US20030129259A1 - Topical lightening compostitions and methods of use - Google Patents

Topical lightening compostitions and methods of use Download PDF

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Publication number
US20030129259A1
US20030129259A1 US10/034,186 US3418601A US2003129259A1 US 20030129259 A1 US20030129259 A1 US 20030129259A1 US 3418601 A US3418601 A US 3418601A US 2003129259 A1 US2003129259 A1 US 2003129259A1
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United States
Prior art keywords
composition
agent
melanin
topical
present
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Abandoned
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US10/034,186
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English (en)
Inventor
Harish Mahalingam
Brian Jones
Gopinathan Menon
Christos Kyrou
Michael Traudt
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Avon Products Inc
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Avon Products Inc
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Priority to US10/034,186 priority Critical patent/US20030129259A1/en
Application filed by Avon Products Inc filed Critical Avon Products Inc
Assigned to AVON PRODUCTS, INC. reassignment AVON PRODUCTS, INC. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: JONES, BRIAN, KYROU, CHRISTOS D., MAHALINGAM, HARISH, MENON, GOPINATHAN K., TRAUDT, MICHAEL
Priority to CA002411222A priority patent/CA2411222C/en
Priority to JP2002348249A priority patent/JP4601898B2/ja
Priority to MXPA02011912A priority patent/MXPA02011912A/es
Priority to US10/319,781 priority patent/US7014844B2/en
Priority to EP02028448A priority patent/EP1325738B1/en
Priority to DE60218125T priority patent/DE60218125T2/de
Priority to PL357931A priority patent/PL211313B1/pl
Priority to CNB021598061A priority patent/CN1293862C/zh
Assigned to AVON PRODUCTS, INC. reassignment AVON PRODUCTS, INC. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: JONES, BRIAN, TRAUDT, MICHAEL, MAHALINGAM, HARISH, KYROU, CHRISTOS D., MENON, GOPINATHAN K.
Publication of US20030129259A1 publication Critical patent/US20030129259A1/en
Priority to US11/215,874 priority patent/US7544351B2/en
Abandoned legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00—Preparations for care of the hair
    • A61Q5/08—Preparations for bleaching the hair
    • 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
    • A61K8/9706—Algae
    • A61K8/9722—Chlorophycota or Chlorophyta [green algae], e.g. Chlorella
    • 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
    • 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]
    • A61K8/9794—Liliopsida [monocotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61K2800/70—Biological properties of the composition as a whole

