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WO2009003996A1 - Composition cosmetique amelioree d'eclaircissement de la peau - Google Patents

Composition cosmetique amelioree d'eclaircissement de la peau Download PDF

Info

Publication number
WO2009003996A1
WO2009003996A1 PCT/EP2008/058427 EP2008058427W WO2009003996A1 WO 2009003996 A1 WO2009003996 A1 WO 2009003996A1 EP 2008058427 W EP2008058427 W EP 2008058427W WO 2009003996 A1 WO2009003996 A1 WO 2009003996A1
Authority
WO
WIPO (PCT)
Prior art keywords
skin lightening
skin
composition
titanium dioxide
particle size
Prior art date
Application number
PCT/EP2008/058427
Other languages
English (en)
Inventor
Jayashree Anand
Lalitagauri Rajwade
Vibhav Ramrao Sanzgiri
Simone Dosu Sethna
Original Assignee
Unilever Plc
Unilever N.V.
Hindustan Unilever Limited
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 Unilever Plc, Unilever N.V., Hindustan Unilever Limited filed Critical Unilever Plc
Priority to CN200880023468A priority Critical patent/CN101686913A/zh
Priority to EP08761408A priority patent/EP2167022A1/fr
Priority to MX2010000271A priority patent/MX2010000271A/es
Publication of WO2009003996A1 publication Critical patent/WO2009003996A1/fr

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/29—Titanium; Compounds 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
    • A61K8/67—Vitamins
    • 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
    • A61K8/67—Vitamins
    • A61K8/671—Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
    • 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
    • A61K8/67—Vitamins
    • A61K8/673—Vitamin B 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
    • A61K8/67—Vitamins
    • A61K8/673—Vitamin B group
    • A61K8/675—Vitamin B3 or vitamin B3 active, e.g. nicotinamide, nicotinic acid, nicotinyl aldehyde
    • 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
    • A61K8/67—Vitamins
    • A61K8/676—Ascorbic acid, i.e. vitamin C
    • 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
    • A61K8/67—Vitamins
    • A61K8/678—Tocopherol, i.e. vitamin E
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/04—Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/41—Particular ingredients further characterized by their size
    • A61K2800/412—Microsized, i.e. having sizes between 0.1 and 100 microns

