EP2863878A2 - Kosmetische und dermatologische zubereitung enthaltend eine oder mehrere substanz(en), die das gen / protein für den rezeptor endo180 modulieren - Google Patents
Kosmetische und dermatologische zubereitung enthaltend eine oder mehrere substanz(en), die das gen / protein für den rezeptor endo180 modulierenInfo
- Publication number
- EP2863878A2 EP2863878A2 EP13725161.7A EP13725161A EP2863878A2 EP 2863878 A2 EP2863878 A2 EP 2863878A2 EP 13725161 A EP13725161 A EP 13725161A EP 2863878 A2 EP2863878 A2 EP 2863878A2
- Authority
- EP
- European Patent Office
- Prior art keywords
- cas
- weight
- collagen
- endo180
- skin
- 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.)
- Ceased
Links
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
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/342—Alcohols having more than seven atoms in an unbroken chain
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/347—Phenols
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/37—Esters of carboxylic acids
- A61K8/375—Esters of carboxylic acids the alcohol moiety containing more than one hydroxy group
-
- 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
- A61Q19/10—Washing or bathing preparations
Definitions
- Cosmetic and dermatological preparation containing one or more substance (s) that modulate the gene / protein for the receptor Endo180
- the invention encompasses cosmetic and dermatological preparations containing one or more substance (s) which modulate the gene / protein for the receptor Endo180, in particular those preparations for use on the skin of a human for the repair and regeneration of the human skin, in particular for improved skin contouring or against age-related skin folds.
- the aim of skin care is also to compensate for the daily loss of fat and water loss of the skin. This is especially important when the natural regeneration capacity is insufficient.
- skin care products to protect against environmental influences, especially from the sun and wind, and delay the aging of the skin.
- Chronic skin aging is e.g. caused by endogenous, genetically determined factors.
- age-related e. to the following structural damage and dysfunctions: a) dryness, roughness and formation of dryness wrinkles,
- Exogenous factors such as UV light and chemical noxae can be cumulatively effective and e.g. accelerate or supplement intrinsic aging processes.
- exogenous factors occur, e.g. to the following structural damage and dysfunction in the skin that go beyond the extent and quality of the damage caused by chronological aging: g) Visible vascular dilations (telangiectasia, cuperosis);
- the present invention relates in particular to products for the care of naturally aged skin (intrinsic and extrinsic skin aging) and to the phenomena listed under a), c), e), h) and j).
- Products for the care of relaxed, especially aged, skin are known per se. They contain e.g. Retinoids (vitamin A acid and / or derivatives thereof) or vitamin A and / or its derivatives.
- Retinoids vitamin A acid and / or derivatives thereof
- their effect on structural damage is limited in their scope.
- the use of vitamin A acid-containing products often causes severe erythematous skin irritation. Retinoids can therefore only be used in low concentrations.
- collagen The main connective tissue protein, collagen, which gives the skin resilience and tensile strength, also undergoes metabolism, from collagen synthesis via fibrillogenesis to degradation and endocytosis. Collagen turnover is a relatively slow process because half-lives are described for collagen 10-15 years (Verzijl et al, 2000).
- Collagen is the most prominent protein in human skin and accounts for approximately 85% of the total protein. Thus, the collagen fibers have a decisive influence on the external appearance of the skin.
- the collagen turnover in the skin depends on the balance between the new formation and the breakdown of the collagen.
- the intrinsic and especially extrinsic aging of the skin leads to reduced collagen synthesis and increased degradation by collagen degrading enzymes such as matrix metalloproteases (MMPs).
- MMPs matrix metalloproteases
- the balance is disturbed, and there is a loss of dermal collagen, which contributes to the wrinkling and declining elasticity of aging skin.
- MMPs matrix metalloproteases
- Fibroblasts possess various receptors for collagen, in particular integrins, discoidin domain receptors (DDRs) and members of the mannose receptor family such as Endo180 (Leitinger and Hohenester, 2007).
