EP2515830A1 - Compositions et méthodes pour l'augmentation de la graisse cellulaire et le blanchiment de la peau - Google Patents

Compositions et méthodes pour l'augmentation de la graisse cellulaire et le blanchiment de la peau

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Publication number
EP2515830A1
EP2515830A1 EP10842740A EP10842740A EP2515830A1 EP 2515830 A1 EP2515830 A1 EP 2515830A1 EP 10842740 A EP10842740 A EP 10842740A EP 10842740 A EP10842740 A EP 10842740A EP 2515830 A1 EP2515830 A1 EP 2515830A1
Authority
EP
European Patent Office
Prior art keywords
composition
skin
cosmeceutically
effective amount
peroxisome proliferator
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.)
Withdrawn
Application number
EP10842740A
Other languages
German (de)
English (en)
Other versions
EP2515830A4 (fr
Inventor
Sarah Bacus
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
0901911 B. C. UNLIMITED LIABILITY COMPANY
Original Assignee
0901911 B C UNLIMITED LIABILITY Co
B C UNLIMITED LIABILITY Co
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 0901911 B C UNLIMITED LIABILITY Co, B C UNLIMITED LIABILITY Co filed Critical 0901911 B C UNLIMITED LIABILITY Co
Publication of EP2515830A1 publication Critical patent/EP2515830A1/fr
Publication of EP2515830A4 publication Critical patent/EP2515830A4/fr
Withdrawn legal-status Critical Current

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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
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • 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
    • 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
    • A61Q19/005—Preparations for sensitive skin

Definitions

  • the present invention relates to a novel anti-wrinkle composition. More specifically, the invention relates to an anti-wrinkle composition whose active ingredient is a compound that acts as an peroxisome proliferator-activated receptor agonist. The invention further relates to a composition for smoothing the appearance of wrinkles in the skin, a composition for promoting lipid formation and a composition for improving skin tenacity, wherein the composition comprises the aforementioned compound, and to a method for reducing wrinkles or related skin signs of aging and a method for improving skin tenacity with the use of the composition.
  • the present invention also relates to a novel bleaching composition. More specifically, the invention relates to a bleaching composition with melatonin as an active ingredient. In addition, the invention can contain vitamin C or vitamin E as an active ingredient. The invention further relates to a composition for dimMshing the appearance of blemishes in the skin, wherein the composition comprises the aforementioned compound. The invention also relates to a method for diminishing blemishes or related skin signs of aging through use of the composition. BACKGROUND
  • Keratinocytes are stratified, squamous epithelial cells found in the skin and mucosa, including oral, esophageal, corneal, conjunctival, and genital epithelia. Keratinocytes provide a protective barrier between host and environment, functioning to prevent substances from the environment from entering the host as well as prevent the loss of important host components to the environment. Keratinocytes undergo differentiation as they progress from the basal layer of the basement membrane to the surface of the skin.
  • the peroxisome proliferator-activated receptors are a family of nuclear hormone receptors that function as ligand-gated transcription factors to facilitate activation and repression. PPARs are involved in a variety of physiological processes and various aspects of metabolic disease. PPARs have been shown to be transcriptionally activated by a diverse group of compounds, including clifibrate-related hypolipidemic drugs, the synthetic arachidonate analog ETYA (5, 8, 11, 14-eicosatetraynoic acid) the leukotriene antagonist LY-171883 and polyunsaturated fatty acids. See Tonotonoz et al.
  • PPARy2 a Lipid-Activated Transcription Factor
  • PPARy The activation of PPARy is primarily through ligand binding (endogenous ligands such as fatty acids or eicosanoids or exogenous ligands such as discussed below) which in turn activates the receptor.
  • endogenous ligands such as fatty acids or eicosanoids or exogenous ligands such as discussed below
  • exogenous ligands such as fatty acids or eicosanoids or exogenous ligands such as discussed below
  • thiazolidinediones e.g. pioglitazone, troglitazone and rosiglitazone
  • PPARy agonist ligands that function to increase insulin sensitivity and are primarily used in the treatment of type 2 diabetes.