Definitions

  • the present invention relates to cosmetic skin lightening composition and in particular to a skin lightening composition that delivers immediate improvements in skin appearance by providing enhanced instant brightness/glow along with the effects of lightening the skin.
  • a tan is essentially the skins' way of increasing its defence against the onslaught of damaging ultra-violet. Tanning protects against sun damage principally by increasing the melanin content of the epidermis. Although more skin pigmentation improves sun protection, intentional UV induced tanning does not necessarily achieve an increase in protective pigmentation as an ultra-violet protective strategy.
  • Melanin which is basically responsible for skin pigmentation is synthesised by melanocytes, a cell type present at dermis-epidermis junction, from an amino acid tyrosine. Tyrosine is acted upon by an enzyme tyrosinase which is the key enzyme in melanogenesis.
  • the conventional skin lightening compositions are based on sunscreens which maintain skin colour against the ultra-violet light. They have been based on materials which absorb/block incident ultra-violet light of the wavelength which produces the tanning of the skin. Other approaches have been to use niacin/niacinamide or other skin lightening agents which are believed to control dispersion of melanosomes or inhibit tyrosinase. Sunscreens alone cannot lighten the skin significantly and their action on the skin is only to reduce the ingress of incident ultra-violet into the skin and is therefore effective only during the day.
  • GB 1 533 1 19 discloses a combination of niacinamide and a suitable mixture of UV absorbers which absorb in the UV range of 290 nm to 360 nm.
  • IN 169917 discloses the use of a silicone compound to synergistically enhance skin lightening benefits obtained from the combination of niacinamide and sunscreens.
  • Certain inorganic substances have also been proposed for use as sunscreens which physically block exposure of the skin to ultra-violet rays.
  • titanium dioxide having a very small particle size. This grade of titanium dioxide, designated as ultrafine TiO 2 , affords a good degree of sun blocking potential without causing any biological skin lightening effect.
  • IN 172889 discloses the use of titanium dioxide at levels from 3% along with octyl methoxy cinnamate to provide protection from excessive exposure to ultra-violet rays over a broad range of wavelengths in the UV-A and UV-B regions.
  • US 5 997 887 and US 5 997 890 disclose topical compositions comprising pigmentary grade particulate material such as titanium dioxide, with a particle size greater than 100nm to about 300nm along with an active vitamin B 3 useful for imparting an essentially immediate visual improvement in skin appearance.
  • pigmentary grade particulate material such as titanium dioxide
  • an object of the present invention is to provide a cosmetic skin lightening composition that delivers immediate improvements in skin appearance by providing enhanced instant glow along with enhanced effects of lightening the skin.
  • compositions including titanium dioxide with a primary particle size in the range greater than 300 nm and up to 1000 nm that synergistically enhances skin lightening efficacy of skin lightening agents while delivering immediate improvements in skin appearance by providing an enhanced instant glow.
  • the effects obtained on skin lightening is particularly surprising as titanium dioxide with a primary particle size range of greater than 300 nm and up to 1000 nm is not a sunscreen, does not penetrate the skin and is not a known skin lightening agent.
  • the present invention relates to a cosmetic skin lightening composition including 0.1% to 10% by weight of one or more of skin lightening agent or a precursor thereof and 0.1 to 5% titanium dioxide with a primary particle size greater than 300 up to 1000 nm in a cosmetically acceptable vehicle.
  • the particle size mentioned for the purposes of the present invention is as measured by the Mac-View particle size distribution (electron microscopy) method (Mountech Co. Ltd.)
  • the present invention relates to a cosmetic skin lightening composition
  • a cosmetic skin lightening composition comprising 0.1 % to 10% by weight of skin lightening agents selected from vitamins B 3 , B 6 , B 12 , C, E, A, D, K, or mixtures thereof, and 0.1 to 5% titanium dioxide with a primary particle size greater than 300 up to 1000 nm in a cosmetically acceptable vehicle.
  • skin lightening agents selected from vitamins B 3 , B 6 , B 12 , C, E, A, D, K, or mixtures thereof, and 0.1 to 5% titanium dioxide with a primary particle size greater than 300 up to 1000 nm in a cosmetically acceptable vehicle.
  • vitamins B 3 , B 6 , B 12 , C, E, A, D, K, or mixtures thereof selected from vitamins B 3 , B 6 , B 12 , C, E, A, D, K, or mixtures thereof
  • titanium dioxide with 0.1 to 5% titanium dioxide with a primary particle size greater than 300 up to 1000 nm
  • a cosmetic skin lightening composition as set forth hereinabove comprising 0.1 to 10 % by weight of at least one organic sunscreen.
  • the invention composition additionally comprises 0.05% to 5% by weight ultra fine titanium dioxide with a particle size in the range 1 -100 nm.
  • composition of the invention is reversible and without any side effects.
  • composition according to the invention is active both during - A -
  • sunscreens which can act only during the day and on both the photoexposed and non-photoexposed part of the skin.
  • the skin lightening agent according to the invention is vitamin B 3 or a derivative thereof and is selected from the group consisting of niacinamide, nicotinic acid esters, non-vasodilating esters of nicotinic acid, nicotinyl amino acids, nicotinyl alcohol esters of carboxylic acids, nicotinic acid N-oxide, niacinamide N-oxide and mixtures thereof.
  • compositions can be advantageously included in the composition to provide for synergistic skin lightening effects.
  • Still other skin lightening agents useful to be incorporated in the composition are polyamino acid sequences with pi in the range 2 to 5.5, and the amino acid forming the polyamino acid sequence can be naturally occurring or synthetic, dextro or levo form, straight chain or cyclised with a molecular weight of 200-20000, hydroquinone and derivatives (eg.
  • the skin lightening agent is employed at a concentration in the range from 0.1 % to 10%, preferably from 0.1 to 5%, more preferably from 0.2 to 1.5%, optimally from 0.3 to 1% by weight of the composition.
  • the organic sunscreens used in the composition according to the invention may be selected from 4-tertiary butyl-4'-methoxy dibenzoylmethane, octyl methoxy cinnamate, benzophenone-3, benzophenone-4, benzophenone-8, diethanolamine methoxy cinnamate, ethyl dihydroxypropyl para amino benzoic acid, glyceryl PABA, homosalate, methyl anthranilate, salicylate, ethylhexyl 2-phenyl-benzimidazole-5-sulphonic acid and others known in the art or any other suitable mixtures thereof.