Definitions

  • the present invention relates to the lightening of the skin, hair, nails and/or lips.
  • the present invention further relates to compositions and methods for lightening the skin, hair, nails and/or lips.
  • Perilla extract is disclosed as a whitening agent in U.S. Pat. Nos. 5,980,904 and Japanese Publications 07025742, 07187989, 10265322, 2001163759, and 2001181173.
  • coconut fruit extract is disclosed as a whitening agent in Japanese Patent No. 2896815 B2.
  • An extract of spongy mass of coconut tissue is employed in a tanning sunscreen composition in U.S. Pat. No. 5,756,099.
  • Skin and hair pigmentation is determined by the level of melanin present in the epidermis and hair fiber, respectively.
  • melanin present in, for example, the epidermis: DHI-melanin, DHICA-melanin and pheomelanin.
  • the different types of melanin vary in color or shade. DHI-melanin is the darkest and is blackish in color.
  • DHICA-melanin is brownish in color.
  • Pheomelanin is the lightest and is reddish in color.
  • Melanin is synthesized in specialized organelles called melanosomes within pigment-producing cells (melanocytes). Melanocytes respond to stimuli to regulate melanin synthesis.
  • a topical composition that provides enhanced levels of lightening, bleaching, hypopigmenting, whitening and/or depigmenting (hereinafter referred to individually and collectively as “lightening” or “lighten”). It would be further desirable to have a topical composition that contains lightening agents that acted to interfere with the conversion of DOPAchrome to DHI-melanin and DHICA-melanin. It would be yet further desirable to have a topical composition that contains lightening agents that act to inhibit or prevent the transfer (uptake) of melanin from the melanocytes to the keratinocytes. It would still yet be further desirable to have methods for lightening the skin, hair, nails and/or lips employing the compositions of the present invention.
  • a topical lightening composition comprising a melanin synthesis-regulating agent, and a vehicle.
  • a topical lightening composition comprising an extract of perilla leaf and a vehicle.
  • a topical lightening composition comprising a lightening agent selected from the group consisting of coconut water, palm water, palm nut milk, pecan nut milk, almond nut milk, cashew nut milk, walnut nut milk, concentrates of the foregoing, and combinations of any of the foregoing, and a vehicle.
  • a lightening agent selected from the group consisting of coconut water, palm water, palm nut milk, pecan nut milk, almond nut milk, cashew nut milk, walnut nut milk, concentrates of the foregoing, and combinations of any of the foregoing, and a vehicle.
  • methods for lightening the skin, hair, lips, and/or nails comprising topically applying any one of these compositions.
  • FIG. 1 illustrates the results of the melanin uptake assay in the Examples.
  • the invention is not limited by any particular characterization of the physiological and/or chemical effects of topical lightening agents.
  • the topical lightening agents useful in the compositions and methods of the present invention lighten the skin by regulating melanin production and inhibiting the uptake of melanin in the skin, hair, lips, and/or nails.
  • One embodiment of the present invention is the employment of a melanin synthesis-regulating agent individually, or in combination with a melanin uptake-inhibiting agent.
  • a melanin synthesis-regulating agent is present in an amount effective to inhibit DCT and/or DHICA polymerase, a superior lightening composition can be attained. It was heretofore unknown in the art that interference in this part of the melanin synthesis pathway could bring about lightening of the skin, hair, lips, and/or nails.
  • a flow chart of the melanin synthesis pathway is as follows:
  • melanin synthesis-regulating agents include coconut water, coconut milk, palm water, palm nut milk, pecan nut milk, almond nut milk, cashew nut milk, walnut nut milk, concentrates of each of the foregoing, or combinations of any of the foregoing.
  • melanin uptake-inhibiting agents include extracts or oils derived from all or parts of the perilla plant, e.g. the leaf, seed, stem, and root.
  • a preferred agent is extract of the perilla leaf.
  • perilla leaf extract as a lightening agent in a topical lightening composition, either individually or in combination with another lightening agent.
  • Perilla leaf extract provides an unexpected enhancement of topical lightening efficacy compared to extracts, concentrates, or oils of other parts of the perilla plant, i.e. the seed, stem and root.
  • the perilla leaf extract can provide topical lightening efficacy at a lower amount compared to extracts of other parts of the perilla plant.
  • Another embodiment of the present invention is the use of any of the following as a topical lightening agent in a composition: coconut water, palm water, palm nut milk, pecan nut milk, almond nut milk, cashew nut milk, walnut nut milk, concentrates of the foregoing, or combinations of any of the foregoing. They can be used as the principal topical lightening agent or in combination with other lightening agents.
  • coconut water is preferred.
  • a freeze-dried concentrate of coconut water is most preferred.
  • coconut water or the concentrate thereof is believed to provide superior lightening efficacy compared to extracts, concentrates, or oils of other parts of the coconut and/or coconut tree, i.e. the fruit, milk, shell, seed, leaf, and bark.
  • Topical lightening agents are present in the present composition at a level sufficient to induce the desired effect of lightening.
  • the amount will vary depending upon the type of agent and the nature and level of desired effect.
  • the lightening agent will typically be present from about 0.001 wt % to about 20 wt %, more preferably from about 0.01 wt % to about 5 wt %, and most preferably from about 0.1 wt % to about 2.5 wt %, based on the total weight of the composition.
  • compositions of the present invention preferably include at least one, more preferably at least two, most preferably at least three, of the following ingredients: aloe barbadensis or an extract thereof, hydrolyzed soy protein, n-glucosamine, gamma-aminobutyric acid, a competitive inhibitor of melanocyte stimulating hormone (MSH) (e.g. hexapeptide-2), clintonia borealis (bluebeard lily) or an extract thereof, milk proteins, hydrolyzed milk proteins, sanguisorba officinalis (burnet), a glutathione reductase inhbitor (e.g. wheat germ) or extracts thereof.