  • PPAR modulate glucose metabolism and insulin sensitivity, thereby reducing plasma glucose and insulin levels in type 2 diabetes.
  • one of the thiazolidinediones, troglitazone acts as an agonist ligand to both PPARa and PPARy, with higher affinity for PPARy.
  • retin-A is used to increase collagen production, decrease elastin loss, decrease production of metalloproteases (which may cause oxidative damage to the skin), disperse melanin granules and exfoliate the layers of dead skin cells from the skin.
  • retin-A has some undesirable side effects and requires monitoring of sun exposure while treating skin.
  • Melatonin is a naturally occurring hormone that has varied expression during the daily cycle. Most commonly, it is know that melatonin affects the circadian rhythms of biological functions, in addition to its role as an antioxidant and its protection of DNA.
  • compositions are disclosed for cosmeceuticals that promote an increase in lipid production in keratinocytes.
  • Methods for preparing comeceutical compositions resulting in the promotion of an increase in lipid production in keratinocytes are also disclosed.
  • compositions are also disclosed for cosmeceuticals that diminish the appearance of skin blemishes.
  • Methods for preparing cosmeceutical compositions resulting in a reduction of skin blemishes are also disclosed.
  • the composition comprises at least one peroxisome proliferator-activated receptor gamma agonist in a cosmeceutically acceptable medicum.
  • the composition comprises troglitazone.
  • the composition comprises troglitazone and fibroblast growth factor.s
  • composition is topically administered or can also be formulated as a leave-on product.
  • the composition contains about 0.0005% to 0.5% by weight peroxisome proliferator-activated receptor gamma agonist. [0018] In another aspect, the composition contains about 0,0005% to 0.5% by weight peroxisome proliferator-activated receptor gamma agonist.
  • the composition contains about 0.005% to 0.05% by weight peroxisome proliferator-activated receptor gamma agonist.
  • the composition comprises at least one peroxisome proliferator-activated receptor gamma agonist and functions to promote lipid formation
  • Another aspect is a method of increasing lipid production in keratinocytes comprising the step of: topically administering a composition comprising a cosmeceutically effective amount of a peroxisome proliferator-activated receptor gamma agonist to a person in need thereof.
  • An additional aspect is a method of increasing lipid production in the skin comprising activation of peroxisome proliferator-activated receptor gamma with a composition containing a) a cosmeceutically acceptable medium and b) a cosmeceutically effective amount of at least one peroxisome proliferator-activated receptor gamma agonist, wherein said agonist has an affinity for peroxisome proliferator-activated receptor gamma.
  • Another aspect of the invention is a method of increasing lipid production in the skin with a composition comprismg troglitazone.
  • compositions comprising: a) a cosmeceutically acceptable medium and b) a cosmeceutically effective amount of melatonin, wherein the composition promotes lightening of the skin.
  • An additional embodiment is a composition comprising about 0.3% by weight melatonin.
  • An additional embodiment is a method of diminishing the appearance of darkened skin blemishes comprising the step of topically administering a composition comprising melatonin.
  • An additional embodiment is a composition comprising: a) a cosmeceutically acceptable medium, b) a cosmeceutically effective amount of at least one peroxisome proliferator-activated receptor gamma agonist and c) a cosmeceutically effective amount of melatonin.
  • Another aspect of the invention is a composition comprising about 0.005% by weight of peroxisome proliferator-activated receptor gamma agonist.
  • An additional aspect is a composition comprising about 0.15% by weight of melatonin.
  • An additional aspect is a composition comprising peroxisome proliferator-activated receptor gamma agonist and melatonin that is topically administered or formulated as a leave-on product.
  • Another aspect of the invention is a composition comprising peroxisome proliferator-activated receptor gamma agonist, melatonin and fibroblast growth factor.