  • the preferred organic sunscreens used in the composition according to the invention may be selected from 4-tertiary butyl-4'-methoxy dibenzoylmethane, octyl methoxy cinnamate or suitable mixtures thereof.
  • the organic sunscreens at a concentration in the range from 0.1 to 10 %, preferably from 0.5 to 8%, more preferably from 1 to 5% by weight of the composition.
  • Titanium dioxide
  • the titanium dioxide may be selected from surface untreated, surface treated, hydrophilically or hydrophobically, powder form or predispersed or a mixture thereof.
  • the preferred primary particle size of titanium dioxide used according to the invention is greater than 300 up to 1000 nm. It is preferred that the primary particle size is in the range 310-750 nm.
  • the particle size mentioned for the purposes of the present invention is as measured by the Mac-View particle size distribution (electron microscopy) method.
  • the composition additionally comprises 0.1 to 5% (preferably 0.2 to 0.8%) by weight of the composition of ultra fine or micronised titanium dioxide with a particle size in the range 1-100nm, preferably 1-50nm and more preferably 5-25nm.
  • the micronised titanium dioxide is especially preferred. This has been found to give additional skin lightening benefits.
  • the vehicle which forms part of the cosmetic composition is one or more substances which are cosmetically acceptable in that they will not harm the skin.
  • Cosmetic compositions to deliver different benefit agents are prepared using different emulsifying systems and vehicles.
  • the vehicles that can be used in the compositions according to the invention can include powder absorbents, binders and carriers, and liquids such as emollients, emulsifiers, propellants, solvents, humectants (e.g polyols, glycerol), thickeners (e.g. Carbopol 934), cetyl alcohol, esters, ethoxylated castor oil, paraffin oils, lanolin and its derivatives, fragrances, colourants and mixtures thereof.
  • the compositions according to the invention for topical application to the skin can be in the form of conventional products such as lotions, powders, creams, ointments, sticks, aerosol and cleansing products.
  • the vehicle is a vanishing cream base which comprises 5-25%, preferably 8-22%, more preferably 10-20%, and optimally 12-20% by weight Ci 2 -C 20 fatty acids and 0.1-10%, preferably 1-5% and optimally 1.5-4% by weight Ci 2 -C 20 fatty acid soap.
  • Vanishing cream base is one of the preferred forms of such a cosmetically acceptable vehicle and gives a desirable matt feel to the skin.
  • the cosmetic skin lightening composition in the form of a cream is prepared using the conventional process used for making oil-in-water emulsions.
  • the titanium dioxide with a particle size greater than 300 up to 1000 nm according to the invention is preferably added during the emulsion process and more preferably is added mid way through the emulsion process.
  • a human volunteer study was conducted by testing various compositions on 50 volunteers of Type IV to V skin (Fitzpatrick scale) who were screened and selected to have a similar kind of skin pigmentation.
  • the compositions had niacinamide purchased from Veer Chemie Ltd., India as the skin lightening agent
  • the inorganic sunscreen used was titanium dioxide with an average particle size of 15 nm sold by Tayca Corporation under the trade name MT100Z.
  • the titanium dioxide with an average particle size of 400 nm sold by Tayca Corporation under the trade name MP40 was used in the experiments to test the efficacy of the formulations in accordance with the invention.
  • compositions according to the invention and the respective controls were prepared in a vanishing cream base and the composition details are presented in table 1.
  • the process used to manufacture the cream was a standard process used for oil-in-water emulsions where the water phase containing the polyol and preservatives was heated and alkali was added to it.
  • the molten oil phase containing the fatty acid, fatty alcohol, etc. was then charged into the water phase in 2 parts - the first led to the formation of the soap and the second part formed the actual emulsion.
  • the batch was repeatedly passed through a homogenizer until a smooth emulsion was formed. Titanium dioxide with an average particle size of 15 nm and the titanium dioxide with an average particle size of 400 nm were added during the emulsion process. Once the emulsion was formed, it was slowly cooled and niacinamide was added at around 40-50 0 C followed by other heat-labile ingredients including other actives. All the ingredients were gently mixed under vacuum and the batch was de-aerated prior to perfume addition.
  • the sample cream was applied at a concentration of 2 mg/cm 2 to areas marked on the volar forearm of the individual volunteers and corresponding untreated areas were maintained for comparison.
  • the volar forearm is chosen to minimise the effect of the sun and study the effect of the biological skin lightening.
  • Cream was applied twice per day.
  • the marked out areas were assessed over a period of 4 weeks without the presence of the cream to assess the biological skin lightening and the data presented is at the end of the period.
  • the assessment was done by an expert panel on a colour scale considering the difference between the treated and untreated area of the forearms, and is presented as the extent of skin lightening in the table 1 that follows.
  • the skin lightening scores presented in table 1 show that increasing the concentration of 15 nm titanium dioxide alone does not significantly improve the skin lightening scores and even a combination of enhanced levels of niacinamide, the skin lightening agent, and the 15nm titanium dioxide gives a marginal improvement in skin lightening benefit.
  • sample cream according to example 1 that did not contain any titanium dioxide with a particle size of 400 nm and example 3 that contained 0.3% titanium dioxide with a particle size of 400 nm as described in table 1 was applied at a concentration of 2 mg/cm 2 to areas marked on the volar forearm of the individual volunteers. Volunteers and the expert panel members were asked to score the brightness of the skin and glow on the skin immediately after application of the cream and also after the composition had completely dried on the skin. Percentage members who stated that composition of example 3, "makes my skin bright" was 93% and "makes my skin glow” was 91%.
  • compositions using 1.25% niacinamide along with MP40 titanium dioxide with a particle size in the range 400 nm and another set with 3.5% niacinamide and 100 - 300 nm particle size titanium dioxide were assessed in a human volunteer study as described above and the data are presented in table 4.
  • aAvailable from the Proctor and Gamble Company Contains 3.5% w/w niacinamide and 1.4% w/w TiO 2 of particle size 100-300nm.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Cosmetics (AREA)

