  • protease enzymes function primarily by providing a desquamatory action to the cosmetic composition. It is believed that the proteases remove damaged (e.g. dry) skin cells on the surface of the skin, thereby reducing the rough feel associated therewith. The protease removes the effect of prior damage to the skin, giving the skin a fresher, more youthful appearance and feel.
  • protease enzymes have the disadvantage of being readily degraded (i.e. they undergo auto lysis) in conventional cosmetic compositions because of the presence of water.
  • Various attempts have been made to stabilise enzymes in cosmetic compositions.
  • a composition in which the enzyme is stabilised to a high degree.
  • Cosmetic products comprising the compositions herein show good absorption, and water retention properties, in addition to 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. See for example WO97/32560, WO97/32561 and WO/94/17830, and brochures from ICI Surfactants: (1) 'Arlatone ' 2121: Natural emulsifier for oil-in-water milks and creams (Ref.
  • a cosmetic composition suitable for topical application to the skin or hair comprising:
  • a cosmetic product comprising (I) a cosmetic composition suitable for topical application to the skin comprising (a) a protease enzyme, or mixtures thereof; (b) from about 2% to about 45% by weight of an emulsifier which is capable of forming liquid crystals in water; and (c) a topical carrier; and (II) a moisturising composition consisting of water and/or comprising other excipients suitable for topical application to the skin having a water activity value > 0.85, preferably > 0.90, more preferably > 0.95 and most preferably > 0.97 and being capable of activating the protease enzyme, or mixtures thereof of component (I), the components (I) and (II) being separately presented for simultaneous or sequential application. Additionally, components (I) and (II) may be mixed prior to application.
  • the emulsifier of component (I) of the cosmetic products herein preferably comprises a mixture of at least one emulsifier having a high HLB and at least one emulsifier having a low HLB with a melting point of at least 45 °C, the ratio of low HLB to high HLB emulsifier being from about 10 : 1 to about 100 : 1.
  • the cosmetic products of this invention display high moisturisation efficacy, as well as good Theological and absorption properties, in addition to skin softness and skin smoothness benefits.
  • the cosmetic products herein make possible the activation of the enzyme during its intended use, the enzyme being activated upon contact with the moisturising composition.
  • a cosmetic method of treatment of the skin or hair comprising applying to the skin or hair a cosmetic product according to the present invention.
  • an emulsifier capable of forming liquid crystals in water for stabilising a protease enzyme, or mixtures thereof, in a skin or hair care composition.
  • a composition comprising a protease enzyme, or mixtures thereof; an emulsifier capable of forming liquid crystals in water; and a topical carrier; for a skin or hair care application.
  • a cosmetic composition suitable for topical application to the skin or hair comprising:
  • the emulsifier in the composition immediately above preferably comprises a mixture of at least one emulsifier having a high HLB and at least one emulsifier having a low HLB with a melting point of at least 45°C, the ratio of low HLB emulsifier to high HLB emulsifier being from about 10 : 1 to about 100 : 1.
  • compositions of the present invention comprise a protease enzyme together with an essential emulsifier component and a topical carrier, as well as various optional ingredients as indicated below. It is to be understood that the moisturising composition of component II of the cosmetic products herein, in addition to containing water, may also contain any of the various optional ingredients described hereinbelow. 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.
  • skin conditioning agent means a material which is capable of providing a cosmetic conditioning benefit to the skin such as moisturization, humectancy (i.e. the ability to retain or hold water or moisture in the skin), emolliency, visual improvement of the skin surface, soothing of the skin, softening of the skin, and improvement in skin feel.
  • 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 water activity a w of a medium containing water is the ratio of the water vapour pressure of the product "P H20 product” to the vapour pressure of pure water “P H2O pure” at the same temperature. It can also be expressed as the ratio of the number of molecules of water “NH 2O " to the total number of molecules
  • compositions can be used for any suitable purpose.
  • the present compositions are suitable for topical application to the skin or hair.
  • the 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.
  • An essential component of the present invention is a protease enzyme.
  • Protease enzymes are classified under the Enzyme Classification number E.C. 3.4
  • proteases in accordance with the Recommendations (1992) of the International Union of Biochemistry and Molecular Biology (IUBMB).