  • FIG. 1 is a photograph of keratmocytes treated with troglitazone and stained for lipids.
  • FIG. 2 is a photograph of human preadipocytes treated with troglitazone and stained for lipids.
  • FIG. 3 is a photograph of human preadipocytes treated with troglitazone and stained for lipids.
  • the present invention is based on the discovery that drugs, such as PPARy agonists, like troglitazone, affect the expression of genes in the lipid metabolic pathways and in turn cause an increase in the production of lipids in keratinocytes.
  • drugs such as PPARy agonists
  • troglitazone the topical administration of troglitazone has been shown to increase the lipid droplets in keratinocytes when compared to untreated cells.
  • the response of keratinocytes to treatment with troglitazone over a 48 hour treatment period results in an increase in lipid production of keratinocytes.
  • PPARs have been shown to induce enzymes of the peroxisomal fatty acid ⁇ - oxidation system and activate transcription of the acyl-CoA oxidase gene (which catalyzes the rate-limiting step in the ⁇ -oxidation pathway).
  • Activation of PPARy also known as NR1C3 based on its relationship to the steroid/thyroid hormone superfamily of nuclear receptors
  • PPARy is the functional receptor for thiazolidinediones (TZDs), a class of insulin-sensitizing drugs which are used in the treatment of type 2 diabetes mellitus.
  • TZDs thiazolidinediones
  • PPARy has also been shown to be involved in differentiation of other cells and tissues, such as macrophages, breast, and colon, and mutations of PPARy that destroy receptor function have been found in sporadic human colon cancer.
  • PPARy functions as a heterodimer with retinoid X receptor (RXR) and binds (as a PPARy/RXR complex) to sequences (DR-1 sites) and activates transcription upon ligand binding.
  • RXR retinoid X receptor
  • PPARy binds and is activated by the synthetic TZD ligands, and natural ligands such as fatty acid derivatives (15-deoxy-prostaglandin h, linoileic acid, PUFAs eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), and 9(S)- hydroxy-octadecadienoic acid (HODE), and several hydroxyeicosatetraenoic acids (HETEs)).
  • fatty acid derivatives (15-deoxy-prostaglandin h, linoileic acid, PUFAs eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), and 9(S)- hydroxy-octadecadienoic acid (HODE), and several hydroxyeicosatetraenoic acids (HETEs)).
  • Rosen et al. "PPARy Is Required for
  • PPARy ligands have also been shown to upregulate fibroblast growth factor 2 (FGF2). See Yasuda et al. "PPAR-y ligands up-regulate basic fibroblast growth factor-induced VEGF release through amplifying SAP /JNK activation in osteoblasts" 2005. Biochemical and Biophysical Research Communications" 328 (1):137-143
  • PPARy also plays a role in adipogenesis in early stages, following increases in the transcription factors, CCAAT/enhancer-binding protein ("C/EBP"), C/ ⁇ and C/ ⁇ .
  • C/EBP CCAAT/enhancer-binding protein
  • PPARy has two isoforms, PPARyl and PPARy2, which are both thought to be competent to stimulate adipogenesis.
  • PPARy expression results in increases in C/EBPa, which promotes the differentiated phenotype, at least in part by increasing the expression of PPARy via positive feedback.
  • PPARy has been shown to be sufficient to induce adipogenesis in a variety of cell types.
  • chimeric mouse analysis has shown PPARy is essential to the process of adipogenesis and may play a role in differentiation of other tissues as well (e.g. sebocytes, macrophages, and colon and breast epithelium). See Rosen et al. 1999.
  • PPARy and C/EBPa could interact to stimulate adipose tissue by activation of the complete adipocyte gene expression, although this may occur in a temporally regulated manner, with PPARy functioning to commit primitive mesodermal cells to the adipose lineage and activate expression of early genes and C EBPa functioning later in the differentiation process for expression of late genes responsible for triggering arrest, terminal differentiation, lipid accumulation, or some combination of these. See Tontonoz et al. 1994; Tontonoz et al. "Fat and Beyond: The Diverse Biology of PPARy” 2008, Annu. Rev. Biochem. 77:289-312.