- DDR2 and Endo180 receptors have been detected in murine skin fibroblasts in association with wound healing and remodeling processes (Olaso et al, 2002, Madsen et al, 2007).
- DDR2 is a receptor tyrosine kinase that is important for fibroblast proliferation as well as collagen fibrillogenesis.
- Endo180 is important for the endocytotic removal of both intact collagen and collagen fragments. Following receptor-mediated collagen endocytosis, the resulting vesicles fuse with lysosomes, and the collagen fragments are subsequently degraded by cathepsins (Rünger et al, 2007). There is evidence that denatured collagens are better absorbed than native ones. For fibroblasts cultured on denatured collagen versus native collagen, the former show increased collagen uptake and COL1A1 expression (Abraham et al, 2007).
- Endo180 and integrin a 2 ßi are receptors on the surface of mesenchymal cells such as dermal fibroblasts and responsible for the uptake of collagen. It has been shown that Endo180 and integrin a 2 are downregulated in photoaged skin or after acute UV stress in vivo (Fig. 1).
- A) Gene expression analysis of endo180 and integrin a 2 in chronic sun-exposed (neck) versus sun-protected skin. Subjects with a clinically diagnosed solar elastosis in the neck were taken full-thickness biopsies from a sun-exposed area (neck) and a sun-protected area (inner upper arm). The mRNA values were normalized to the 18S rRNA values. n . 8 B) Gene expression analysis of Endo180 and integrin a 2 after acute UV stress (2 minimal erythema can (MED)) in vivo. After 24h and 48h full skin punching (buttocks) were taken for analysis. Punch biopsies from unirradiated areas were used as controls.
- MED minimal erythema can
- B) Analysis of collagen internalization by flow cytometry. One day after SSR irradiation (135 mJ / cm 2 ), the cells were incubated for 24 h with collagen fluorescein [25 ⁇ g / ml] and the fraction of cells that had taken up collagen fluorescein was determined. The control was unirradiated cells. It was found that the collagen uptake after SSR irradiation was reduced by about 30%. n 6
- the fibroblast is surrounded pericellularly by degraded collagen
- the object of the present invention was therefore to find ways that avoid the disadvantages of the prior art.
- Another object of the present invention was to provide skin care preparations and skin care preparations, which preparations should soothe and beautify the body exterior.
- the receptor Endo180 is responsible for the uptake of collagen fragments by fibroblasts. Its expression decreases in photoaged skin. It would be desirable to stimulate the expression of Endo180 in the aging skin as an anti-aging approach.
- perfume raw material (s) selected from the group
- Hexenol cis-3 (CAS No .: 928-96-1), tetrahydromuguol (CAS No .: 78-69-3), limonene D-pure (CAS No .: 5989-27-5), benzyl salicylate (CAS No.
- perfume raw material selected from the group Coumarin (CAS No .: 91-64-5), Iraldeine alpha iff (CAS No .: 127-41-3), Farnesol (CAS No: 4602-84-0), Lilial (CAS no.
- Particularly advantageous active ingredients used according to the invention are coumarin (CAS No .: 91-64-5), dihydromyrcenol (CAS No .: 18479-58-8), cinnamic aldehyde (CAS No .: 104-55-2), Florosa ( CAS No .: 63500-71 -0), hexyl salicylate (CAS No .: 6259-76-3), hydroxycitronellal (CAS No .: 107-75-5) and lyral (CAS No .: 31906-04 -4).
- Thymol 89-83-8 109 The use of preparations according to the invention having a cosmetically effective content of one or more active ingredients used according to the invention - eg. B. in the form of the examples mentioned - leads to a surprising improvement in the appearance of the aged skin.
- Cosmetic or dermatological preparations according to the invention preferably contain from 0.00001 to 50% by weight, preferably from 0.001 to 20% by weight, of one or more active ingredients used according to the invention, based on the total weight of the preparation.
