US20060188559A1 - Topical cosmetic compositions comprising alpha arbutin - Google Patents
Topical cosmetic compositions comprising alpha arbutin Download PDFInfo
- Publication number
- US20060188559A1 US20060188559A1 US11/060,348 US6034805A US2006188559A1 US 20060188559 A1 US20060188559 A1 US 20060188559A1 US 6034805 A US6034805 A US 6034805A US 2006188559 A1 US2006188559 A1 US 2006188559A1
- Authority
- US
- United States
- Prior art keywords
- alpha arbutin
- arbutin
- alpha
- composition
- liposome
- 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.)
- Abandoned
Links
- BJRNKVDFDLYUGJ-ZIQFBCGOSA-N alpha-Arbutin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC1=CC=C(O)C=C1 BJRNKVDFDLYUGJ-ZIQFBCGOSA-N 0.000 title claims abstract description 19
- 229940033280 alpha-arbutin Drugs 0.000 title claims abstract description 19
- 239000000203 mixture Substances 0.000 title claims description 14
- 230000000699 topical effect Effects 0.000 title abstract description 4
- 239000002537 cosmetic Substances 0.000 title description 4
- 239000002502 liposome Substances 0.000 claims abstract description 15
- 235000012871 Arctostaphylos uva ursi Nutrition 0.000 claims abstract description 12
- 244000003892 Vaccinium erythrocarpum Species 0.000 claims abstract description 11
- 210000002966 serum Anatomy 0.000 claims abstract description 4
- 235000019155 vitamin A Nutrition 0.000 claims description 3
- 239000011719 vitamin A Substances 0.000 claims description 3
- SNPLKNRPJHDVJA-ZETCQYMHSA-N D-panthenol Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCCO SNPLKNRPJHDVJA-ZETCQYMHSA-N 0.000 claims description 2
- 235000015097 nutrients Nutrition 0.000 claims description 2
- 229940101267 panthenol Drugs 0.000 claims description 2
- 235000020957 pantothenol Nutrition 0.000 claims description 2
- 239000011619 pantothenol Substances 0.000 claims description 2
- 206010040829 Skin discolouration Diseases 0.000 abstract description 6
- 102000003425 Tyrosinase Human genes 0.000 abstract description 5
- 108060008724 Tyrosinase Proteins 0.000 abstract description 5
- IIGMITQLXAGZTL-UHFFFAOYSA-N octyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCCCCCCC IIGMITQLXAGZTL-UHFFFAOYSA-N 0.000 abstract description 3
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000035515 penetration Effects 0.000 abstract 1
- QIGBRXMKCJKVMJ-UHFFFAOYSA-N Hydroquinone Chemical compound OC1=CC=C(O)C=C1 QIGBRXMKCJKVMJ-UHFFFAOYSA-N 0.000 description 16
- XUMBMVFBXHLACL-UHFFFAOYSA-N Melanin Chemical compound O=C1C(=O)C(C2=CNC3=C(C(C(=O)C4=C32)=O)C)=C2C4=CNC2=C1C XUMBMVFBXHLACL-UHFFFAOYSA-N 0.000 description 14
- 210000003491 skin Anatomy 0.000 description 7
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 3
- AHMIDUVKSGCHAU-UHFFFAOYSA-N Dopaquinone Natural products OC(=O)C(N)CC1=CC(=O)C(=O)C=C1 AHMIDUVKSGCHAU-UHFFFAOYSA-N 0.000 description 3
- AHMIDUVKSGCHAU-LURJTMIESA-N L-dopaquinone Chemical compound [O-]C(=O)[C@@H]([NH3+])CC1=CC(=O)C(=O)C=C1 AHMIDUVKSGCHAU-LURJTMIESA-N 0.000 description 3
- 235000010445 lecithin Nutrition 0.000 description 3
- 229940067606 lecithin Drugs 0.000 description 3
- 239000000787 lecithin Substances 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- 206010064127 Solar lentigo Diseases 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 238000001816 cooling Methods 0.000 description 2
- VJNCICVKUHKIIV-UHFFFAOYSA-N dopachrome Chemical compound O=C1C(=O)C=C2NC(C(=O)O)CC2=C1 VJNCICVKUHKIIV-UHFFFAOYSA-N 0.000 description 2
- BJRNKVDFDLYUGJ-RMPHRYRLSA-N hydroquinone O-beta-D-glucopyranoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=CC=C(O)C=C1 BJRNKVDFDLYUGJ-RMPHRYRLSA-N 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 210000002752 melanocyte Anatomy 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 2
- 230000029058 respiratory gaseous exchange Effects 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 231100000419 toxicity Toxicity 0.000 description 2