Abstract

L'invention concerne une composition cosmétique d'éclaircissement de la peau, contenant : de 0,1 à 10% en poids d'un agent d'éclaircissement de la peau; de 0,1 à 5% en poids de dioxyde de titane présentant une taille de particules primaires supérieure à 300 nm et inférieure ou égale à 1000 nm; ainsi qu'un excipient cosmétiquement acceptable.
PCT/EP2008/058427 2007-07-05 2008-07-01 Composition cosmetique amelioree d'eclaircissement de la peau WO2009003996A1 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
CN200880023468A CN101686913A (zh) 2007-07-05 2008-07-01 改进的用于皮肤变淡的美容组合物
EP08761408A EP2167022A1 (fr) 2007-07-05 2008-07-01 Composition cosmetique amelioree d'eclaircissement de la peau
MX2010000271A MX2010000271A (es) 2007-07-05 2008-07-01 Composicion cosmetica mejorada para aclarar la piel.

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1286/MUM/2007 2007-07-05
IN1286MU2007 2007-07-05

Publications (1)

Publication Number Publication Date
WO2009003996A1 true WO2009003996A1 (fr) 2009-01-08

Family

ID=39877936

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2008/058427 WO2009003996A1 (fr) 2007-07-05 2008-07-01 Composition cosmetique amelioree d'eclaircissement de la peau

Country Status (4)

Country Link
EP (1) EP2167022A1 (fr)
CN (1) CN101686913A (fr)
MX (1) MX2010000271A (fr)
WO (1) WO2009003996A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011089571A2 (fr) 2010-01-21 2011-07-28 L'oreal Composition cosmétique comprenant au moins un composé fluorophore
US20200085702A1 (en) * 2016-12-22 2020-03-19 L'oreal Oil-in-water emulsion comprising a specific surfactant system
JP2021519342A (ja) * 2018-03-21 2021-08-10 ベネター ジャーマニー ゲ−エムベーハー 二酸化チタン

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5997887A (en) * 1997-11-10 1999-12-07 The Procter & Gamble Company Skin care compositions and method of improving skin appearance
WO2001070190A2 (fr) * 2000-03-23 2001-09-27 Unilever Plc Compositions cosmetiques
US20050013784A1 (en) * 2001-02-08 2005-01-20 The Procter & Gamble Company Mask composition
US20050019356A1 (en) * 2003-07-25 2005-01-27 The Procter & Gamble Company Regulation of mammalian keratinous tissue using N-acyl amino acid compositions
JP2006257021A (ja) * 2005-03-17 2006-09-28 Shiseido Co Ltd 皮膚化粧料

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5997887A (en) * 1997-11-10 1999-12-07 The Procter & Gamble Company Skin care compositions and method of improving skin appearance
WO2001070190A2 (fr) * 2000-03-23 2001-09-27 Unilever Plc Compositions cosmetiques
US20050013784A1 (en) * 2001-02-08 2005-01-20 The Procter & Gamble Company Mask composition
US20050019356A1 (en) * 2003-07-25 2005-01-27 The Procter & Gamble Company Regulation of mammalian keratinous tissue using N-acyl amino acid compositions
JP2006257021A (ja) * 2005-03-17 2006-09-28 Shiseido Co Ltd 皮膚化粧料

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DATABASE WPI Week 200670, Derwent World Patents Index; AN 2006-673867, XP002502711 *
POPOV ALEXEY P ET AL: "Effect of size of TiO2 nanoparticles embedded into stratum corneum on ultraviolet-A and ultraviolet-B sun-blocking properties of the skin", JOURNAL OF BIOMEDICAL OPTICS, SPIE, BELLINGHAM, WA, US, vol. 10, no. 6, 8 December 2005 (2005-12-08), pages 64037/1 - 64037/9, XP002435985, ISSN: 1083-3668 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011089571A2 (fr) 2010-01-21 2011-07-28 L'oreal Composition cosmétique comprenant au moins un composé fluorophore
US20200085702A1 (en) * 2016-12-22 2020-03-19 L'oreal Oil-in-water emulsion comprising a specific surfactant system
US11607374B2 (en) * 2016-12-22 2023-03-21 L'oreal Oil-in-water emulsion comprising a specific surfactant system
JP2021519342A (ja) * 2018-03-21 2021-08-10 ベネター ジャーマニー ゲ−エムベーハー 二酸化チタン

Also Published As

Publication number Publication date
CN101686913A (zh) 2010-03-31
EP2167022A1 (fr) 2010-03-31
MX2010000271A (es) 2010-04-27

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