  • PPARy operates at the center of the adipogenic cascade in a feedback loop with C/EBPa. It participates in a variety of signaling pathways operating CCAAT/enhancer-binding protein upstream of PPARy, including the hedgehog and Wnt pathways, C/ ⁇ and - ⁇ , and EBFs.
  • C/ ⁇ and C/ ⁇ C/ ⁇ and C/ ⁇
  • SREBP-lc SREBP-lc
  • Kruppel-like factor-5 KLF5
  • KLF15 zinc-finger protein 423
  • Zfp423 zinc-finger protein 423
  • Ebfl early B-cell factor
  • PPARy activates nearly all of the genes required for this process. These genes include aP2 which is required for transport of free fatty acids (FFAs) and perilipin which is a protein covering the surface of mature lipid droplets in adipocytes.
  • FFAs free fatty acids
  • perilipin a protein covering the surface of mature lipid droplets in adipocytes.
  • LPL lipoprotein lipase
  • ACS acyl-CoA synthase
  • ACAT acetyl-CoA acetyltransferase
  • PLA phospholipase A
  • GPDH glycerol-3-phosphate dehydrogenase
  • Troglitazone is a member of the thiazolidinedione class of drugs, an anti-diabetic and antiinflammatory drug. Other members of this drug family include: pioglitazone and rosiglitazone; which, like troglitazone, have all been shown to activate PPARs. Troglitazone is a ligand to both PPARa and PPARy (binding more strongly to PPARy). Structurally, troglitazone [(RS)-5-(4-[(6-hydroxy-2,5,7,8-tetr ⁇
  • troglitazone use has been associated with a decrease of nuclear factor kappa-B (NF- ⁇ - an important cellular transcription regulator for the immune response) and a concomitant increase in its inhibitor ( ⁇ ⁇ ).
  • NF- ⁇ - an important cellular transcription regulator for the immune response NF- ⁇ - an important cellular transcription regulator for the immune response
  • ⁇ ⁇ the inhibitor of the TZDs
  • the observed increase in lipid production upon treatment with troglitazone has many desired effects in management of skin and skin disorders, including anti-ageing, anti- wrinkle and/or an anti-cellulite effects, rmnimizing the appearance of wrinkles, blemishes, skin lines, oily skin, acne, dry skin, xerosis, ichthyosis, dandruff, brownish spots, keratosis, melasma, lentigines, age spots, dark circles around eyes, skin pigmentation, topical inflammation, liver spots, pigmented spots, wrinkles, blemishes, skin lines, oily skin, acne, warts, eczema, pruritic skin, psoriasis, inflammatory dermatoses, disturbed keratinization, dandruff, bacterial infection, fungal infection, wound healing, body odor, and skin changes associated with aging.
  • the present invention is based on the discovery that hormones, such as melatonin, affect the coloration of darkened spots on the surface of the skin and can diminish the appearance of such spots when placed in a cosmeceutical composition.
  • hormones such as melatonin
  • the addition of vitamin C or vitamin E to the composition also promotes the reduction of darkened skin spots and promotes bleaching of the skin.
  • the observed decrease in the appearance of darkened skin blemishes upon treatment with a melatonin composition has many desired effects in management of skin and skin disorders, including anti-ageing, minimizing the appearance of wrinkles, blemishes, dry skin, xerosis, ichthyosis, dandruff, brownish spots, keratoses, melasma, lentigines, age spots, dark circles around eyes, skin pigmentation, topical inflammation, liver spots, pigmented spots, skin lines, oily skin, acne, warts, eczema, pruritic skin, psoriasis, inflammatory dermatoses, disturbed keratinization, dandruff, bacterial infection, fungal infection, wound healing, body odor, and skin changes associated with aging.
