WO2008090489A2 - Cosmetic skincare use of iron gluconate combinations - Google Patents

Cosmetic skincare use of iron gluconate combinations Download PDF

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Publication number
WO2008090489A2
WO2008090489A2 PCT/IB2008/050131 IB2008050131W WO2008090489A2 WO 2008090489 A2 WO2008090489 A2 WO 2008090489A2 IB 2008050131 W IB2008050131 W IB 2008050131W WO 2008090489 A2 WO2008090489 A2 WO 2008090489A2
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Prior art keywords
skin
composition
potassium
silicon
iron gluconate
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PCT/IB2008/050131
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French (fr)
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WO2008090489A3 (en
Inventor
Alexandra Chastagner
Isabelle Besne
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L'oreal
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Publication of WO2008090489A3 publication Critical patent/WO2008090489A3/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365Hydroxycarboxylic acids; Ketocarboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4906Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
    • A61K8/4913Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/58Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing atoms other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur or phosphorus
    • A61K8/585Organosilicon compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/005Preparations for sensitive skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/08Anti-ageing preparations

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Emergency Medicine (AREA)
  • Gerontology & Geriatric Medicine (AREA)
  • Cosmetics (AREA)

Abstract

The present invention relates to the field of skincare and is more particularly directed toward proposing the cosmetic use of at least one combination of iron gluconate and of at least one compound comprising the element, especially the mineral element, chosen from potassium, silicon and sodium, especially for preventing and/or treating the signs of aging of the skin and the associated clinical signs.

Description

Cosmetic skincare use of iron gluconate combinations
The present invention relates to the field of skincare and is more particularly directed toward proposing the cosmetic use of a specific mixture comprising at least iron gluconate, for skincare. Human skin consists of three compartments, namely an upper compartment, the epidermis, the dermis and the hypodermis.
The hypodermis, which is the energy reservoir of the body, is essentially constituted of a type of cell specialized in accumulating and storing fats, the adipocytes.
As more particularly regards natural human epidermis, it is mainly composed of three types of cells: keratinocytes, which form the vast majority, melanocytes, and Langerhans cells. Each of these cell types contributes via its intrinsic functions toward the essential role played by the skin.
As regards the dermis, it gives the epidermis a solid support. It is also its nourishing factor. It is mainly constituted by fibroblasts and by an extracellular matrix, itself composed mainly of collagen, elastin and a substance known as ground substance, these components being synthesized by the fibroblasts. In normal skin, i.e. non- pathological and unscarred skin, the fibroblasts are in the quiescent state, i.e. nonproliferative.
Now, pronounced slowing-down of cell metabolism, especially of the energy metabolism of "aged" fibroblasts compared with fibroblasts qualified as being young, has been observed. This slowing-down of cell metabolism and especially of cell energy metabolism is reflected by the appearance of signs of aging of the skin, especially impairment in the biomechanical properties of the skin (loss of firmness, tonicity, elasticity, etc.), loss of luminosity, loss of radiance of the complexion, impairment in the surface aspect of the skin, and/or impairment in the grain of the skin.
The present invention is more specifically concerned with preventing and/or treating the signs of aging of the skin and the abovementioned clinical signs.
The inventors have thus discovered the beneficial effects of iron gluconate, especially in combination with at least one element, especially a mineral element chosen from potassium, silicon and sodium, on the metabolic activity of the skin, and in particular an effect on the production of cellular ATP. Thus, the main subject of the invention is a composition for topical application that is useful for caring for the skin, comprising, in a physiologically acceptable medium, at least one combination of iron gluconate and of at least one element, especially a mineral element chosen from potassium, silicon and sodium. The composition according to the invention and/or the combination of elements, especially of mineral elements, according to the invention is particularly suitable for preventing and/or treating skin disorders associated with a reduction in the cellular energy metabolism of the skin, and/or loss of luminosity, loss of radiance of the complexion and/or impairment in the surface aspect of the skin, impairment of the grain of the skin and/or impairment of the biomechanical properties of the skin, in particular induced by chronological aging, but also induced by photoaging.
For the purposes of the invention, the expression "cellular energy metabolism" is intended to cover all the intracellular chemical reactions that lead to the production of energy molecules such as ATP (adenosine triphosphate). These energy molecules enable the cell to perform the biochemical syntheses that participate toward its correct functioning, in particular for fibroblasts, matrix syntheses, proliferation and migration. As representative molecules capable of serving as substrates for this production of ATP, mention may be made of lipids, carbohydrates and proteins. Among the carbohydrates, mention may be made of glucose. Thus, the inventors have observed that iron gluconate, and in particular mixtures combining it with other elements, especially mineral elements, prove to be advantageous for maintaining and/or improving the cellular energy metabolism of the skin, glucose consumption, ATP production and, consequently, the synthesis of extracellular matrix and cell proliferation and/or migration. Thus, the stretchability, tonicity, firmness, suppleness and/or elasticity properties of the skin, the luminosity and/or radiance of the complexion, the surface aspect of the skin, and/or the grain of the skin are maintained and/or improved. The skin is firmed and regenerated. In parallel, the luminosity of the skin and/or the smooth aspect of the skin are improved.
According to one particular embodiment, the composition comprises iron gluconate, in combination with at least potassium. More particularly, the composition may comprise iron gluconate in combination with potassium and silicon, and in particular with potassium, silicon and sodium.
According to one particular embodiment, the invention relates to a composition in accordance with the invention comprising, besides iron gluconate, silicon in the form of a silanol derivative and more particularly in the form of methyl silanol mannuronate.
In general, the mineral elements combined with the iron gluconate are in an ionic form that can be assimilated by the skin.
According to another embodiment of the invention, the cosmetic composition is in any galenical form suitable for application to the skin, in particular in the form of an optionally gelled aqueous or aqueous-alcoholic solution, a dispersion of the lotion type, which may be a two-phase lotion, an oil-in-water, water-in-oil or multiple emulsion, an aqueous gel, a dispersion of oil in an aqueous phase with the aid of spherules, or alternatively a powder. Preferably, the cosmetic composition according to the invention is in the form of a water-in-oil solid emulsion.
A subject of the invention is also the use, especially the cosmetic use, of iron gluconate, especially in combination with at least one element, especially a mineral element chosen from potassium, silicon and sodium, as an active agent for maintaining and/or improving the cellular energy metabolism of the skin, for preventing and/or treating the signs of aging of the skin, and most particularly for preventing and/or treating impairment in luminosity, loss of radiance of the complexion, impairment of the surface aspect of the skin, and/or impairment of the grain of the skin and/or for maintaining and/or improving the bio mechanical properties of the skin, and/or for stimulating the energy mechanism of fibroblasts.
A subject of the invention is also the use, especially the cosmetic use, of iron gluconate, especially in combination with at least one element, especially a mineral element chosen from potassium, silicon and sodium, for the preparation of a composition for maintaining and/or improving cellular energy metabolism, for preventing and/or treating the signs of aging of the skin, for preventing and/or treating impairment in luminosity, loss of radiance of the complexion, impairment in the surface aspect of the skin and/or impairment in the grain of the skin and/or for maintaining and/or improving the bio mechanical properties of the skin, and/or for stimulating the energy mechanism of fibroblasts.
The invention is also directed toward a process for the cosmetic or therapeutic treatment of the skin, especially human skin, which is directed especially toward maintaining and/or improving cellular energy metabolism, preventing and/or treating the signs of aging, preventing and/or treating impairment in luminosity, loss of radiance of the complexion, impairment in the surface aspect of the skin and/or impairment in the grain of the skin and/or maintaining and/or improving the bio mechanical properties of the skin, comprising at least the application to the surface of said skin of a composition as defined previously.