  • MSH melanocyte stimulating hormone
  • compositions of the present invention can be used to effectively lighten skin, hair, lips and nails be topically applying the composition having an effective amount of the topical lightening agent.
  • the present compositions should preferably be rubbed onto/into the scalp so that the composition can penetrate into the hair follicles or root shafts and be absorbed into the hair during the melanin production process.
  • compositions of the present invention can be applied to treat a variety of skin conditions, including freckles, age spots, dark spots, hyperpigmentation, post-. inflammatory hyperpigmentation, (e.g. post-acne hyperpigmentation), discoloration, melasma, yellowing, and dark circles under the eyes.
  • the present compositions may include any vehicle known in the art. Suitable vehicles include, but are not limited to, water; one or more vegetable oils; esters such as octyl palmitate, isopropyl myristate and isopropyl palmitate; ethers such as dicapryl ether and dimethyl isosorbide; alcohols such as ethanol and isopropanol; fatty alcohols such as cetyl alcohol, stearyl alcohol and behenyl alcohol; isoparaffins such as isooctane, isododecane and isohexadecane; silicone oils such as dimethicones and polysiloxanes; hydrocarbon oils such as mineral oil, petrolatum, isoeicosane and polyisobutene; polyols such as propylene glycol, glycerin, butylene glycol, pentylene glycol and hexylene glycol; or combinations thereof.
  • Suitable vehicles include, but are not limited to, water; one or
  • the present compositions may include additional skin whitening agents known in the art.
  • useful agents include the following: hydroquinone, kojic acid, licorice and/or its derivatives, ascorbic acid/ascorbic acid derivatives, arbutin, bearberry, Glycyrrhiza glabra and its derivatives, and Chlorella vulgaris extract.
  • Other whitening agents are disclosed in U.S. Pat. No. 5,980,904, which is incorporated by reference herein.
  • compositions may include one or more of the following ingredients: anesthetics, anti-allergenics, antifungals, antimicrobials, anti-inflammatories, antiseptics, chelating agents, colorants, emollients, exfollients, film formers, fragrances, humectants, insect repellents, lubricants, moisturizers, pharmaceutical agents, preservatives, skin protectants, skin penetration enhancers, stabilizers, surfactants, thickeners, viscosity modifiers, or vitamins.
  • compositions can be made into any suitable product form.
  • product forms include, but are not limited to, a cream, lotion, ointment, gel, foam, pomade, aerosol spray, pump spray, a stick, towelette, or patch.
  • DOPAchrome Tautomerase (DCT) activity was assayed according to the method disclosed in Chakraborty et al., 1998, Effect of arbutin on melanogenic proteins in human melanocytes, Pigment Cell Res. 11: 206-212. Specifically, ice-cold DOPA (0.5 mg per ml of 0.1 M sodium phosphate buffer, pH 6.8) was mixed with Ag 2 O (30 mg Ag 2 O: 1 mg DOPA) for about 1 minute and filtered through a 0.22 ⁇ m Millipore filter. DCT was assayed spectrophotometrically by adding up to 0.1 ml cell extract to 0.5 ml of a solution of freshly prepared DOPAchrome ( ⁇ 0.5 mg/ml).
  • DOPAchrome Tautomerase (DCT) activity was assayed according to the method disclosed in Chakraborty et al., 1998, Effect of arbutin on melanogenic proteins in human melanocytes, Pigment Cell Res. 11: 206-212. Specifically, ice-
  • a DHICA polymerase assay was done according to the method disclosed in Chakraborty et al., 1996, Polymerization of 5,6-dihydroxyindole-2-Carboxylic acid to melanin by the pmel17/silver locus protein, Eur. J. Biochem. 236: 180-188. Specifically, the cell extract (0.5 ml, 150-200 ⁇ g protein) was passed through a wheat germ agglutinin column (1 ml bed volume) equilibrated with lysis buffer. The bound material was eluted with 0.5 ml 1M N-acetyl glucosamine, which contains crude DHICA polymerization factor and other melanogenic proteins.
  • Confluent cultures of B16 melanocytes produce moderate levels of melanosomes. However, to induce elevated melanosome production in this cell line, semi-confluent (60%) cultures of B16 cells were treated for approximately 36 hours with normal growth medium supplemented with 10 mM ammonium chloride (final conc.). The medium was then aspirated and the hypermelanotic cells were washed (2 ⁇ 2 ml) with distilled water to provide a hypotonic stress to the cells. An aliquot (2 ml) of a hypotonic lysis solution (0.02% NP-40 in water) was added to each plate and the plates were incubated for approximately 5 min at room temperature.
  • a hypotonic lysis solution 0.02% NP-40 in water
  • the cellular material from three (3) culture plates were pooled in a 15 ml conical tube and centrifuged at approximately (200 ⁇ g) for 5 minutes to remove cellular debris.
  • the resulting supernatant containing melanosomes was transferred to a clean 15 ml conical tube and centrifuged (850 ⁇ g) for 20 minutes.
  • the resulting pellet containing the isolated melanosomes were resuspended in 1 ml of Phosphate Buffered Saline (PBS) and stored at 4° C. until used.
  • PBS Phosphate Buffered Saline
  • NHEKs normal human epidermal keratinocytes
  • DMEM/KGM-2 the appropriate growth medium
  • the cells were treated with different concentations of perilla leaf extract (powder form or aqueous form). The cells were then returned to the incubator for approximately 1.5 hours.
  • each well of keratinocytes was treated with the amount of melanosomes isolated from a single plate of B16 cells.
  • the 24 well plates of treated keratinocytes were centrifuged for 15 minutes at 1,000 rpm to facilitate the deposition of the melanosomes onto the surface membranes of the keratinocytes. The plates were then returned to the incubator for 1.25 hours.
  • the cells in each well of keratinocytes were rinsed (3 ⁇ 1 ml) with PBS, removed from the plate using trypsin/EDTA, washed with PBS.
  • the internalized melanin was extracted from the cells according to a modified method of Bessou-Touya, S., et al. (Chimeric human epidermal reconstructs to study the role of melanocytes and keratinocytes in pigmentation and photoprotection. J. Invest. Dermatol., 111:1103-1108, 1998) and quantified spectrophotometrically by determining the melanin-specific absorbance at 405 nm.