- 230000001988 toxicity Effects 0.000 description 2
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 2
- 230000002087 whitening effect Effects 0.000 description 2
- PCTMTFRHKVHKIS-BMFZQQSSSA-N (1s,3r,4e,6e,8e,10e,12e,14e,16e,18s,19r,20r,21s,25r,27r,30r,31r,33s,35r,37s,38r)-3-[(2r,3s,4s,5s,6r)-4-amino-3,5-dihydroxy-6-methyloxan-2-yl]oxy-19,25,27,30,31,33,35,37-octahydroxy-18,20,21-trimethyl-23-oxo-22,39-dioxabicyclo[33.3.1]nonatriaconta-4,6,8,10 Chemical compound C1C=C2C[C@@H](OS(O)(=O)=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2.O[C@H]1[C@@H](N)[C@H](O)[C@@H](C)O[C@H]1O[C@H]1/C=C/C=C/C=C/C=C/C=C/C=C/C=C/[C@H](C)[C@@H](O)[C@@H](C)[C@H](C)OC(=O)C[C@H](O)C[C@H](O)CC[C@@H](O)[C@H](O)C[C@H](O)C[C@](O)(C[C@H](O)[C@H]2C(O)=O)O[C@H]2C1 PCTMTFRHKVHKIS-BMFZQQSSSA-N 0.000 description 1
- FLPJVCMIKUWSDR-UHFFFAOYSA-N 2-(4-formylphenoxy)acetamide Chemical compound NC(=O)COC1=CC=C(C=O)C=C1 FLPJVCMIKUWSDR-UHFFFAOYSA-N 0.000 description 1
- OSCJHTSDLYVCQC-UHFFFAOYSA-N 2-ethylhexyl 4-[[4-[4-(tert-butylcarbamoyl)anilino]-6-[4-(2-ethylhexoxycarbonyl)anilino]-1,3,5-triazin-2-yl]amino]benzoate Chemical compound C1=CC(C(=O)OCC(CC)CCCC)=CC=C1NC1=NC(NC=2C=CC(=CC=2)C(=O)NC(C)(C)C)=NC(NC=2C=CC(=CC=2)C(=O)OCC(CC)CCCC)=N1 OSCJHTSDLYVCQC-UHFFFAOYSA-N 0.000 description 1
- ICIDSZQHPUZUHC-UHFFFAOYSA-N 2-octadecoxyethanol Chemical compound CCCCCCCCCCCCCCCCCCOCCO ICIDSZQHPUZUHC-UHFFFAOYSA-N 0.000 description 1
- LXAHHHIGZXPRKQ-UHFFFAOYSA-N 5-fluoro-2-methylpyridine Chemical compound CC1=CC=C(F)C=N1 LXAHHHIGZXPRKQ-UHFFFAOYSA-N 0.000 description 1
- 244000139693 Arctostaphylos uva ursi Species 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 1
- -1 Tyrosine amino acid Chemical class 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 238000013019 agitation Methods 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 229940073669 ceteareth 20 Drugs 0.000 description 1
- 229940081733 cetearyl alcohol Drugs 0.000 description 1
- 229940074979 cetyl palmitate Drugs 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 239000012141 concentrate Substances 0.000 description 1
- 239000003581 cosmetic carrier Substances 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 231100000433 cytotoxic Toxicity 0.000 description 1
- 230000001472 cytotoxic effect Effects 0.000 description 1
- 230000002939 deleterious effect Effects 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 229940008099 dimethicone Drugs 0.000 description 1
- 239000004205 dimethyl polysiloxane Substances 0.000 description 1
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 210000002615 epidermis Anatomy 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 229930182478 glucoside Natural products 0.000 description 1
- 150000008131 glucosides Chemical class 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 229930182470 glycoside Natural products 0.000 description 1
- 150000002338 glycosides Chemical class 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 235000008216 herbs Nutrition 0.000 description 1
- PXDJXZJSCPSGGI-UHFFFAOYSA-N hexadecanoic acid hexadecyl ester Natural products CCCCCCCCCCCCCCCCOC(=O)CCCCCCCCCCCCCCC PXDJXZJSCPSGGI-UHFFFAOYSA-N 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 239000002085 irritant Substances 0.000 description 1
- 231100000021 irritant Toxicity 0.000 description 1
- 210000002510 keratinocyte Anatomy 0.000 description 1
- 231100001252 long-term toxicity Toxicity 0.000 description 1
- 230000003061 melanogenesis Effects 0.000 description 1
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 1
- 229960002216 methylparaben Drugs 0.000 description 1
- FJJWJAFSUDWTTR-UHFFFAOYSA-N n,n-dihydroxyaniline Chemical compound ON(O)C1=CC=CC=C1 FJJWJAFSUDWTTR-UHFFFAOYSA-N 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
- 229960003415 propylparaben Drugs 0.000 description 1
- 230000036555 skin type Effects 0.000 description 1