  • composition of the invention contains a PPA y agonist in the presence of melatonin in a cosmeceutically acceptable medium/vehicle.
  • composition according to the invention also comprises a dermatologically/cosmetically acceptable vehicle to act as a diluent, dispersant or carrier for the ⁇ ⁇ agonist and/or melatonin.
  • vehicle can comprise materials commonly employed in skin care products such as water, liquid or solid emollients, silicone oils, emulsifiers, solvents, humectants, thickeners, powders, propellants and the like.
  • vehicle ingredients include water, glycerin, hydrogenated polyisobutene, cetearyl alcohol, ceteareth-20, macadamia integrifolia seed oil (macademia nut oil), dimethicone, tocopheryl acetate, stearoxytrimethylsilane, stearyl alcohol, panthenol, farnesol, benzyl alcohol, phenoxyethanol, acrylates/C 10-30 alkyl acrylate crosspolymer, sodium hydroxide, citric acid for lotions or water, petrolatum, glyceryl polymethacrylate, dicaprylyl ether, glycerin, dimethicone, glyceryl stearate, cetyl alcohol, primus amygdalus dulcis (sweet almond) oil, PEG-30 glyceryl stearate, tocopheryl acetate, benzyl alcohol, phenoxyethanol, sodium hydroxide, acrylates/C 10-30 alkyl acryl
  • a preferred vehicle is Cetaphil®.
  • Other agents which can be employed in the present application in the dermatologically acceptable vehicle include fibroblast growth factor (e.g. basic fibroblast growth factor, fibroblast growth factor 2); acetyl hexapeptide, tromethamine, glutathione peroxidase, grapefruit, glycolic acid, heparin sulfate, acetyl hexapeptide, tromethamine, glycolic acid, sphingoid and phospholipid derivatives (e.g. ceramides, phytosphingosine, sphingosine, pseudoceramides, phospholipids, lysophospholipids); antioxidants (e.g. glutathione) and vitamins [e.g.
  • tocopherol and derivatives ascorbic acid and derivatives, niacinamide and derivatives, vitamin complexes, alpha-lipoic acid, retinol and derivatives, panthenol, vitamin C (including vitamin C derivatives), vitamin E; antiinflammatories (e.g. bisabolol, allantoin, phytantriol), Coenzyme Q10, Idebenone; botanical agents such as polyphenolics, flavonoids or isoflavones]; moisturizing agents (e.g.
  • the cosmeceutically effective amount of a PPAR agonist that is used in the cosmeceutically acceptable composition has a concentration of about 0.5% to 0.0001% PPAR agonist preferably from about 0.1% to 0.0005%, and most preferably about 0.05% to 0.005%.
  • the cosmeceutically effective amount of a PPAR agonist is partially dependent on the cells or the individual being treated and higher concentrations may be necessary to achieve desired results, in addition higher concentrations may result in increased side effects.
  • the Formulation Table shows exemplary calculations for producing products of 0.01% and 0.005% PPAR agonist, similar calculations can be used to produce a cosmeceutically acceptable composition at the desired concentration.
  • the cosmeceutically effective amount of melatonin that is used in the cosmeceutically acceptable composition has a concentration of about 0.5% to 0.00001% melatonin. In one embodiment, the preferred melatonin concentration is about 0.3%. In another embodiment, the preferred melatonin concentration is about 0.0015%.
  • the cosmeceutically effective amount of melatonin is partially dependent on the cells or the individual being treated and higher concentrations may be necessary to achieve desired results, in addition higher concentrations may result in increased side effects.
  • the Formulation Table shows exemplary calculations for producing products of 0.1% and 0.5% melatonin, similar calculations can be used to produce a cosmeceutically acceptable composition at the desired concentration
  • the dermatologically acceptable vehicle will usually form from about 80% to about 99.999%, preferably from about 90% to about 99.995% and most preferably about 99.99% by weight of the composition, and can, in the absence of other cosmetic adjuncts, form the balance of the composition.