Finally, the invention relates to iron gluconate in combination with at least one element, especially a mineral element chosen from potassium, silicon and sodium, for maintaining and/or improving the cellular energy metabolism of the skin.
In the context of the present invention, the expression "biomechanical properties of the skin" means the stretchability, tonicity, firmness, suppleness and/or elasticity properties of the skin.
The expression "signs of aging of the skin" means any change in the outer appearance of the skin caused by aging, whether it is chronobio logical and/or extrinsic aging, in particular photo-induced and/or hormone -related aging, for instance wrinkles and fine lines, wizened skin, flaccid skin, thinned skin, dull, lifeless skin, lack of elasticity and/or firmness and/or suppleness and/or tonicity of the skin, impairment in the surface aspect of the skin or impairment in the grain of the skin, but also any internal change in the skin that is not systematically reflected by a modified external appearance, for instance any internal degradation of the skin, particularly a decrease in cellular metabolism. This expression "signs of aging of the skin" is considered as being equivalent to the expression "skin disorders induced by chronological aging and/or extrinsic aging and/or hormone-related aging".
The compositions according to the invention may be cosmetic, pharmaceutical and/or dermatological compositions, and are more particularly cosmetic compositions. For the purposes of the present invention, a cosmetic composition denotes a composition that is capable of producing an esthetic and comfort effect on the skin, or alternatively that has a beauty purpose, for example for protecting it, keeping it in good condition, modifying its appearance, and especially enhancing its beauty. It may be in the form of a nutritional product and thus a product to be administered orally. Thus, the cosmetic use that is the subject of the present invention in its various embodiments may be implemented topically or orally. Similarly, it is understood in the context of the present invention that "cosmetic use" covers the use of products administered topically and/or orally, for producing an esthetic and comfort effect on the skin, or alternatively for beauty purposes, for example in order to protect it, keeping it in good condition or modify its appearance, and especially enhance its beauty. According to one variant of the invention, it is more particularly a composition intended for topical application.
Combination according to the invention
As stated previously, the compositions according to the invention contain at least iron gluconate.
The element iron is an element that is essential to the body. It forms part of the constitution of hemoglobin and thus participates in the transportation of oxygen in the blood. It is also present in several respiratory enzymes, for instance cytochrome oxidase, catalase or peroxidase. The inventors have noted that this element, especially combined with at least potassium, silicon and/or sodium can favorably act on the dermal matrix, by means of increased activation of cell metabolism and targeted action on the fibroblasts, with the effect especially of stimulating the consumption of glucose and the production of ATP.
Skin treated according to the invention is found to be softer, smoother, more dense, rebounding and luminous. The combinations under consideration according to the invention constitute per se a regenerating skincare treatment.
The inventors have also noted that the combination of iron gluconate and of silicon, more particularly in the form of a silanol derivative and even more particularly in the form of methyl silanol mannuronate, works synergistically on the synthesis of collagen III. As regards the other elements, especially the mineral elements, that may be combined with iron, they are also known as being important factors in the physiology of the human body.
In reality, potassium and sodium are introduced into the composition according to the present invention in the form of mineral elements. As regards silicon, it may be introduced in crystalline or soluble mineral form as outlined hereinbelow, but also in "organic" form, i.e. when said silicon is in the form of a derivative in which at least one of the covalent bonds of the silicon atom involves a carbon-based organic molecule, as also outlined hereinbelow. Potassium, the main cation of the intracellular sector, is the most abundant mineral in the human body after calcium and phosphorus. It intervenes especially in the mechanism of the sodium/potassium pump and promotes ion exchanges between the interior and the exterior of cells, thus participating in improving the osmotic balance of cells. As regards sodium, it intervenes in maintaining the acid-based equilibrium of the blood and also participates in maintaining the osmotic pressure and water regulation of the body by means of the sodium-potassium pump.
As regards silicon, it is, with iron and magnesium, the most abundant trace element in the human body. It is especially a constituent of the macromolecules of connective tissue (collagen, elastin, structure glycoprotein and proteoglycan). Via the formation of bridges, it participates in protecting these macromolecules and thus contributes toward the firmness and elasticity of the skin.
As regards the associated mineral elements featured in the compositions and considered in the uses according to the invention, they may be used in various forms. They may especially be in the form of an anhydrous or hydrated, mineral or organic salt or a chelated complex. The salts that may be suitable for use may be, for example, carbonates, bicarbonates, sulfates, phosphates, ascorbates, glycerophosphates, chlorides, nitrates, citrates, acetates, hydroxides, salts of α-hydroxy acids (citrate, tartrate, lactate, gluconate or malate) or of fruit acids, or alternatively salts of amino acids (aspartate, arginate or fumarate) or salts of fatty acids (palmitate, oleates, caseinate or behenate) or alternatively salts derived from pyrrolidonecarboxylic acid. As iron gluconate that may be used according to the invention, mention may be made especially of the product sold by the company SEPPIC under the name Givobio G FE®.
More particularly, the iron gluconate may be used in combination with a chelating agent, for instance pentasodium pentetate, also known as the pentasodium salt of diethylenetriaminepentaacetic acid.
By way of example of a pentasodium salt of diethylenetriaminepentaacetic acid, mention may be made especially of the product sold as an aqueous 40% solution under the name Dissolvine D 40® by the company Akzo Nobel. Specifically, the presence of such a chelating agent makes it possible to prevent the oxidation of iron II to iron III.
As regards potassium, it may be used in the form of a salt as mentioned above, and more particularly in the form of a potassium salt of L-pyrrolidonecarboxylic acid, also known as potassium-PCA, such as the product sold under the name Kalidone® by the company UCIB (Solabia).
As regards silicon, it is usually used:
- in the form of oxidized compounds: silica (Siθ2) and silicates. In this case silica and silicate are often, respectively, combined with other metallic components and bonded to various metal cations, - in the form of "organic" silicon. In this respect, mention is made of silanol
R3SiOH, silane diol R2Si(OH)2 and silane triol RSi(OH)3; the radical R generally being a methyl group. This organic silicon is naturally present in certain plants, and also at the surface of grains of sand where they may be formed from silica via the action of microorganisms. These organic derivatives are water-soluble. According to one particular embodiment of the invention, silicon is generally used in the form of a silicon derivative, more particularly of a silanol derivative, in particular of a silanol ester, more particularly in the form of methyl silanol mannuronate, especially such as Algisium C® (methylsilanol mannuronate as an aqueous 1% solution) sold by the company Exsymol. As regards sodium, it may be introduced in the form of one of the abovementioned solvents. More particularly, it is sodium lactate. Mention may be made especially of sodium lactate sold as an aqueous 60% solution under the name Arlacs by the company ADM.
In general, each of the abovementioned compounds may be present in a content ranging from 0.0001% to 10% by weight, preferably from 0.0005% to 5% by weight and even more preferably from 0.001% to 2% by weight relative to the total weight of the composition.
Advantageously, the iron gluconate optionally in combination with a chelating agent may be used in an iron/other mineral(s) weight ratio of at least 0.001, in particular ranging from 5 to 0.001, more particularly from 2 to 0.001 and especially from 0.05 to 0.001.
According to one embodiment of the invention, the iron gluconate is present in a proportion of at least 0.1 %o and may be combined with at least 0.5%o of potassium, at least 0.6%o of sodium and/or at least 0.0 l%o of silicon.
More particularly, the iron gluconate is used in chelated form.
Additional cosmetic active agents
According to one advantageous embodiment, the compositions according to the invention may also comprise one or more additional cosmetic active agents.