- 229940100459 steareth-20 Drugs 0.000 description 1
- 210000000498 stratum granulosum Anatomy 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 235000019156 vitamin B Nutrition 0.000 description 1
- 239000011720 vitamin B Substances 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/45—Ericaceae or Vacciniaceae (Heath or Blueberry family), e.g. blueberry, cranberry or bilberry
-
- 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
- A61K8/14—Liposomes; Vesicles
-
- 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
- A61K8/602—Glycosides, e.g. rutin
-
- 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
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
-
- 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
- A61K2800/74—Biological properties of particular ingredients
- A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
- A61K2800/782—Enzyme inhibitors; Enzyme antagonists
Definitions
- the invention relates to topical cosmetic compositions, in particular, human skin lightening compositions, comprising admixtures of alpha arbutin and bearberry extract used for topical application.
- the present invention is a novel topically applied dermocosmetic composition comprising certain admixtures of the glucoside alpha arbutin and the botanical extract bearberry to be used in skin lightening.
- Melanocytes are located deep in the stratum granulosum, produce melanin, and through an unknown mechanism the melanin rises through about 100 cell layers to the surface where they exist as unsightly dark spots.
- Tyrosinase is the enzyme which catalyzes the amino acid tyrosine into dopa (dihydroxyphenylamine), as well as the change from dopa into dopaquinone.
- Skin lightening products are designed to inhibit the action of tyrosinase.
- Hydroquinone is the most common inhibitor of the enzyme tyrosinase. Hydroquinone is OTC Monographed (United States Food and Drug Administration 21 CFR) as a Category I skin lightener/skin bleacher/skin whitener in the concentration limits of 1.5-2.0% by weight. Used in this concentration, no clinical trials and no pre-market clearance are necessary in the USA marketplace. Used in higher concentrations than 2% by weight, hydroquinone compositions legally require a prescription in the USA marketplace. Production of hydroquinone preparations over 2% by weight requires an approved ANDA (Approved New Drug Application-21 CFR 394). However, hydroquinone is an irritant to some individuals, particularly those with light skin types, and may be cytotoxic to melanocytes. It is not legally marketed in Japan, the Union of South Africa and several other countries at present, and several other countries are considering denying legal marketing clearance because of concern about long term toxicity.
- Alpha arbutin avoids the direct toxicity of hydroquinone and the indirect toxicity of beta arbutin which easily hydrolyses to hydroquinone.
- Alpha arbutin acts more slowly than hydroquinone, taking a slightly longer time to meet the customer's skin lightening objectives when used alone.
- This invention involves the use of alpha arbutin and bearberry extract in combination, This combination is synergistic in skin whitening effectiveness, as the bearberry extract serves to potentiate the alpha arbutin.
- the alpha-glucosidic bond has a higher stability than the beta gluosidic bond, giving greater stability and greater effectiveness than beta arbutin.
- This invention teaches that the use of polyolprepolymer-2, when admixed with the serum comprised of alpha arbutin and octyl stearate, can be administered into the human skin using a liposome advanced delivery mechanism.
- Liposomes can easily be formed by those familiar in the art of liposome manufacture, using either preformed empty liposomes (Brookosomes MT) or by using ultra high pressure (20,000-40,000 PSI) in the usual microfluidizer.