  • the troglitazone is maintained at a concentration of about 0.005% or 0.01% by weight in a cosmeceutically acceptable medium (e.g. about 10 gms of vehicle, with about 0.5mg or 1 mg troglitazone, respectively).
  • the melatonin is maintained at a concentration of about 0.03% by weight in a cosmeceutically acceptable medium.
  • melatonin is maintained at a concentration of about 0.15% by weight in a cosmeceutically acceptable medium in combination with troglitazone at a concentration of about 0.005% by weight.
  • vitamin C or vitamin E are also included in the compositions and are maintained at a therapeutically effective vitamin concentration of about 0.5% in a cosmeceutically acceptable medium.
  • the skin care formulations can be an aqueous solution, a water-in-oil (w/o) emulsion, an oil-in-water (o/w) emulsion, a dispersion of lipids, an aqueous, water-alcohol, oil or oil-alcohol gel, a solid stick, a wet-wipe or an aerosol.
  • w/o water-in-oil
  • o/w oil-in-water
  • a dispersion of lipids an aqueous, water-alcohol, oil or oil-alcohol gel, a solid stick, a wet-wipe or an aerosol.
  • the dermatologically acceptable vehicle itself is an (w/o) or (o/w) emulsion, it can contain 5 to 50% of an oilphase and 47 to 94.95% water, with respect to the weight of the whole formulation.
  • the topical composition according to the present invention, the usual manner for preparing skin care products may be employed.
  • the active components are generally incorporated in a dermatologically acceptable carrier in conventional manner.
  • the active components can suitably be dissolved or dispersed in a portion of the water or another solvent or liquid to be incorporated in the composition.
  • the preferred compositions are oil-in-water or water-in-oil emulsions.
  • the composition may be in the form of conventional skin-care products such as a cream, gel or lotion or the like.
  • the composition can also be in the form of a so-called "rinse-off' product, e.g., a bath or shower gel, possibly containing a delivery system for the actives to promote adherence to the skin during rinsing.
  • the product is a "leave-on” product; a product to be applied to the skin without a deliberate rinsing step soon after its application to the skin.
  • the composition can be formulated for night creams with a thicker delivery system or with variations in the amount of the PPAR agonist or melatonin for day creams formulated with less PPAR agonist or melatonin in a thinner delivery system.
  • the inventive composition may be packaged in any suitable manner such as in a jar, a bottle, tube, roll-ball, or the like, in the conventional manner.
  • the active ingredients described in the present invention may be applied one or more times daily to the portion of skin requiring treatment.
  • the improvement in skin appearance will usually become significantly visible by about two weeks, depending on the status of the initial skin condition, the concentration of the active components used in the composition, the volume of composition used and the frequency of application.
  • a small quantity, about 0.25 ml, of the composition is applied to the skin from a suitable container or applicator and spread over and/or rubbed into the skin using the hands or fingers or a suitable device.
  • the composition is formulated as a "leave-on" product and does not require any gloves or special applicators for effective use. Once applied to the skin in the affected area, the composition will begin to elicit the desired effect and promote lipid production.
  • keratinocytes treated with of 2.5 uM troglitazone for 48 hours show an increase in lipid production in the cells, evidenced by the lipid droplets stained with Oil Red O as compared to the absence and/or low prevalence of lipid droplets in the DMSO control.
  • Fig. 2 preadipocytes treated with of 1.1 uM troglitazone for about 48 hours show an increase in the lipid production (quantity and the size of lipid droplets) as evidenced by the lipid droplets stained with Oil Red O. Increases in lipid droplet after troglitazone treatment is also seen in Fig. 3.
  • Example 3 Anti Wrinkle Day Cream
  • Anti Spot formulation can diminish up to 90% of skin hyper pigmentation.