These active agents may be chosen from moisturizers, desquamating agents, agents for improving the barrier function, depigmenting agents, antioxidants, dermo- decontracting agents, anti-glycation agents, agents for stimulating the synthesis of dermal and/or epidermal macro molecules and/or for preventing their degradation, agents for stimulating fibroblast or keratinocyte proliferation and/or keratinocyte differentiation, agents for promoting the maturation of the horny envelope, NO-synthase inhibitors, peripheral benzodiazepine receptor (PBR) antagonists, agents for increasing the activity of the sebaceous glands, agents for stimulating the energy metabolism of cells, agents for promoting the capillary circulation of the skin around the eyes, and calmatives.
According to a first mode, the composition according to the invention comprises at least one moisturizer. According to another mode, the composition according to the invention comprises at least one desquamating agent. According to another mode, the composition according to the invention comprises at least one agent for improving the barrier function.
According to another mode, the composition according to the invention comprises at least one depigmenting agent. According to another mode, the composition according to the invention comprises at least one antioxidant.
According to another mode, the composition according to the invention comprises at least one dermo-decontracting agent.
According to another mode, the composition according to the invention comprises at least one anti-glycation agent.
According to another mode, the composition according to the invention comprises at least one agent for stimulating the synthesis of dermal and/or epidermal macro molecules and/or for preventing their degradation.
According to another mode, the composition according to the invention comprises at least one agent for stimulating fibroblast or keratinocyte proliferation and/or keratinocyte differentiation.
According to another mode, the composition according to the invention comprises at least one agent for promoting maturation of the horny envelope.
According to another mode, the composition according to the invention comprises at least one additional agent for stimulating the energy metabolism of cells.
According to another mode, the composition according to the invention comprises at least one agent for promoting the capillary circulation of the skin.
According to another mode, the composition according to the invention comprises at least one calmative and/or anti-irritant. Examples of such compounds are described below.
1. Moisturizers or humectants
Moisturizers or humectants that will especially be used include a moisturizer chosen from glycerol and derivatives thereof, urea and derivatives thereof, especially Hydro vance® sold by National Starch, hyaluronic acid, AHAs, BHAs, acrylic acid homopolymers, for instance Lipidure-HM® from NOF Corporation, beta-glucan from Mibelle-AG-Biochemistry; a mixture of passionflower oil, apricot oil, corn oil and rice bran oil sold by Nestle under the name NutraLipids®; a C-glycoside derivative such as those described in patent application WO 02/051 828 and in particular C-CC-D- xylopyranoside-2-hydroxypropane in the form of a solution containing 30% by weight of active material in a water/propylene glycol mixture (60/40% by weight) such as the product sold by Chimex under the trade name Mexoryl SBB®; an oil of musk rose sold by Nestle; an oil of the microalga Prophyridium cruentum enriched with zinc, sold by
Vincience under the name Algualane Zinc®; spheres of collagen and of chondroitin sulfate of marine of origin (Atelocollagen) sold by the company Engelhard Lyon under the name Marine Filling Spheres; hyaluronic acid spheres such as those sold by the company Engelhard Lyon; and arginine.
Preferred moisturizers that will be used include glycerol or a C-glycoside derivative such as those described in patent application WO 02/051 828 and in particular C-α-D-xylopyranoside-2-hydroxypropane in the form of a solution containing 30% by weight of active material in a water/propylene glycol mixture (60%/40% by weight), such as the product manufactured by Chimex under the trade name Mexoryl SBB®.
2. Desquamating agents
Mention may be made of β-hydroxy acids, such as 5-n-octanoylsalicylic acid; urea; glycolic acid, citric acid, lactic acid, tartaric acid, malic acid or mandelic acid; A-(I- hydroxyethyl)piperazine-l-propanesulfonic acid (HEPES); an extract of Sophora japonica; honey; N-acetyl glucosamine; sodium methyl glycine diacetate, and mixtures thereof.
Preferred desquamating agents that will be used are 5-n-octanoylsalicylic acid and 4-(2-hydroxyethyl)piperazine-l-propanesulfonic acid (HEPES).
3. Agents for improving the barrier function
As agents for improving the barrier function, mention may be made especially of arginine, an extract of Thermus thermophilics, an extract of wild yam (Dioscorea villosa) rhizome, an extract of yeast, an extract of chestnut, an extract of cedar buds, arginine, ceramides especially of type 3 (stearoyl-4-hydroxysphinganine as the INCI name) and type 5 (hydroxypalmitoyl sphinganine as the INCI name); and mixtures thereof. Preferred agents that will be used are ceramides, especially of type 3 (stearoyl- 4-hydroxysphinganine as the INCI name) and type 5 (hydroxypalmitoyl sphinganine as the INCI name).
4. Depigmenting agents
Depigmenting agents that may especially be mentioned include vitamin C and derivatives thereof and especially vitamin CG, CP and 3-0 ethyl vitamin C, alpha and beta arbutin, ferulic acid, kojic acid, resorcinol and derivatives thereof, calcium D-pantheteine sulfonate, lipoic acid, ellagic acid, vitamin B3, a kiwi fruit {Actinidia chinensis) juice sold by Gattefosse, an extract of Paeonia suffruticosa root, such as the product sold by the company Ichimaru Pharcos under the name Botanpi Liquid B®.
Preferred depigmenting agents that will be mentioned include vitamin C and derivatives thereof, and especially vitamins CG and CP.
5. Antioxidants
Mention may be made especially of tocopherol and esters thereof, in particular tocopheryl acetate; ascorbic acid and derivatives thereof, in particular magnesium ascorbyl phosphate and ascorbyl glucoside; ferulic acid; serine; ellagic acid, polyphenols, tannins, tannic acid, epigallocatechins and natural extracts containing them, anthocyans, rosemary extracts, olive leaf extracts, for instance those from the company Silab, green tea extracts, resveratrol and derivatives thereof, ergothioneine, N-acetylcysteine, an extract of the brown alga Pelvetia caniculata, for instance Pelvetiane® from Secma, chlorogenic acid, biotin, chelating agents, such as BHT and BHA, N,N'-bis(3,4,5-trimethoxy- benzyl)ethylenediamine and salts thereof; idebenone, plant extracts, for instance Pronalen Bioprotect TM from the company Provital; coenzyme QlO, bioflavonoids, SODs, phytanetriol, lignans, melatonin, pidolates, glutathione, caprylyl glycol, phloretin, a jasmine extract such as the product sold by Silab under the name Helisun®; hesperitin laurate such as Flavagrum PEG® from the company Engelhard Lyon; an extract of Paeonia suffruticosa root, such as the product sold by the company Ichimaru Pharcos under the name Botanpi Liquid B®.
Tocopheryl acetate and ascorbyl glucoside will preferably be used. 6. Dermo-relaxing or dermo-decontracting agents
Examples that may be mentioned include adenosine, manganese gluconate, wild yam, sea fennel, an extract of Acmella oleracea, for instance Gatuline® from Gattefosse, glycine and alverine. Adenosine will preferably be used.
7. Anti-gly cation agents
The term "anti-glycation agent" means a compound that prevents and/or reduces the glycation of skin proteins, in particular dermal proteins such as collagen. Mention may be made especially of extracts of plants of the Ericacea family, such as an extract of blueberry (Vaccinium angustifolium or Vaccinium myrtillus), for example the product sold under the name Blueberry Herbasol Extract PG by the company Cosmetochem, ergothioneine and derivatives thereof, and an extract of black tea, for instance Kombuchka® from Sederma, and mixtures thereof.