  • Useful 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, X 995 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:
  • Gly at position Glyl66 is replaced with Asn, Ser, Lys, Arg, His, Gin,
  • the Gly at position Gly 169 is replaced with Ser; the Met at position Met222 is replaced with Gin, Phe, Cys, His, Asn, Glu, Ala or Thr; or
  • Met222 is replaced with Cys
  • Protease B is disclosed by Genencor International, Inc. (San Francisco, California) European Patent EP-B-251 ,446 (granted December 28, 1994 and published January 7, 1988) as characterized by the wild- type BPN' amino acid with the mutations in one or more of the following amino acids: Tyr21, Thr22, Ser24, Asp36, Ala 45, Ala48, Ser49, Met50, His67, Ser87, Lys94, Val95, Gly97, SerlOl, Glyl02, Glyl03, Ilel07, Glyl 10, Met 124, Glyl27, Glyl28, Prol29, Leul35, Lysl70, Tyrl71, Prol72, Aspl97, Met 199, Ser 204, Lys213, Tyr214, Gly215, and Ser221; or two or more of the amino acids listed above and Asp32, Ser33, Tyrl04, Alal
  • 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, Glul56, Glyl 66, Glyl 69, Phel89, 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.
  • Example of such 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 incorporated by reference.
  • the enzyme is preferably present at a level of from about 0.0001% to about 5%, more preferably from about 0.0005% to about 1%, and especially from about 0.001% to about 0.1 % by weight of the composition.
  • 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.
  • Suitable means for identifying liquid crystals include x-ray diffraction, NMR spectroscopy and transmission electron microscopy.
  • the emulsifier 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 incorporated 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 16 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; Cg 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 Glu
  • the low HLB emulsifiers useful herein are selected from the group consisting of saturated C 16 to C 0 fatty alcohols; saturated C ⁇ 6 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) 6 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 16 to C 30 fatty alcohols; saturated C 16 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 Ci - C 0 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 Bl from Henkel, La Grange, Illinois, U.S.A.; alkoxylated derivatives of Ci - C 30 fatty acids, such as PEG-20-stearate, available under the trade name Myrj 49 from ICI, PEG-40-stearate, available under the trade name Myrj 52 from ICI, and
  • 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 0 ethers of polyols; alkoxylated ethers of C]-C 0 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.
  • compositions of the present invention comprise a safe and effective amount of a dermatologically acceptable carrier, suitable for topical application to the skin or hair within which the essential materials and optional other materials are incorporated to enable the essential materials and optional components to be delivered to the skin or hair at an appropriate concentration.
  • the carrier can thus act as a diluent, dispersant, solvent, or the like for the protease enzyme(s) and the emulsifier component which ensures that they can be applied to and distributed evenly over the selected target at an appropriate concentration.
  • the carrier can be solid, semi-solid or liquid. Highly preferred carriers are liquid or semi- solid, such as creams, lotions and gels. Preferably the carrier is in the form of a lotion, cream or a gel, more preferably one which has a sufficient thickness or yield point to prevent the particles from sedimenting.
  • the carrier can itself be inert or it can possess dermatological benefits of its own.
  • the carrier should also be physically and chemically compatible with the essential components described herein, and should not unduly impair stability, efficacy or other use benefits associated with the compositions of the present invention.
  • the type of carrier ultilised in the present invention depends on the type of product form desired for the composition.
  • the topical compositions useful in the subject invention may be made into a wide variety of product forms such as are known in the art. These include, but are not limited to, lotions, creams, gels, sticks, ointments, and pastes. These product forms may comprise several types of carriers including, but not limited to, solutions, emulsions, and gels.
  • Preferred carriers contain a dermatologically acceptable, hydrophilic diluent.
  • Suitable hydrophilic diluents include water, organic hydrophilic diluents such as Ci - C 4 monohydric alcohols and low molecular weight glycols and polyols, including propylene glycol, polyethylene glycol (e.g. of MW 200-600), polypropylene glycol (e.g.
  • the diluent is preferably liquid. Water is an especially preferred diluent.
  • the composition preferably comprises at least about 20% of the hydrophilic diluent.
  • Preferred carriers comprise an emulsion comprising a hydrophilic phase, especially an aqueous phase, and a hydrophobic phase e.g., a lipid, oil or oily material.
  • a hydrophilic phase will be dispersed in the hydrophobic phase, or vice versa, to form respectively hydrophilic or hydrophobic dispersed and continuous phases, depending on the composition ingredients.
  • the term "dispersed phase” is a term well-known to one skilled in the art which means that the phase exists as small particles or droplets that are suspended in and surrounded by a continuous phase.
  • the dispersed phase is also known as the internal or discontinuous phase.
  • the emulsion may be or comprise (e.g., in a triple or other multi-phase emulsion) an oil-in-water emulsion or a water-in-oil emulsion such as a water-in-silicone emulsion.