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US10/034,186 2001-12-28 2001-12-28 Topical lightening compostitions and methods of use Abandoned US20030129259A1 (en)

Priority Applications (10)

Application Number Priority Date Filing Date Title
US10/034,186 US20030129259A1 (en) 2001-12-28 2001-12-28 Topical lightening compostitions and methods of use
CA002411222A CA2411222C (en) 2001-12-28 2002-11-06 Topical lightening compositions and methods of use
JP2002348249A JP4601898B2 (ja) 2001-12-28 2002-11-29 局所性ライトニング組成物およびその使用方法
MXPA02011912A MXPA02011912A (es) 2001-12-28 2002-12-02 Composiciones aclaradoras topicas y metodos para su uso.
US10/319,781 US7014844B2 (en) 2001-12-28 2002-12-13 Lightening compositions and methods of use
EP02028448A EP1325738B1 (en) 2001-12-28 2002-12-19 Non therapeutical methods and medical uses for depigmenting the skin
DE60218125T DE60218125T2 (de) 2001-12-28 2002-12-19 Nicht therapeutisches Verfahren sowie therapeutische Anwendungen zur Hautdepigmentierung
PL357931A PL211313B1 (pl) 2001-12-28 2002-12-20 Kompozycje rozjaśniające do miejscowego stosowania i sposób ich stosowania
CNB021598061A CN1293862C (zh) 2001-12-28 2002-12-27 局部颜色调浅组合物及其使用方法
US11/215,874 US7544351B2 (en) 2001-12-28 2005-08-31 Topical lightening compositions and methods of use

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US10/034,186 US20030129259A1 (en) 2001-12-28 2001-12-28 Topical lightening compostitions and methods of use

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US10/319,781 Continuation-In-Part US7014844B2 (en) 2001-12-28 2002-12-13 Lightening compositions and methods of use
US11/215,874 Continuation US7544351B2 (en) 2001-12-28 2005-08-31 Topical lightening compositions and methods of use

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US10/319,781 Expired - Fee Related US7014844B2 (en) 2001-12-28 2002-12-13 Lightening compositions and methods of use
US11/215,874 Expired - Fee Related US7544351B2 (en) 2001-12-28 2005-08-31 Topical lightening compositions and methods of use

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US11/215,874 Expired - Fee Related US7544351B2 (en) 2001-12-28 2005-08-31 Topical lightening compositions and methods of use

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US (3) US20030129259A1 (enExample)
EP (1) EP1325738B1 (enExample)
JP (1) JP4601898B2 (enExample)
CN (1) CN1293862C (enExample)
CA (1) CA2411222C (enExample)
DE (1) DE60218125T2 (enExample)
MX (1) MXPA02011912A (enExample)
PL (1) PL211313B1 (enExample)

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US8486376B2 (en) 2002-10-25 2013-07-16 Foamix Ltd. Moisturizing foam containing lanolin
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US20050287089A1 (en) 2005-12-29
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US7544351B2 (en) 2009-06-09
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US20030157202A1 (en) 2003-08-21
MXPA02011912A (es) 2005-07-29
CA2411222C (en) 2010-01-19
EP1325738A2 (en) 2003-07-09
DE60218125T2 (de) 2007-11-22
US7014844B2 (en) 2006-03-21
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CN1293862C (zh) 2007-01-10
CA2411222A1 (en) 2003-06-28

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