8. Agents for stimulating the synthesis of dermal and/or epidermal macro molecules and/or for preventing their degradation
As active agents for stimulating the synthesis of dermal and/or epidermal macro molecules and/or for preventing their degradation, mention may be made especially of: synthetic peptides such as iamin, biopeptide CL or palmitoyl oligopeptide sold by the company Sederma; peptides extracted from plants, such as the soybean hydrolyzate sold by the company Coletica under the trade name Phytokine®; rice peptides such as
Nutripeptide® from Silab, methylsilanol mannuronate such as Algisium C® sold by Exsymol; folic acid; and an extract of Medicago sativa (alfalfa) such as the product sold by
Silab under the name Vitanol®; a peptide extract of hazelnut such as the product sold by the company Solabia under the name Nuteline C®; arginine; an extract of Aphanizomenon flos-aquae (Cyanophyceae) sold under the name Lanablue® by Atrium Biotechnologies, the malt extract sold by the company Coletica under the trade name Collalift®; lycopene; an extract of lychee; an extract of moringa such as Arganyl LS 9781® from Cognis; an extract of Vaccinium myrtillus such as those described in patent application FR- A-2 814 950; retinol and derivatives, in particular retinyl palmitate; the extract of Saccharomyces cerevisiae sold by the company LSN under the trade name Cytovitin®; a peptide extract of hazelnut such as the product sold by the company Solabia under the trade name Nuteline
C®; {2-[acetyl(3-trifluoromethylphenyl)amino]-3-methylbutyrylamino}acetic acid, also known as N-[N-acetyl, N'-(3-trifluoromethyl)phenylvalyl]glycine, or N-acetyl-N-[3-
(trifluoromethyl) phenyl] valyl glycine or acetyl trifluoromethyl phenyl valylglycine, or an ester thereof with a Ci-C6 alcohol; an extract of rice peptides such as Colhibin® from
Pentapharm, or an extract of Phyllanthus emblica such as Emblica® from Rona; the extract of the brown alga Padina pavonica sold by the company Alban Mϋller under the trade name HSP3®; the Saccharomyces cerevisiae extract available especially from the company Silab under the trade name Firmalift® or from the company LSN under the trade name Cytovitin®; an extract of Laminaria ochroleuca such as Laminaine® from Secma; essence of Mamaku from Lucas Meyer; the extract of lupin sold by the company Silab under the trade name Structurine®; the extract of Fagus sylvatica beech buds sold by the company Gattefosse under the trade name Gatuline® RC; a C-glycoside derivative such as those described in patent application WO 02/051 828 and in particular C-CC-D- xylopyranoside-2-hydroxypropane in the form of a solution containing 30% by weight of active material in a water/propylene glycol mixture (60%/40% by weight) such as the product sold by Chimex under the trade name Mexoryl SBB®.
9. Agents for stimulating fibroblast or keratinocyte proliferation and/or keratinocyte differentiation
As agents for stimulating fibroblast or keratinocyte proliferation and/or keratinocyte differentiation, mention will be made especially of plant proteins or polypeptides, extracted especially from soybean (for example a soybean extract sold by the company LSN under the name Eleseryl SH-VEG 8® or sold by the company Silab under the trade name Raffermine®); an extract of hydro lyzed soybean proteins such as Ridulisse® from Silab; a peptide extract of hazelnut such as the product sold by the company Solabia under the name Nuteline C®; adenosine; phloroglucinol, a yeast extract such as Stimoderm® from CLR; a peptide extract of lupin, such as the product sold by the company Silab under the trade name Structurine® ; a water-soluble extract of corn, such as the product sold by the company So labia under the trade name Phytovityl®; a peptide extract of Voandzeia substerranea such as the product sold by the company Laboratoires
Serobiologiques under the trade name Filladyn LS 9397®; retinol and esters thereof, including retinyl palmitate.
10. Agents for promoting the maturation of the horny envelope
Agents that participate in the maturation of the horny envelope, which becomes impaired with age and induces a decrease in transglutaminase activity, may be used in the compositions of the invention. Examples that may be mentioned include urea and derivatives thereof and in particular Hydrovance® from National Starch and the other active agents mentioned in L'Oreal patent application FR 2 877 220 (unpublished).
11. Agents for stimulating the energy metabolism of cells The active agent for stimulating the energy metabolism of cells may be chosen, for example, from biotin, an extract of Saccharomyces cerevisiae such as Phosphovital® from Sederma, the mixture of sodium, manganese, zinc and magnesium salts of pyrrolidonecarboxylic acid, for instance Physiogenyl® from So labia, a mixture of zinc, copper and magnesium gluconate, such as Sepitonic M3® from SEPPIC, and mixtures thereof; a beta-glucan derived from Saccharomyces cerevisiae, such as the product sold by the company Mibelle AG Biochemistry.
12. Agents for promoting the cutaneous microcirculation
The active agent acting on the cutaneous microcirculation may be used for preventing dulling of the complexion. It may be chosen, for example, from the extract of bitter orange blossom (Remoduline® from Silab), extracts of Ruscus, of escin, of common horse chestnut, of ivy, of ginseng and of melilot, caffeine, nicotinate and derivatives thereof, an extract of black tea such as Kombuchka from Sederma; rutin salts; an extract of the alga Corallina officinalis, such as the product sold by Codif; and mixtures thereof. As preferred agents, mention will be made of caffeine, and extracts of Ruscus, of escin and of common horse chestnut. 13. Calmatives or anti- irritants
The term "calmative" means a compound that can reduce the sensation of stinging, itching or tautness of the skin. Mention will be made especially of: provitamin B5 or D-panthenol, β-glycyrrhetinic acid and salts or derivatives thereof (stearyl glycyrrhetate, 3-stearoyloxyglycyrrhetic acid or glycyrrhetinic acid monoglucuronide) and also plants containing them (e.g.: Glycyrrhiza glabra); ursolic acid and salts thereof; extracts of Centella asiatica, Canola oil, bisabolol; camomile extracts, allantoin; a mixture of water lily blossom extract and of palmitoylproline, such as the product sold under the name Seppicalm VG by the company SEPPIC, Aloe vera, rose
® water, an extract of mint, in particular of mint leaves, for instance Calmiskin from Silab, aniseed derivatives, filamentous bacteria, for instance Vitreoscilla filiformis as described in patent EP 761 204, an extract of rose petals, for instance Rose Flower Herbasol extract from the company Cosmetochem, shea butter, a fermented extract of Alteromonas sold under the name Abyssine® by the company Atrium Biotechnologies; spring water from the Vichy basin, such as waters originating from the Celestin, Chomel, Grande-Grille, Hόpital, Lucas and Pare sources, and preferably water from the Lucas source; an extract of Eperua falcata bark, such as the product sold by the company Cognis under the name Eperuline®; an extract of Paeonia suffruticosa root, such as the product sold by the company Ichimaru
Pharcos under the name Botanpi Liquid B®; extracts of peony, and mixtures thereof.
Preferred calmatives that will especially be mentioned include extracts of rose, extracts of mint, extracts of peony, an extract of Vitreoscilla filiformis, provitamin B5 or D-panthenol and β-glycyrrhetinic acid and salts or derivatives thereof. These additional active agents may be present in the composition in a content ranging from 0.001% to 20% by weight, preferably from 0.01% to 10% by weight and more preferentially from 0.01% to 5% by weight relative to the total weight of the composition. Physiologically acceptable medium
The composition according to the invention may be intended for cosmetic or pharmaceutical application, particularly dermatological application. Preferably, the composition according to the invention is intended for cosmetic application. As stated previously, the composition according to the invention may be administered orally according to a first variant, in which case it is in the form of a nutritional product, or topically according to a second variant, which is the preferred mode of administration according to the invention.
Thus, the composition according to the present invention is more particularly intended for topical application to the skin.
The physiologically acceptable medium is preferentially a cosmetically or dermato logically acceptable medium, i.e. a medium that is odorless, colorless or without any unpleasant appearance, and which does not cause any stinging, tautness or redness that is unacceptable to the user. The expression "physiologically acceptable medium" comprises a medium that is compatible with human keratin materials such as the skin, mucous membranes, the nails, the scalp and/or the hair.