  • Oil-in-water emulsions typically comprise from about 1% to about 60% (preferably about 1% to about 30%) of the dispersed hydrophobic phase and from about 1% to about 99% (preferably from about 40% to about 90%) of the continuous hydrophilic phase; water-in- oil emulsions typically comprise from about 1% to about 98% (preferably from about 40% to about 90%) of the dispersed hydrophilic phase and from about 1% to about 50% (preferably about 1% to about 30%) of the continuous hydrophobic phase.
  • Preferred compositions herein are oil-in-water emulsions.
  • compositions herein are incorporated in a cosmetic product comprising:
  • a cosmetic composition suitable for topical application to the skin or hair comprising (a) a protease enzyme, or mixtures thereof; (b) from about 2% to about 45% by weight of an emulsifier which is capable of forming liquid crystals in water; and (c) a topical carrier; and
  • (XT) a moisturising composition consisting of water and or comprising other excipients suitable for topical application to the skin or hair having a water activity value > 0.85, preferably > 0.90, more preferably > 0.95 and most preferably > 0.97, and being capable of activating the protease enzyme, or mixtures thereof of component (I), the components (I) and (XT) being separately presented for simultaneous or sequential application.
  • the cosmetic products herein may be presented, for example, in a dual compartment container, two separate containers, or a kit comprising two containers, wherein instructions for use are also included.
  • compositions herein preferably additionally comprise at least one polyhydric alcohol in a concentration of from about 20% to about 80%, more preferably from about 20% to about 70%, 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.
  • compositions of the present invention include a polyhydric alcohol
  • concentration of the combined polyhydric alcohol and emulsifier is in the range of from about 20% to about 99%, preferably about 20% to about 95% and especially about 25% to about 90% by weight of the composition.
  • compositions of the present invention additionally comprise a salt selected from alkali metal and alkaline earth metal salts, and mixtures thereof, preferably sodium, calcium and magnesium salts, and mixtures thereof.
  • compositions herein preferably comprise from about 50 ppm to about 400 ppm of the salt, based on the amount of metal ion.
  • compositions herein may comprise additional enzymes selected from lipases, phospholipases, glycosidases, lactoperoxidases and cellulases, and mixtures thereof.
  • 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% to about 60%, preferably from about 1% to about 30%, and more preferably from about 1% to about 10%.
  • the oil phase components of the compositions herein comprise an emollient material or mixtures thereof, a polyol carboxylic acid ester 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. 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. Emollient materials
  • 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* is selected from H or CH3, R ⁇ , R3 and R 4 are independently selected from Ci -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 Ci -C4 alkyl substituted benzyl and R5 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, N.J. 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 (H) include but are not limited to C 12- 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, sucrose pentaoleate, sucrose hexaoleate, sucrose heptaoleate, sucrose octaoleate, sorbitol hexaester in which the carboxylic acid ester moieties are palmitoleate and arachidate in a 1 :2 molar ratio, and the octaester of sucrose wherein the esterifying carboxylic acid moieties are laurate, linoleate and behenate in a 1 :3:4 molar ratio.
  • Other materials include cottonseed oil
  • compositions preferably 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, polyalkoxylated 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 ⁇ .s'l, preferably from about 0.65 to about 10,000 mm ⁇ .s'l at 25°C. The viscosity can be measured by means of a glass capillary viscometer as set forth in Dow Corning Corporate 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.
  • essentially non-volatile polyalkylarylsiloxanes for example, polymethylphenylsiloxanes, having viscosities of about 0.65 to 30,000 mm ⁇ .s"! at 25°C.
  • 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 incorporating 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 nonvolatile polyalkyl and polyaryl siloxane gums.
  • a silicone oil phase comprises a silicone gum or a mixture of silicones including the silicone gum. Typically, silicone gums have a viscosity at
  • 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. Specific examples of 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 incorporated into the composition as part of a silicone gum-fluid blend.
  • the silicone gum When the silicone gum is incorporated 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'l to about 100 mm ⁇ .s"!,
  • 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-!.
  • 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
  • silicone component 0.65 to 100 mm ⁇ .s'l.
  • An example of this silicone component is Dow Corning Q2-1403 (85% 5 mm 2 ⁇ "1 Dimethicone Fluid/15% Dimethiconol) and Dow Corning Q2-1401 available from Dow Corning.
  • silicone components suitable for use in a silicone oil phase herein are crosshnked polyorganosiloxane polymers, optionally dispersed in a fluid carrier.
  • the crosshnked 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 crosshnked 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.
  • crosshnked 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 crosshnked polyorganosiloxane polymer and silicone fluid. Particularly preferred for use herein especially in combination with the organic amphiphilic emulsifier material is KSG-18.
