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
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/55—Phosphorus compounds
• • 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
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/37—Esters of carboxylic acids
• • 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
  • A61K8/606—Nucleosides; Nucleotides; Nucleic acids
• • 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
• • 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
• • 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
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
  • A61Q19/08—Anti-ageing preparations

Definitions

• the invention relates to cosmetic and pharmaceutical compositions.
• the invention relates to cosmetic and pharmaceutical compositions which enhance skin cell energy and rejuvenate aging skin cells.
• the present invention now provides a means for enhancing the ATP levels of aged fibroblasts.
• the invention provides a method for increasing ATP levels in aging cells which comprises applying to the skin an effective amount of ADP, AMP, or oxaloacetic acid, or a combination thereof.
• the method is particularly useful in increasing energy in skin cells, particularly fibroblasts.
• the invention also provides cosmetic and pharmaceutical compositions for topical application to the skin comprising effective amounts of ADP, AMP, or oxaloacetate, or a combination thereof in a cosmetically or pharmaceutically acceptable carrier.
• the terms "ADP", "AMP” and "oxaloacetic acid” shall include safe and effective derivatives thereof which retain qualitatively the same activity.
• the present invention is based on an observation that the extrinsic provision of ADP, AMP or oxaloacetic acid (oxaloacetate) to skin cells results in an increase of cell energy present in the cells so treated.
• ADP, AMP or oxaloacetic acid is provided to normal fibroblasts in culture, ATP levels can be increased substantially.
• use of ADP and/or AMP and/or oxaloacetic acid as active agents in the treatment and prevention of skin aging is indicated.
• compositions of the invention comprise effective amounts of ADP, AMP or a combination thereof, in combination with a cosmetically or pharmaceutically acceptable carrier.
• effective amount is meant that amount of the active agent which can increase the amount of ATP in a treated cell at least about 10%, preferably at least about 20%, more preferably at least about 30%, and most preferably at least about 40%, relative to untreated cells.
• concentration of the active agent will be from about 0.001-10%, preferably about 0.01-5%, by weight of the total composition; the concentration may be varied depending upon the intended frequency of use of the composition, lower concentrations being employed with more frequent applications.
• the active components can be formulated with a variety of cosmetically and/or pharmaceutically acceptable carriers.
• pharmaceutically or cosmetically acceptable carrier refers to a vehicle, for either pharmaceutical or cosmetic use, which vehicle delivers the active components to the intended target and which will not cause harm to humans or other recipient organisms.
• pharmaceutical or cosmetic will be understood to encompass both human and animal pharmaceuticals or cosmetics.
• Useful carriers include, for example, water, acetone, ethanol, ethylene glycol, propylene glycol, butane-1, 3-diol, isopropyl myristate, isopropyl palmitate, or mineral oil.
• the carrier may be in any form appropriate to the mode of delivery, for example, solutions, colloidal dispersions, emulsions (oil-in-water or water-in- oil) , suspensions, creams, lotions, gels, foams, mousses, sprays and the like.
• the active agents of the invention can be used alone to increase the energy level of skin cells generally, so as to delay or reverse the onset of the cellular symptoms of aging.
• aging as used in the present specification and claims, is meant both photoaging, i.e., the premature aging which occurs as the result of excessive exposure to UV rays, and chronological aging, i.e., the naturally occurring, normal aging of the skin which occurs over time, even without prolonged sun exposure.
• the compositions of the invention are particularly suited for enhancing the energy levels of fibroblasts and keratinocytes in both normal and aging skin. Increase in energy levels of fibroblasts can be expected to delay or reverse the decrease in collagen and elastin production that characterizes aged fibroblasts.
• the increase in energy levels of keratinocytes can be expected to result in a delay in the thinning of the epidermis observed in aging skin.
• the use of the active agents of the invention is not limited to skin cells, however, but may also be expected to aid in energy increase in, for example, aging muscle or other connective tissue cells.
• Treatment of aging skin, or prevention of aging in normal, non-aged skin is preferably achieved by regular application of the composition over a period of time.
• a preferred method of obtaining the benefits of the composition is via chronic topical application of a safe and effective amount of a composition containing the mixture, to prevent or delay development of skin damage which may result from photo- or chronoaging, or to prevent worsening of or to reverse already established damage.
• topical application of the composition in an amount of from about 0.1 ⁇ g/cm 2 to 2 mg/cm 2 of exposed skin, be performed from about once per week to about 4 or 5 times daily, preferably from about 3 times a week to about 3 times daily, most preferably about once or twice per day.
