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
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)
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 |
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US11/060,348 US20060188559A1 (en) | 2005-02-18 | 2005-02-18 | Topical cosmetic compositions comprising alpha arbutin |
Related Child Applications (1)
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US11/745,632 Division US7431949B2 (en) | 2005-02-18 | 2007-05-08 | Topical cosmetic compositions containing alpha arbutin |
Publications (1)
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US20060188559A1 true US20060188559A1 (en) | 2006-08-24 |
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Family Applications (2)
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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 Active US7431949B2 (en) | 2005-02-18 | 2007-05-08 | Topical cosmetic compositions containing alpha arbutin |
Family Applications After (1)
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US11/745,632 Active 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 |
TW200918099A (en) * | 2007-09-14 | 2009-05-01 | Nitto Denko Corp | Drug carriers |
MX2010005285A (en) * | 2007-11-14 | 2010-06-02 | Omp Inc | Skin treatment compositions. |
US20100158842A1 (en) * | 2008-10-09 | 2010-06-24 | Spectrum Dynamics Llc | Natural skin whitener: 4-hydroxy-oxindole-3-acetic acid |
WO2021074718A1 (en) * | 2019-10-16 | 2021-04-22 | Tripod Maria | Cream for treating acne and melasma |
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JP2009256268A (en) * | 2008-04-18 | 2009-11-05 | Pias Arise Kk | Retinoid stabilized composition, skin external preparation and cosmetic comprising the composition |
US9445975B2 (en) | 2008-10-03 | 2016-09-20 | Access Business Group International, Llc | Composition and method for preparing stable unilamellar liposomal suspension |
KR101355216B1 (en) * | 2012-11-19 | 2014-01-28 | 홍소영 | A facial mask sheet comprising a composition comprising liposomes for accelerating percutaneous absorptionn |
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 |
CN114344186A (en) * | 2020-10-14 | 2022-04-15 | C·扎维拉 | Pigment stabilizer |
Also Published As
Publication number | Publication date |
---|---|
US20070207110A1 (en) | 2007-09-06 |
US7431949B2 (en) | 2008-10-07 |
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