  • 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, Postfach D-8000 Kunststoff 22 and Abil (RTM) from Th.
  • 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.
  • 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, crosshnked poly(N-vinylpyrrolidones), polysaccharides, natural or synthetic gums, polyvinylpyrrolidone, and polyvinylalcohol.
  • Suitable anionic thickening agents include acrylic acid/ethyl acrylate copolymers, carboxyvinyl polymers and crosshnked 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 Corporation, 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.
  • Humectants include acrylic acid/ethyl acrylate copolymers, carboxyvinyl polymers and crosshnked copolymers of alkyl vinyl ethers and maleic anhydride.
  • 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%o 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 monoethanolamine; acetamide monoethanolamine; 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 any of
  • At least part (up to about 5% by weight of composition) of an additional humectant can be incorporated 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, incorporated herein by reference.
  • Preferred additional humectants are selected from urea, panthenol and mixtures thereof.
  • compositions herein A wide variety of optional ingredients such as neutralising agents, perfumes, and colouring agents, can also be added to the 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 rpms and Heliopath Stand).
  • 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%, 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 (RTM) IM-
  • 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 11, 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 VIE, 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-benzylidene camphor, 3-(4-methylbenzylidene) 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 Sabat
  • the sunscreens can comprise 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 comprise 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 octenylsuccinic 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 materials being dispersed in 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% of the particles fall within 3 ⁇ m either side of the respective median value.
  • Suitable particulate materials are organic or organosihcone and preferably organosihcone polymers. Prefe ⁇ ed particles are free-flowing, solid, materials. By “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
  • 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 prefe ⁇ ed 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.
  • Vitamin B component
  • 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 Cj-C22 > preferably C ⁇ -
  • Ci -Cg 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 prefe ⁇ ed.
  • 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
  • vitamin B3 compounds may be used herein. Prefe ⁇ ed 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 refe ⁇ ed to, and hereinafter alternatively refe ⁇ ed to as "retinoid dermatitis").
  • retinoid dermatitis often refe ⁇ ed to, and hereinafter alternatively refe ⁇ ed 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 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)
  • retinoic acid including all-trans retinoic acid and/or 13-cis-retinoic acid
  • Preferred retinoids are retinol, retinyl palmitate, retinyl acetate, retinyl proprionate, retinal and combinations thereof. More prefe ⁇ ed 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.
  • the cosmetic compositions herein preferably have a water activity ⁇ 0.85, more preferably ⁇ 0.75, and most preferably ⁇ 0.70.
  • compositions of the invention are preferably in the form of a moisturising cream or lotion, which can be applied to the skin or hair.
  • the invention is illustrated by the following examples.
  • Protease F 0.010 0.015 0.05 0.00 0.030 0.025 0.020
  • the gel comprises 74-83% (w/w) cyclomethicone (D5), 12 - 16% (w/w) polysilicone 11 and 12
  • compositions are made as follows:
  • compositions display high enzyme stability, as well as good rheological and absorption properties, in addition to skin feel, skin softness and skin smoothness benefits.

Abstract

Composition cosmétique à usage local sur la peau ou les cheveux, comprenant : (a) une protéase ou des mélanges de celle-ci ; et (b) environ 2 % à environ 45 % en poids d'un émulsifiant capable de former des cristaux liquides dans l'eau et comprenant un mélange d'au moins un émulsifiant présentant un HLB élevé et d'au moins un émulsifiant présentant un HLB faible, avec un point de fusion d'au moins 45 °C, le rapport entre l'émulsifiant à faible HLB et l'émulsifiant à HLB élevé étant d'environ 10 :1 à environ 100 :1. Les compositions de l'invention présentent une stabilité enzymatique élevée et les produits les contenant ont une efficacité hydratante élevée et présentent des bonnes propriétés rhéologiques et d'absorption, outre qu'ils rendent la peau agréable au toucher, douce et lisse.
EP00961833A 1999-11-08 2000-09-13 Compositions cosmetiques Withdrawn EP1227790A1 (fr)

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US8936796B2 (en) 2008-02-25 2015-01-20 The Procter & Gamble Company Hair care compositions comprising sucrose polyesters
US8936798B2 (en) 2008-02-25 2015-01-20 The Procter & Gamble Company Hair care compositions comprising sucrose polyesters

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CN1420760A (zh) 2003-05-28
MXPA02004613A (es) 2002-09-02
JP2003520205A (ja) 2003-07-02
WO2001034111A1 (fr) 2001-05-17
IE990935A1 (en) 2002-04-03
AU7373000A (en) 2001-06-06

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