The composition according to the invention may be in any galenical form normally used in cosmetics and dermatology. It may especially be in the form of an optionally gelled aqueous or aqueous- alcoholic solution, a dispersion of the lotion type, which may be a two-phase lotion, an oil- in-water, water-in-oil or multiple emulsion, an aqueous gel, a dispersion of oil in an aqueous phase with the aid of spherules, these spherules possibly being polymer nanoparticles such as nanospheres or nanocapsules, or, better still, lipid vesicles of ionic and/or nonionic type, or alternatively a powder.
Thus, the composition may comprise any constituent usually used in the envisioned application.
Mention may be made especially of water, solvents, oils of mineral, animal and/or plant origin especially as detailed hereinbelow, waxes as described hereinbelow, in particular pigments, fillers, surfactants, cosmetic or dermatological active agents, UV- screening agents, polymers, gelling agents and preserving agents. Needless to say, a person skilled in the art will take care to select this or these optional additional compound(s), and/or the amount thereof, such that the advantageous properties of the compounds according to the invention are not, or are not substantially, adversely affected by the envisioned addition. The compositions according to the invention advantageously contain at least one liquid fatty phase.
The compositions according to the invention may be in the form of emulsion compositions.
When the compositions are in anhydrous form, they may be in the form of liquids, soft pastes, sticks, compacted or cast products, or alternatively loose powders.
Advantageously, they may be in the form of emulsion.
The compositions according to the invention may advantageously be in the form of an emulsion obtained by dispersing an aqueous phase in a fatty phase (W/O) or a fatty phase in an aqueous phase (O/W), of liquid or semiliquid consistency of the milk type, or of soft, semisolid or solid consistency of the cream or gel type, or alternatively in the form of a multiple emulsion (W/O/W or 0/W/O). These compositions are prepared according to the usual methods.
The compositions of this type may have the form of a care or makeup product for the face and/or the body, and may be conditioned, for example, in the form of a cream in a jar or of a fluid in a tube or in a pump-dispenser bottle.
The emulsions generally contain at least one emulsifier chosen from amphoteric, anionic, cationic and nonionic emulsifϊers, used alone or as a mixture. The emulsifϊers are chosen in a suitable manner according to the emulsion to be obtained (W/O or O/W). The emulsifϊers are generally present in the composition in a proportion that may range, for example, from 0.3% to 30% by weight and preferably from 0.5% to 20% by weight relative to the total weight of the composition.
For the O/W emulsions, examples of emulsifiers that may be mentioned include nonionic surfactants, and especially polyol esters of fatty acids with a saturated or unsaturated chain containing, for example, from 8 to 24 carbon atoms and better still from 12 to 22 carbon atoms, and oxyalkylene derivatives thereof, i.e. derivatives comprising oxyethylene and/or oxypropylene units, such as glyceryl esters of Cs-C24 fatty acids, and the oxyalkylene derivatives thereof; polyethylene glycol esters of Cs-C24 fatty acids, and the oxyalkylene derivatives thereof; sorbitol esters of Cs-C24 fatty acids, and the oxyalkylene derivatives thereof; sugar (sucrose, glucose or alkylglucose) esters of Cs-C24 fatty acids and the oxyalkylene derivatives thereof; esters of fatty alcohols; esters of sugar and Cs-C24 fatty alcohols, and mixtures thereof. As examples of oils that may be used in the composition of the invention, mention may be made of:
- hydrocarbon-based oils of animal origin, such as perhydrosqualene;
- hydrocarbon-based oils of plant origin, such as liquid triglycerides of fatty acids of 4 to 10 carbon atoms, such as heptanoic or octanoic acid triglycerides or alternatively, for example, sunflower oil, corn oil, soybean oil, marrow oil, grapeseed oil, sesame seed oil, hazelnut oil, apricot oil, macadamia oil, arara oil, sunflower oil, castor oil, avocado oil, caprylic/capric acid triglycerides such as those sold by the company Stearineries Dubois or those sold under the names Miglyol 810, 812 and 818 by the company Dynamit Nobel, jojoba oil or shea butter oil; - synthetic esters and ethers in particular of fatty acids, such as the oils of formulae RiCOOR2 and RiOR2 in which Ri represents a fatty acid residue containing from 8 to 29 carbon atoms and R2 represents a branched or unbranched hydrocarbon-based chain containing from 3 to 30 carbon atoms, such as, for example, purcellin oil, isononyl isononanoate, isopropyl myristate, 2-ethylhexyl palmitate, 2-octyldodecyl stearate, 2-octyldodecyl erucate or isostearyl isostearate; hydroxylated esters such as isostearyl lactate, octyl hydroxystearate, octyldodecyl hydroxystearate, diisostearyl malate, triisocetyl citrate, and fatty alcohol heptanoates, octanoates and decanoates; polyol esters such as propylene glycol dioctanoate, neopentyl glycol diheptanoate and diethylene glycol diisononanoate; and pentaerythritol esters such as pentaerythrityl tetraisostearate; - linear or branched hydrocarbons of mineral or synthetic origin, such as volatile or nonvolatile liquid paraffins and derivatives thereof, isohexadecane, isododecane, petroleum jelly, polydecenes or hydrogenated polyisobutene such as Parleam
® oil ;
- natural or synthetic essential oils such as, for example, eucalyptus oil, lavandin oil, lavender oil, vetiver oil, Litsea cubeba oil, lemon oil, sandalwood oil, rosemary oil, camomile oil, savory oil, nutmeg oil, cinnamon oil, hyssop oil, caraway oil, orange oil, geraniol oil, cade oil and bergamot oil; - fatty alcohols containing from 8 to 26 carbon atoms, such as cetyl alcohol, stearyl alcohol, and the mixture thereof (cetylstearyl alcohol), octyldodecanol, 2-butyloctanol, 2-hexyldecanol, 2-undecylpentadecanol, oleyl alcohol or linoleyl alcohol;
- partially hydrocarbon-based and/or silicone-based fluoro oils such as those described in document JP-A-2-295 912;
- silicone oils such as volatile or nonvolatile polydimethylsiloxanes (PDMSs) containing a linear or cyclic silicone chain, which are liquid or pasty at room temperature, in particular cyclopolydimethylsiloxanes (cyclomethicones) such as cyclohexasiloxane; polydimethylsiloxanes comprising alkyl, alkoxy or phenyl groups, pendant or at the end of a silicone chain, these groups containing from 2 to 24 carbon atoms; phenylsilicones such as phenyl trimethicones, phenyl dimethicones, phenyltrimethylsiloxydiphenylsiloxanes, diphenyl dimethicones, diphenylmethyldiphenyltrisiloxanes, 2-phenylethyl trimethylsiloxy silicates and polymethylphenylsiloxanes;
- mixtures thereof. The term "hydrocarbon-based oil" in the list of oils mentioned above means any oil predominantly comprising carbon and hydrogen atoms, and optionally ester, ether, fluoro, carboxylic acid and/or alcohol groups.
The other fatty substances that may be present in the oily phase are, for example, fatty acids containing from 8 to 30 carbon atoms, for instance stearic acid, lauric acid, palmitic acid and oleic acid.
As waxes that may be used according to the invention, mention may be made of waxes of animal origin such as beeswax, spermaceti, lanolin wax and lanolin derivatives, plant waxes such as carnauba wax, candelilla wax, ouricury wax, Japan wax, cocoa butter, cork fiber wax or sugarcane wax, mineral waxes, for example paraffin wax, petroleum jelly wax, lignite wax or microcrystalline waxes or ozokerites, synthetic waxes, among which are polyethylene wax, polytetrafluoroethylene wax and the waxes obtained by Fisher-Tropsch synthesis, or silicone waxes, hydrogenated oils that are solid at 25°C, such as hydrogenated castor oil, hydrogenated jojoba oil, hydrogenated palm oil, hydrogenated tallow and hydrogenated coconut oil, and fatty esters that are solid at 25°C, for instance the C20-C40 alkyl stearate sold under the trade name Kester Wax K82H by the company Koster Keunen. These fatty substances may be chosen in a varied manner by a person skilled in the art in order to prepare compositions having the desired properties, for example in terms of consistency or texture.