- a serum comprised of alpha arbutin 0.01-6.0% w/w (more preferably 1-4% w/w) plus bearberry extract 0.01% w/w (most preferably 1-3% w/w) is admixed with polyolprepolymer-2 0.5-10% w/w (most preferably 1-3% w/w), and this combination is further prepared into a liposome form with the use of lecithin, water and ultra high pressure microfludizer.
- the liposome formation is well known to those familiar in the use of the ultra high PSI providing microfluidizer.
- This invention additionally teaches the serum-liposome admixture being further admixed into a gel or cream carrier as an advanced delivery system used in cosmetic, esthetician, spa and dermatology office settings.
- this stabilized alpha arbutin-polyolprepolymer 2-liposome concentrate which has been diluted into a cosmetic carrier, is potentiated with the admixture of the proven botanical extract, bearberry extract.
- additional nutrients including Vitamins A, B, C, E and Panthenol may be included in the liposome addition process.
- the most preferable embodiment composition is as follows: Part Ingredient INCI Percentage by weight A Aqua (water) qs 100% A Methylparaben 0.23 A Glycerin 4 A EDTA disodium 0.12 B Cetearyl alcohol, ceteareth 20 9 B Propylparaben 0.12 B Cetyl palmitate 2 B Dimethicone 50 1 B Steareth-20 1 C Alpha arbutin 3 C Octyl stearate 7 C Polyolprepolymer-2 2 D Lecithin, Water 1 (Brookosomes MT) Lecithin, Vitamins A, C & E 1 E Bearberry Extract 1 (Gatulin-Gattefosse)
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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)
- Epidemiology (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Birds (AREA)
- Botany (AREA)
- Medicinal Chemistry (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Engineering & Computer Science (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Biotechnology (AREA)
- Medical Informatics (AREA)
- Alternative & Traditional Medicine (AREA)
- Molecular Biology (AREA)
- Dermatology (AREA)
- Cosmetics (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
-
6,695,260 May, 2003 Ley, et al. 6,537,527 March, 2002 Kvalnes, et al 6,492,326 December, 2002 Robinson, et al 6,077,503 June, 2000 Dornoff, et al. 5,980,904 November, 1999 Ley, et Al. 5,932,608 August, 1999 Nguyen, et. Al. 5,854,327 October, 1998 Neis, et al. 5,747,006 May, 1998 Dornoff, et al. 5,700,784 December, 1997 Shinujima, et al 5,310,730 April, 1987 Tokugan, et al 4,764,505 March, 1985 Tokugan, et al 4,278,656 December, 1992 Leverett et al. -
672746 September, 1995 EP. 95/01157 January, 1995 WO. 2577805 January, 1994 FR -
- Abstracts of Japan, Vol. 11, No. 297 (C448)(2744) Sep. 25, (JPA 620 896081, Apr. 24, 1987.
- Centerchem Brochure: Alpha Arbutin, Norwalk, Conn. 2001.
- Cosmetics & Toiletries, vol. 111, pp.43-51, Giuseppe Prota, PhD, Melatanins and Melanogenesis, 1996
- Gattefosse Brochure: “Gatulene Whitening,” BP603-F 69804 St. Priest Cedex, France.
- Laboratoire Serobiologiques brochure: “Dermawhite,” Nancy, France.
- Chemical Abstracts, Vol. 87, No 5, Columbus, Ohio. Abstract 28987, 1995.
- Youngken, H. W., Textbook of Pharmacognosy, p. 639, Blakiston, Philadelphia, 1948.
- Rodale's Illustrated Encyclopedia of Herbs, p 170, Rodale Press, Emmaus, Pa. 1997.
- Polyolprepolymer-2, Brochure, Barnet, Englewood Cliffs, N.J. 1999.
- Brookosomes, Liposome Brochure, Brook's Industries Inc., South Plainfield, N.J. 2000.
- Chemical Abstracts (121.91340) Skin Lightening Property Containing Gentistic Acid Ester. Glycosides, Shinijiana, et. al. 1994.
- The invention relates to topical cosmetic compositions, in particular, human skin lightening compositions, comprising admixtures of alpha arbutin and bearberry extract used for topical application.
- The present invention is a novel topically applied dermocosmetic composition comprising certain admixtures of the glucoside alpha arbutin and the botanical extract bearberry to be used in skin lightening.