  • the integration of natural components such as pro antioxidants and activator factors found in human cells into the formulation allows cream to clarify birth marks, sun spots, age marks, hormonal induced hyperpigmentation and much more.
  • Perfetation's Anti Spot does not increase the risk of skin damage from sun exposure. Use twice a day applied directly to designated areas. The cream may oxidize and darken with time but will remain effective throughout use.
  • Reconstruction Night Cream regenerates tissue damage and substantially diminishes signs of age in only two weeks. Composition stimulates cells to enhance production of fundamental ingredients found in human cells that rejuvenate and maintain the healthy natural appearance of your skin. Reconstruction-Night Cream also stops the appearance of facial wrinkles. Apply every evening directly over clean skin. The cream may oxidize and darken with time but will remain effective throughout use.
  • a 0.1 mg/ul solution of Troglitazone is made in DMSO.
  • a 0.005% by weight composition an aliquot of 100 uls of the 0.1 mg/ul Troglitazone solution is added to 200 grams of lotion or cosmeceutically acceptable medium and mixed thoroughly.
  • a 0.0005% by weight composition an aliquot of 10 uls of a 0.1 mg/ul Troglitazone solution is added to 200 grams of lotion or cosmeceutically acceptable medium and mixed thoroughly. Additional concentrations can be made from a concentrated stock solution by methods known to one of ordinary skill in the art.
  • the cosmeceutical formulation (lotion) can be stored at ambient temperature for topical use on those areas of the skin wherein additional lipid production is desired.
  • a 0.1 mg/ul solution of Melatonin is made in DMSO. To make a 0.1% by weight composition, an aliquot of 100 uls of the stock solution is added to 200 grams of lotion or cosmeceutically acceptable medium and mixed thoroughly. Additional concentrations can be made from a concentrated stock solution by methods known to one of ordinary skill in the art. The cosmeceutical formulation (lotion) can be stored at ambient temperature for topical use on those areas of the skin wherein additional lipid production is desired. [0079] While the present invention has been described with respect to what is presently considered to be the preferred embodiments, it is to be understood that the invention is not limited to the disclosed embodiments. To the contrary, the invention is intended to cover various modifications and equivalent arrangements included within the spirit and scope of the appended claims. The scope of the following claims is to be accorded the broadest interpretation so as to encompass all such modifications and equivalent structures and functions.

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Abstract

La présente invention a pour objet des compositions et des méthodes pour le traitement des cellules, telles que les kératinocytes et les adipocytes, pour augmenter leur teneur lipidique, et des compositions et des méthodes pour le traitement des cellules cutanées pour diminuer l'aspect des imperfections.
EP10842740.2A 2009-12-21 2010-12-21 Compositions et méthodes pour l'augmentation de la graisse cellulaire et le blanchiment de la peau Withdrawn EP2515830A4 (fr)

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US28869509P 2009-12-21 2009-12-21
US28867709P 2009-12-21 2009-12-21
US31567210P 2010-03-19 2010-03-19
PCT/US2010/061659 WO2011084824A1 (fr) 2009-12-21 2010-12-21 Compositions et méthodes pour l'augmentation de la graisse cellulaire et le blanchiment de la peau

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EP2515830A1 true EP2515830A1 (fr) 2012-10-31
EP2515830A4 EP2515830A4 (fr) 2014-06-04

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JP2001261560A (ja) * 2000-01-13 2001-09-26 Sankyo Co Ltd トログリタゾンを含有する運動神経細胞の変性又は死の阻害剤
WO2002013812A1 (fr) * 2000-08-17 2002-02-21 Pershadsingh Harrihar A Traitements de maladies inflammatoires
WO2004073622A2 (fr) * 2003-02-17 2004-09-02 Smithkline Beecham Corporation Methode therapeutique et compositions destinees a une administration topique
WO2007099172A1 (fr) * 2006-03-03 2007-09-07 Mavi Sud S.R.L. Mélatonine et compositions à base de substances immunostimulantes

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