The compositions according to the invention may comprise a volatile oil. For the purposes of the invention, the term "volatile oil" means an oil that is capable of evaporating on contact with keratin materials in less than one hour, at room temperature and atmospheric pressure. The volatile organic solvent(s) and volatile oils of the invention are volatile organic solvents and volatile cosmetic oils that are liquid at room temperature, with a nonzero vapor pressure, at room temperature and atmospheric pressure, ranging in particular from 0.13 Pa to 40 000 Pa (10~3 to 300 mmHg), in particular ranging from 1.3 Pa to 13 000 Pa (0.01 to 100 mmHg) and more particularly ranging from 1.3 Pa to 1300 Pa (0.01 to 10 mmHg).
Volatile oils that may be mentioned, inter alia, include cyclic or linear silicones containing from 2 to 6 silicon atoms, such as cyclohexasiloxane, dodecamethylpentasiloxane, decamethyltetrasiloxane, butyl trisiloxane and ethyl trisiloxane. It is also possible to use branched hydrocarbons, for instance isododecane, and also volatile perfluoroalkanes such as dodecafluoropentane and tetradecafluorohexane, sold under the names PF 5050® and PF 5060® by the company 3M, and perfluoro morpholine derivatives, such as 4-trifluoromethylperfluoromorpholine sold under the name PF 5052® by the company 3M.
The amount of oily phase present in the compositions according to the invention may range, for example, from 0.01% to 50% by weight and preferably from 0.1% to 30% by weight relative to the total weight of the composition.
The compositions according to the invention may also comprise at least one dyestuff chosen, for example, from pigments, nacres, dyes and materials with an effect, and mixtures thereof.
These dyestuffs may be present in a content ranging from 0.01% to 50% by weight and preferably from 0.01% to 30% by weight relative to the total weight of the composition. The compositions according to the invention may also comprise a filler especially in a content ranging from 0.01% to 50% by weight and preferably ranging from 0.01% to 30% by weight relative to the total weight of the composition. These fillers may be mineral or organic and of any form, platelet-shaped, spherical or oblong, irrespective of the crystallographic form (for example lamellar, cubic, hexagonal, orthorhombic or amorphous). Mention may be made of silica, talc, mica, kaolin, lauroyllysine, starch, boron nitride, PTFE powders, PMMA powders, methylsilsesquioxane resin powders (for instance Tospearl 145A from GE Silicone), hollow hemispherical silicone resin particles (for instance NLK 500, NLK 506 and NLK 510 from Takemoto Oil and Fat), barium sulfate, precipitated calcium carbonate, magnesium carbonate, magnesium hydrogen carbonate, hydroxyapatite, glass or ceramic microcapsules, and metal soaps derived from organic carboxylic acids containing from 8 to 22 carbon atoms and preferably from 12 to 18 carbon atoms, for example zinc stearate, magnesium stearate or lithium stearate, zinc laurate or magnesium myristate.
The composition according to the invention may also contain various adjuvants commonly used in cosmetics, such as sequestrants; fragrances; and thickeners and gelling agents. The amounts of these various adjuvants and the nature thereof will be chosen such that they do not harm the properties of the composition.
Advantageously, the composition according to the invention may be in the form of a water-in-oil solid emulsion.
More particularly, it is a water-in-oil solid emulsion containing a particular silicone surfactant of the alkyl dimethicone copolyol type, in combination with at least one oil and at least one wax. The corresponding water-in-oil solid emulsions have the advantage of not transferring.
The silicone surfactant of the alkyl dimethicone copolyol type may especially be chosen from the compounds sold under the following names:
- Abil WE 09, Abil WS 08 and Abil EM 90 by the company Goldschmidt, - Q2 5200 by the company Dow Corning, and
- 218- 1138 by the company General Electric.
The product Abil WE 09, which is a mixture of cetyldimethicone copolyol (CTFA name), polyglyceryl-4 isostearate and hexyl laurate (33.3%/33.3%/33.4%), is preferably used. The alkyl dimethicone copolyol silicone surfactant is used in a proportion of from 0.5% to 40% by weight and preferably in a proportion of from 2% to 12% by weight relative to the total weight of the emulsion. The fatty phase of the solid emulsion according to the invention comprises at least one oil and at least one wax.
The emulsion according to the invention may comprise 10% to 40% by weight and preferably 18% to 30% by weight of at least one oil, relative to the total weight of the emulsion.
The emulsion according to the invention preferably comprises at least one silicone oil.
As examples of silicone oils used in the invention, mention may be made of:
- cyclic volatile silicones containing from 3 to 8 and preferably 4 to 6 silicon atoms, for instance cyclotetradimethylsiloxane, cyclopentadimethylsiloxane or cyclohexadimethylsiloxane;
- cyclocopolymers of the dimethylsiloxane/methylalkylsiloxane type, such as Silicone FZ 3109 sold by the company Union Carbide, which is a dimethylsiloxane/methyloctylsiloxane eye Io copolymer; - linear volatile silicones containing from 2 to 9 silicon atoms, for example hexamethyldisiloxane, hexylheptamethyltrisiloxane and octylheptamethyltrisiloxane;
- polyalkylsiloxanes containing trimethylsilyl end groups, preferably those whose viscosity at 25°C is less than or equal to 0.06 m2/s, among which mention may be made of linear polydimethylsiloxanes, and especially those sold under the name Dow Corning Fluid 200 by the company Dow Corning, and alky lmethylpo Iy silo xanes such as cetyldimethicone (CTFA name);
- phenylsilicone oils.
Volatile silicone oils are preferably used in the invention. As volatile oils preferentially used according to the invention, mention may also be made of hydrocarbon-based oils containing from 8 to 16 carbon atoms, and especially volatile Cs-Ci6 isoparaffinic oils, for instance isododecane, isodecane and isohexadecane.
The emulsion according to the invention may also contain other oils and pasty fatty substances especially as defined previously. This composition may be more or less fluid and may have the appearance of a white or colored cream, an ointment, a milk, a lotion, a serum, a paste or a mousse. It may optionally be applied to the skin in aerosol form. It may also be in solid form, for example in the form of a stick.
The examples that follow serve to illustrate the invention without, however, being limiting in nature. Depending on the case, the compounds are cited as the chemical names or as the CTFA names (International Cosmetic Ingredient Dictionary and Handbook).
EXAMPLE 1:
In vitro demonstration of the stimulatory activity of a mixture in accordance with the invention on the cellular energy metabolism of aged fibroblasts
To demonstrate the activity of a composition in accordance with the invention, the cellular energy metabolism was selected. A model of aged human fibroblasts in culture was selected, on which two parameters having an influence on metabolism were evaluated: glucose consumption and intracellular ATP content. Correlating an increase in glucose with an increase in the amount of intracellular ATP makes it possible to circumvent the possibility of the increase in this amount of ATP being in fact associated with a reduction in its use.
The aged fibroblasts are matured by successive passages (18 passages) and compared, for basal activity, with younger fibroblasts, i.e. fibroblasts with a lower number of passages (8 passages).
1- Protocol
The activity of the active agents alone was evaluated at the following concentrations (percentages given as active material):
Concentration 1 Concentration 2 |
Figure imgf000024_0001
A mixture in accordance with the invention is evaluated at the following active agent concentrations (percentages given as active material):
Figure imgf000025_0001
a) Assay of the consumed glucose
The fibroblasts are inoculated on 96-well plates at a rate of 8500 fibroblasts/well. The fibroblasts are maintained for 24 hours at 37°C and 5% CO2 in a normal culture medium (DMEM, L-glutamine 2 mM, penicillin/streptomycin
50 IU/ml/50 μg/ml, 10% fetal calf serum). The medium is then removed and replaced with medium containing or not containing the test mixture.