- Certain humans at different phases of their lifetime, and from different parts of the world, and in differing phases of their health develop excess melanin and/or colored blemishes on the skin. This excess melanin can occur on any part of the human body, but most commonly appear on the face and back of the hands. These dark spots are caused by high levels of melanin in the keratinocytes located in the top layer of the epidermis.
- Melanocytes are located deep in the stratum granulosum, produce melanin, and through an unknown mechanism the melanin rises through about 100 cell layers to the surface where they exist as unsightly dark spots.
- Biochemically, the process is:
-
- Tyrosine amino acid (from diet) goes to Dopa; Dopa goes to Dopaquinone;
- Dopaquinone goes to Dopachrome; Dopachrome goes to Melanin. Melanin deposits are seen as the dark spots on the surface of the human skin. They may be called “sun spots” or “age spots” or “liver spots.”
- Tyrosinase is the enzyme which catalyzes the amino acid tyrosine into dopa (dihydroxyphenylamine), as well as the change from dopa into dopaquinone. Skin lightening products are designed to inhibit the action of tyrosinase.
- Hydroquinone is the most common inhibitor of the enzyme tyrosinase. Hydroquinone is OTC Monographed (United States Food and Drug Administration 21 CFR) as a Category I skin lightener/skin bleacher/skin whitener in the concentration limits of 1.5-2.0% by weight. Used in this concentration, no clinical trials and no pre-market clearance are necessary in the USA marketplace. Used in higher concentrations than 2% by weight, hydroquinone compositions legally require a prescription in the USA marketplace. Production of hydroquinone preparations over 2% by weight requires an approved ANDA (Approved New Drug Application-21 CFR 394). However, hydroquinone is an irritant to some individuals, particularly those with light skin types, and may be cytotoxic to melanocytes. It is not legally marketed in Japan, the Union of South Africa and several other countries at present, and several other countries are considering denying legal marketing clearance because of concern about long term toxicity.
- Alpha arbutin avoids the direct toxicity of hydroquinone and the indirect toxicity of beta arbutin which easily hydrolyses to hydroquinone. Alpha arbutin acts more slowly than hydroquinone, taking a slightly longer time to meet the customer's skin lightening objectives when used alone. This invention involves the use of alpha arbutin and bearberry extract in combination, This combination is synergistic in skin whitening effectiveness, as the bearberry extract serves to potentiate the alpha arbutin. Moreover, the alpha-glucosidic bond has a higher stability than the beta gluosidic bond, giving greater stability and greater effectiveness than beta arbutin.
- This patent teaches that the use of polyolprepolymer-2 in an admixture with alpha arbutin/bearberry extract. This is in order to both extend the stability of the alpha arbutin to avoid possible deleterious effects due to oxidation related to the oxygen in the atmosphere as well as that caused by cell respiration potentiators found in epidermal respiration,
- This invention teaches that the use of polyolprepolymer-2, when admixed with the serum comprised of alpha arbutin and octyl stearate, can be administered into the human skin using a liposome advanced delivery mechanism. Liposomes can easily be formed by those familiar in the art of liposome manufacture, using either preformed empty liposomes (Brookosomes MT) or by using ultra high pressure (20,000-40,000 PSI) in the usual microfluidizer.
- In the preferred embodiment of this invention, a serum comprised of alpha arbutin 0.01-6.0% w/w (more preferably 1-4% w/w) plus bearberry extract 0.01% w/w (most preferably 1-3% w/w) is admixed with polyolprepolymer-2 0.5-10% w/w (most preferably 1-3% w/w), and this combination is further prepared into a liposome form with the use of lecithin, water and ultra high pressure microfludizer. The liposome formation is well known to those familiar in the use of the ultra high PSI providing microfluidizer.
- This invention additionally teaches the serum-liposome admixture being further admixed into a gel or cream carrier as an advanced delivery system used in cosmetic, esthetician, spa and dermatology office settings.
- Additionally, this stabilized alpha arbutin-polyolprepolymer 2-liposome concentrate, which has been diluted into a cosmetic carrier, is potentiated with the admixture of the proven botanical extract, bearberry extract. Moreover, additional nutrients including Vitamins A, B, C, E and Panthenol may be included in the liposome addition process.