• chromenic application it is meant herein that the period of topical application may be over the lifetime of the user, preferably for a period of at least about one month, more preferably from about three months to about twenty years, more preferably from about six months to about ten years, more preferably still from about one year to about five years, thereby resulting in the treatment or prevention of the external signs of photoaging and chronological aging.
• the compositions of the invention may also be used on a less frequent basis, for example, once or twice a month, as a sort of "spa treatment" with a higher level of active component provided on these occasions.
• the actives of the invention can also be combined with other anti-aging or skin-enhancing agents.
• the actives of the invention can be combined, for example, with one or more of the following products: alpha- or beta- hydroxy acids, such as lactic acid, glycolic acid, citric acid, alpha-hydroxyoctanoic acid, alpha-hydroxydecanoic acid, alpha-hydroxylauric acid, tartaric acid, glucouronic acid, galactouronic acid, alpha-hydroxybutyric acid, alpha- hydroxyisobutyric acid, malic acid, mandelic acid, pyruvic acid, and tartronic acid, and salicylic acid; retinoids, such as retinol, retinyl acetate, retinyl palmitate, retinyl butyrate, retinyl oleate, retinyl linoleate, and retinoic acid; and DHEA and derivatives thereof.
• alpha- or beta- hydroxy acids
• the formulation in addition to the carrier and active agents, also can comprise other components which may be chosen depending on the carrier and/or the intended use of the formulation. Additional components include, but are not limited to, water soluble colorants (such as FD&C Blue #1) ; oil soluble colorants (such as D&C Green #6) ; water soluble sunscreens (such as Eusolex 232) ; oil soluble sunscreens (such as octyl methoxycinnamate) ; particulate sunscreens (such as zinc oxide) ; antioxidants (such as BHT) ; chelating agents (such as disodium EDTA) ; emulsion stabilizers (such as carbomer) ; preservatives (such as methyl paraben) ; fragrances (such as pinene) ; flavoring agents (such as sorbitol) ; humectants (such as glycerine) ; waterproofing agents (such as PVP/Eicosene Copolymer) ; water soluble film
• compositions can be therapeutic products, ADP and/or AMP and/or oxaloacetic acid being the sole actives, or in combination with other actives.
• the compositions can also be a makeup products, for example, a lipstick, foundation, concealer, bronzer, blush, eyeshadow and the like.
• Normal human dermal fibroblasts are grown to confluence in flasks, and then divided into three different treatment sets. Testing is done at the point at which the cells have undergone 32 population doublings. The treatments are with ADP (Sigma), AMP(Yamasa Shoyu Co., Inc.), and creatine monophosphate (Sigma) , each at five different concentrations ranging from 0.01-1.0 mM. The growth medium serves as a control.
• the cells are treated for a period of 2 hours, and then trypsinized, washed and resuspended to 6X10 6 cells/ml.
• the cells are treated with a releasing agent, sodium lauryl sulfate, which causes the ATP contained within the cells to be released.
• the releasate is then added to a solution containing luciferin and luciferase.
• Luciferase utilizes the energy provided by free ATP to convert luciferin to oxyluciferin.
• the light released by this reaction is read on a spectrophotometer; the amount produced is proportional to the amount of ATP available.
• the ATP levels are calculated from an ATP standard curve, and then normalized on a per cell basis. The results are shown in Table 1. TABLE 1
• This example illustrates the increase in cell energy levels produced by treatment of cells with oxaloacetic acid.
• Normal human dermal fibroblasts are grown to subconfluence in flasks, treated with oxaloacetic acid for two hours with three samples, having concentrations of 0.05 mM, 0.50mM and 1.0 mM. The cells are then trypsinized, washed and resuspended to 6X10 6 cells/ml. The treated cells have undergone four passages. The cells are further treated and analyzed as described in the previous example, with the amount of ATP calculated at the various dosages. The results are shown in Table 2.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Dermatology (AREA)
• Birds (AREA)
• Epidemiology (AREA)
• Chemical & Material Sciences (AREA)
• Biochemistry (AREA)
• Molecular Biology (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Pharmacology & Pharmacy (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Medicinal Chemistry (AREA)
• Engineering & Computer Science (AREA)
• Organic Chemistry (AREA)
• Emergency Medicine (AREA)
• Gerontology & Geriatric Medicine (AREA)
• Cosmetics (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

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• 1999
  • 1999-04-22 EP EP99919884A patent/EP1003473A1/de not_active Ceased
  • 1999-04-22 AU AU37504/99A patent/AU744295B2/en not_active Expired
  • 1999-04-22 JP JP55424999A patent/JP2001503447A/ja active Pending
  • 1999-04-22 CA CA002294482A patent/CA2294482C/en not_active Expired - Lifetime
  • 1999-04-22 KR KR10-1999-7012177A patent/KR100426753B1/ko not_active IP Right Cessation
  • 1999-04-22 WO PCT/US1999/008497 patent/WO1999055302A1/en not_active Application Discontinuation

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