The glucose assay takes place after 24 hours. An untreated young fibroblast control was performed in parallel. The glucose was assayed via the colorimetric method with o-toluidine (Sigma Tl 199).
The viability of the cell lawn at the end of the experiment was evaluated via the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) reduction colorimetric test.
b) Evaluation of the intracellular ATP
The aged fibroblasts are precultured in normal medium (DMEM containing 10% FCS at 37°C and 5% CO2) and then cultured in medium depleted in fetal calf serum and enriched in glucose (DMEM containing 1 g/1 of glucose and 1% FCS). After incubation, the culture medium is removed and replaced with medium containing or not containing the test mixture. The cells were then incubated at 37°C for 2 hours. An untreated young fibroblast control was performed in parallel. After incubation, the medium was removed and the cell lawns frozen at -200C.
The ATP was then extracted with Tris 100 mM/EDTA 4 mM, pH 7.75.
The ATP assay is then performed using a specific kit (ATP Biolum, Roche 11699695) according to the supplier's indications.
2- Results a. Glucose consumption
Figure imgf000026_0001
ND: not determined
The addition of insulin at 10 μg/ml (positive control) to the medium significantly stimulated the glucose consumption by the aged fibroblasts, and represents 140% after 24 hours. This result validates the test.
Sodium lactate tested at 1.2% and 0.24% markedly slowed down the glucose consumption.
Potassium PCA tested at 1% did not significantly modify the glucose consumption of the aged fibroblasts.
Silicon mannuronate tested at 0.1% and 0.02% did not significantly modify the glucose consumption of the aged fibroblasts. Iron gluconate tested at 0.04% had a tendency to stimulate the glucose consumption by the aged fibroblasts.
Figure imgf000027_0001
* : statistically significant difference relative to the control medium ND: not determined
It is noted that the young fibroblasts with a lower number of passages show lower glucose consumption than the aged fibroblasts. This result has already been demonstrated on this type of cell culture in which the fibroblasts are mature by successive passages (Goldstein S. et al., J. Cell Physiol. 1982, 112 (3), 419-424).
Mixture Ml representative of a combination in accordance with the invention has a significant stimulatory effect on glucose consumption at 24 hours, and a synergistic effect relative to the results of the four active agents taken individually.
b. Evaluation of the amount of intracellular ATP
Figure imgf000027_0002
statistically significant difference relative to the control medium
It is noted that the level of intracellular ATP is greatly reduced with age: the
ATP concentration in the aged fibroblasts after 2 hours of treatment was 0.059 μM, whereas in the young fibroblasts, this level of intracellular ATP was significantly higher (310% of the control after 2 hours).
Treatment with the mixture at the higher concentrations (Ml) significantly increased the amount of ATP in the cells (194% after 2 hours).
These results as a whole show that iron gluconate, especially in combination with potassium PCA, sodium lactate and silicon mannuronate, stimulates the energy metabolism of fibroblasts, by stimulating the glucose consumption and the cellular ATP production of the aged fibroblasts. This combination of minerals is provided for the benefit of regenerating and anti-aging compositions intended for maintaining and/or improving the cellular energy metabolism of the skin, for preventing and/or treating the signs of aging of the skin, and most particularly for preventing and/or treating cutaneous signs associated with impairment in luminosity, loss of radiance of the complexion, impairment of the surface aspect of the skin, and/or impairment in the grain of the skin and/or for maintaining and/or improving the bio mechanical properties of the skin.
EXAMPLE 2 Demonstration of the effect of a combination of iron gluconate with a silanol derivative (silicon) on collagen III
Protocol:
- normal human dermal fibroblasts are inoculated in 10% or 1% FCS (fetal calf serum) medium and incubated to the point of confluence,
- the products, i.e. the mixture and the controls, are tested in suitable formats, for 24 hours.
The following are then performed:
- TGFβ is used as reference, - the mRNA is extracted. The RNAs are prepared from a pool of two cultural wells.
- the cDNAs are quantified by reverse transcription, and
- a 1st series of Q-PCRs is performed on the marker G3PDH to confirm the homogeneity of the preparations to be compared. The Q-PCR is carried out in triplicate using pairs of specific primers of the sequence of the G3PDH (reference markers) and of the sequence of the selected markers; i.e. the sub-units validated by collagen III (COL 3). The differential expressions relative or not relative to G3PDH are quantified. Results: expression of collagen III by RT-PCR. The table below collates the test results:
Figure imgf000029_0001
The results are expressed as percentages relative to the control.
The percentages of Algisium C® are indicated as weight of Active Material.
Under the experimental conditions of this study, the reference TGF-β at 10 ng/ml does not modify the expression of the gene coding for collagen III relative to the control (tendency towards increase).
Iron gluconate, at the two concentrations tested, does not show any marked difference with the control regarding the expression of the various collagens.
Algisium C® does not show any marked difference with the control regarding the expression of the various collagens. However, a slight tendency at a concentration of 1% to increase the expression of collagen III (+ 50%) relative to the control is noted.
Treatment of fibroblasts with the combination of the two active agents makes it possible to observe a strong tendency towards increasing the synthesis of collagen III (+92% for Ml and +96% for M2 relative to the control).
Conclusion:
On fibroblasts, it has been demonstrated under the experimental conditions of this study that the treatments with iron gluconate alone or with Algisium C® alone have no marked effect on the expression of collagen III (slight tendency towards increasing the expression of collagen III at a concentration of 1% with Algisium C®). EXAMPLE 3
Composition for topical application of W/O emulsion type
Amounts are expressed as percentages relative to the total weight of the composition
AM = active material
PHASE H - Paraffin wax 5
- Preserving agent 0.1
- Polyethylene wax 1.3
- Isohexadecane 6
- Silica 2 - Dimethicone 5 cSt 8
- Octyldodecanol 1
PHASE E
- Mixture of oxyethylenated oxypropylenated poly methylcetyl dimethyl methyl-siloxane, polyglycerol- ated isostearate (4 mol) and hexyl laurate, sold under the name Abil WE 09 by the company Goldschmidt 9
- Nylon powder 2
- Sodium lactate as an aqueous 60% solution sold under the name Arlacs by the company ADM 1
(i.e. 0.6% AM)
- Potassium PCA sold under the name Kalidone® by the company UCIB (Solabia) 1
(i.e. 0.5% AM) - Methylsilanol mannuronate (methylsilanol mannuronate as an aqueous 1% solution) 1
(i.e. 0.01% AM) - Iron gluconate sold by the company SEPPIC under the name Givobio G FE® 0.01
(i.e. 0.01% AM)
- DTPA sold under the name Dissolvine D 40® by the company Akzo Nobel 0.048
(containing 0.02% AM)
- Glycerol 5
- Preserving agent 1
- Sterilized demineralized water qs 100
The composition was prepared according to the following procedure:
The mixture comprising the waxes and the nonvolatile oils is heated to 900C until a clear, uniform mixture is obtained; the volatile oils are then added with stirring at
700C. The mixture of ingredients of the aqueous phase is then prepared by heating to 85°C, and the aqueous phase is then introduced at 85°C into the oily phase, with stirring until the water-in-oil emulsion is obtained.
The emulsion is poured at 65-67°C into a preheated dish and is then allowed to cool to room temperature until the solid emulsion is obtained.
A solid skincare cream with a uniform texture, which applies easily to the skin, is obtained.