- Clinical testing using before and after microscopic videos establishes that this potentiation takes place in clinical, human usage.
- The most preferable embodiment composition is as follows:
Part Ingredient INCI Percentage by weight A Aqua (water) qs 100% A Methylparaben 0.23 A Glycerin 4 A EDTA disodium 0.12 B Cetearyl alcohol, ceteareth 20 9 B Propylparaben 0.12 B Cetyl palmitate 2 B Dimethicone 50 1 B Steareth-20 1 C Alpha arbutin 3 C Octyl stearate 7 C Polyolprepolymer-2 2 D Lecithin, Water 1 (Brookosomes MT) Lecithin, Vitamins A, C & E 1 E Bearberry Extract 1 (Gatulin-Gattefosse) - Manufacturing procedure for the most preferred embodiment is as follows:
-
- The hot part B (80 degrees C.) is mixed into the hot part A (80 degrees C.) to form the conventional emulsion core. Continue mixing and cooling.
- Part C is prepared in a separate jacketed kettle at about 45 degrees C.
- As part AB is mixing and cooling to about 45 degrees C., slowly add part C with mixing, then slowly add part D (all liposomes).
- Continue to mix and cool part ABCD to about 35 degrees C. Slowly add with high agitation the Part E. Continue to mix and cool to 25 degrees C.
Claims (4)
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11/060,348 US20060188559A1 (en) | 2005-02-18 | 2005-02-18 | Topical cosmetic compositions comprising alpha arbutin |
| US11/745,632 US7431949B2 (en) | 2005-02-18 | 2007-05-08 | Topical cosmetic compositions containing alpha arbutin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11/060,348 US20060188559A1 (en) | 2005-02-18 | 2005-02-18 | Topical cosmetic compositions comprising alpha arbutin |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| US11/745,632 Division US7431949B2 (en) | 2005-02-18 | 2007-05-08 | Topical cosmetic compositions containing alpha arbutin |
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| US20060188559A1 true US20060188559A1 (en) | 2006-08-24 |
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| US11/060,348 Abandoned US20060188559A1 (en) | 2005-02-18 | 2005-02-18 | Topical cosmetic compositions comprising alpha arbutin |
| US11/745,632 Expired - Lifetime US7431949B2 (en) | 2005-02-18 | 2007-05-08 | Topical cosmetic compositions containing alpha arbutin |
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| US11/745,632 Expired - Lifetime US7431949B2 (en) | 2005-02-18 | 2007-05-08 | Topical cosmetic compositions containing alpha arbutin |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009256268A (en) * | 2008-04-18 | 2009-11-05 | Pias Arise Kk | Retinoid stabilized composition, skin external preparation and cosmetic comprising the composition |
| KR101355216B1 (en) * | 2012-11-19 | 2014-01-28 | 홍소영 | A facial mask sheet comprising a composition comprising liposomes for accelerating percutaneous absorptionn |
| US9445975B2 (en) | 2008-10-03 | 2016-09-20 | Access Business Group International, Llc | Composition and method for preparing stable unilamellar liposomal suspension |
| US9949913B2 (en) * | 2016-03-14 | 2018-04-24 | Jan Marini Skin Research | Luminate face lotion |
| US20220110852A1 (en) * | 2020-10-14 | 2022-04-14 | Chanda Zaveri | Pigment Stabilizers |
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| US20080312174A1 (en) * | 2007-06-05 | 2008-12-18 | Nitto Denko Corporation | Water soluble crosslinked polymers |
| CA2698812A1 (en) * | 2007-09-14 | 2009-03-19 | Nitto Denko Corporation | Drug carriers |
| JP6071166B2 (en) | 2007-11-14 | 2017-02-01 | オーエムピー インコーポレイテッドOMP,Inc. | Skin treatment composition |
| US20100158842A1 (en) * | 2008-10-09 | 2010-06-24 | Spectrum Dynamics Llc | Natural skin whitener: 4-hydroxy-oxindole-3-acetic acid |
| BR112021025797A2 (en) * | 2019-10-16 | 2022-02-01 | Maria Tripod | Cream for acne and melasma treatment |
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Also Published As
| Publication number | Publication date |
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| US7431949B2 (en) | 2008-10-07 |
| US20070207110A1 (en) | 2007-09-06 |
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