Daily application of this skincare cream makes it possible to obtain an overall regenerating and anti-aging effect reflected by a more uniform skin grain and softer, smoother, more supple skin. The skin appears to be regenerated and more tonic, and the wrinkles reduced.
EXAMPLE 4
Other formulations
Eye contour gel - Sodium lactate as an aqueous 60% solution sold under the name Arlacs by the company ADM 0.1 (0.06% AM)
- Potassium PCA sold under the name Kalidone® by the company UCIB (Solabia) 0.1 (0.05% AM) - Methylsilanol mannuronate (methylsilanol mannuronate as an aqueous 1 % solution) 0.1 (0.001 % AM)
- Iron gluconate sold by the company SEPPIC under the name Givobio G FE® 0.01 (0.01% AM) - DTPA sold under the name Dissolvine D 40® by the company Akzo Nobel 0.048 (0.02% AM)
- Escin 0.2
- Glycerol 3
- Propylene glycol 1 - Carbomer 0.6
- Xanthan gum 0.2
- Preserving agents 0.10
- Water qs 100
Calmative lotion
- Sodium lactate as an aqueous 60% solution sold under the name Arlacs by the company ADM 0.1 (0.06% AM)
- Potassium PCA sold under the name Kalidone® by the company UCIB (Solabia) 0.1 (0.05% AM) - Methylsilanol mannuronate (methylsilanol mannuronate as an aqueous 1% solution) 0.1 (0.001% AM)
- Iron gluconate which may be used according to the invention; mention may be made in particular of that sold by the company SEPPIC under the name Givobio G FE® 0.01 (0.01% AM) - DTPA sold under the name Dissolvine D 40® by the company Akzo Nobel 0.048 (0.02% AM)
- Rose extract 0.05
- Solvents 5
- Glycerol 5 - Surfactants 1
- Preserving agents 0.10
- Water qs 100

Claims

1. A composition for topical application, that is useful for caring for the skin, comprising, in a physiologically acceptable medium, at least one combination of iron gluconate and of at least one element, especially a mineral element chosen from potassium, silicon and sodium.
2. The composition as claimed in claim 1, in which the iron gluconate is combined with at least potassium.
3. The composition as claimed in claim 1 or 2, in which the iron gluconate is combined with at least potassium and silicon.
4. The composition as claimed in claim 1, in which the iron gluconate is combined with at least one silicon element in the form of a silanol derivative.
5. The composition as claimed in the preceding claim, in which the silanol derivative is methylsilanol mannuronate.
6. The composition as claimed in any one of the claims, comprising at least one combination of iron gluconate and of at least potassium, silicon and sodium.
7. The composition as claimed in any one of the preceding claims, also comprising an iron-chelating agent.
8. The composition as claimed in any one of claims 1 to 3, 6 and 7, in which combined mineral elements, potassium and sodium, are in ionic form.
9. The composition as claimed in any one of the preceding claims, combining iron gluconate with at least sodium lactate, potassium PCA, methyl silanol mannuronate and DTPA.
10. The composition as claimed in any one of the preceding claims, in which the elements forming said combination are present, respectively, in a proportion of from
0.0001% to 1% by weight, preferably from 0.0005% to 5% by weight and even more preferably from 0.001% to 2% by weight relative to the total weight of the composition.
11. The composition as claimed in any one of the preceding claims, in which the iron gluconate is present in a proportion of at least 0.1 %o and is combined with at least 0.5%o of potassium, at least 0.6%o of sodium and/or at least 0.0 l%o of silicon.
12. The composition as claimed in any one of the preceding claims, which is in the form of an optionally gelled aqueous or aqueous-alcoholic solution, a dispersion of the lotion type, which may be a two-phase lotion, an oil-in-water, water-in-oil or multiple emulsion, an aqueous gel, a dispersion of oil in an aqueous phase with the aid of spherules, or alternatively a powder.
13. The composition as claimed in the preceding claim, characterized in that the composition is in the form of a water-in-oil solid emulsion.
14. The composition as claimed in the preceding claim, in which said emulsion contains a surfactant of the alkyldimethicone copolyol type in combination with at least one oil and at least one wax.
15. The cosmetic use of iron gluconate in combination with at least one mineral element chosen from potassium, silicon and sodium, as an active agent for maintaining and/or improving the cellular energy metabolism of the skin.
16. The cosmetic use of iron gluconate in combination with at least one element, especially a mineral element chosen from potassium, silicon and sodium, as an active agent for maintaining and/or improving the biomechanical properties of the skin.
17. The cosmetic use of iron gluconate in combination with at least one element, especially a mineral element chosen from potassium, silicon and sodium, as an active agent for preventing and/or treating the signs of aging of the skin.
18. The cosmetic use of iron gluconate in combination with at least one element, especially a mineral element chosen from potassium, silicon and sodium, as an active agent for preventing and/or treating impairment in luminosity and/or loss of radiance of the complexion.
19. The cosmetic use of iron gluconate in combination with at least one element, especially a mineral element chosen from potassium, silicon and sodium, as an active agent for preventing and/or treating an impairment in the surface aspect of the skin and/or impairment in the grain of the skin.
20. The cosmetic use of iron gluconate in combination with at least one element, especially a mineral element chosen from potassium, silicon and sodium, as an active agent for stimulating the energy metabolism of fibroblasts.
21. Iron gluconate in combination with at least one element, especially a mineral element chosen from potassium, silicon and sodium, for maintaining and/or improving the cellular energy metabolism of the skin.
22. The use as claimed in any one of claims 15 to 21, in which the iron gluconate is used in the form of the composition as defined in claims 1 to 14.
23. A cosmetic skin treatment process comprising at least the application to the surface of said skin of a composition as defined according to any one of claims 1 to 14.
24. The process as claimed in the preceding claim, characterized in that it is directed toward maintaining and/or improving cellular energy metabolism, preventing and/or treating the signs of aging of the skin, preventing and/or treating impairment in luminosity, loss of radiance of the complexion, impairment of the surface appearance of the skin and/or impairment in the grain of the skin and/or maintaining and/or improving the bio mechanical properties of the skin.
PCT/IB2008/050131 2007-01-23 2008-01-15 Cosmetic skincare use of iron gluconate combinations WO2008090489A2 (en)

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Application Number Priority Date Filing Date Title
FR0752839A FR2911495B1 (en) 2007-01-23 2007-01-23 COSMETIC USE OF IRON ASSOCIATIONS FOR SKIN CARE.
FR0752839 2007-01-23
US88934807P 2007-02-12 2007-02-12
US60/889,348 2007-02-12

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CN109106685A (en) * 2018-08-08 2019-01-01 浙江工业大学 A kind of embedding insulin multiple emulsion and its preparation and application
CN110974716A (en) * 2019-12-31 2020-04-10 华熙生物科技股份有限公司 Composition for preventing and treating striae gravidarum

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FR3028177B1 (en) * 2014-11-06 2018-09-14 L'oreal USE OF THE ASSOCIATION OF ASCORBIC ACID AND ELLAGIC ACID AS A SOOTHING AGENT

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US9421180B2 (en) 2011-09-30 2016-08-23 Perio Sciences, Llc Antioxidant compositions for treatment of inflammation or oxidative damage
US10918613B2 (en) 2011-09-30 2021-02-16 Perio Sciences, Llc Antioxidant compositions for treatment of inflammation or oxidative damage
CN109106685A (en) * 2018-08-08 2019-01-01 浙江工业大学 A kind of embedding insulin multiple emulsion and its preparation and application
CN110974716A (en) * 2019-12-31 2020-04-10 华熙生物科技股份有限公司 Composition for preventing and treating striae gravidarum
CN110974716B (en) * 2019-12-31 2023-02-03 华熙生物科技股份有限公司 Composition for preventing and treating striae gravidarum

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