- the cosmetic or dermatological preparations according to the invention may be composed as usual and serve for the treatment, care and cleansing of the skin. They preferably contain 0.002-10.0% by weight, more preferably 0.002-5.0% by weight, very preferably 0.005-3.0% by weight, based on the total weight of the preparations, of one or more according to the invention used active ingredients.
- Emulsions are advantageous dosage forms in the sense of the present invention, e.g. in the form of a cream, a lotion, a cosmetic milk are advantageous and contain e.g. Fats, oils, waxes and / or other fatty substances, as well as water and one or more emulsifiers, as they are commonly used for such a type of formulation.
- Medicinal topical compositions according to the present invention usually contain one or more drugs in effective concentration.
- drugs for the sake of simplicity, reference is made to the clear distinction between cosmetic and medical use and corresponding products to the statutory provisions of the Federal Republic of Germany (for example, Cosmetics Regulation, Food and Medicines Act).
- the cosmetic or dermatological preparation in the sense of the present invention is a solution or emulsion or dispersion, it is possible to use as solvent:
- Oils such as triglycerides of capric or caprylic acid, but preferably castor oil;
- Fats, waxes and other natural and synthetic fats preferably esters of fatty acids with lower C-number alcohols, e.g. with isopropanol, propylene glycol or glycerol, or esters of fatty alcohols with alkanoic acids of low C number or with fatty acids;
- Alcohols, diols or polyols of low C number, and their ethers preferably ethanol, isopropanol, propylene glycol, glycerol, ethylene glycol, ethylene glycol monoethyl or monobutyl ether, propylene glycol monomethyl, monoethyl or monobutyl ether, diethylene glycol monomethyl or monoethyl ether and analogous products ,
- mixtures of the abovementioned solvents are used.
- alcoholic solvents water can be another ingredient.
- the oil phase of the emulsions, oleogels or hydrodispersions or lipodispersions in the context of the present invention is advantageously selected from the group of esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids having a chain length of 3 to 30 carbon atoms and saturated and / or unsaturated, branched and / or unbranched alcohols having a chain length of from 3 to 30 carbon atoms, from the group of esters of aromatic carboxylic acids and saturated and / or unsaturated, branched and / or unbranched alcohols having a chain length of from 3 to 30 carbon atoms. atoms.
- ester oils can then advantageously be chosen from the group isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyl stearate, isononyl isononanoate, 2-ethylhexyl palmitate, 2-ethylhexyl laurate, 2-hexyldecyl stearate, 2-octyl dodecyl palmitate, oleyl oleate, oleyl erucate, erucyl oleate, erucyl erucate, and synthetic, semi-synthetic and natural mixtures of such esters, eg jojoba oil.
- the oil phase can be advantageously selected from the group of branched and unbranched hydrocarbons and waxes, the silicone oils, the dialkyl ethers, the group of saturated or unsaturated, branched or unbranched alcohols, and the fatty acid triglycerides, namely the triglycerol esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids of a chain length of 8 to 24, in particular 12 to 18 carbon atoms.
- the fatty acid triglycerides can be advantageously selected from the group of synthetic, semi-synthetic and natural oils, e.g. Olive oil, sunflower oil, soybean oil, peanut oil, rapeseed oil, almond oil, palm oil, coconut oil, palm kernel oil, and the like.
- Alcohols, diols or polyols of low C number, and their ethers preferably ethanol, isopropanol, propylene glycol, glycerol, ethylene glycol, ethylene glycol monoethyl or monobutyl ether, propylene glycol monomethyl, monoethyl or monobutyl ether, diethylene glycol monomethyl or monoethyl ether and analogous products, furthermore low C-number alcohols, eg Ethanol, isopropanol, 1, 2-propanediol, glycerol and in particular one or more thickening agents, which or which can be advantageously selected from the group of silica, aluminum silicates, polysaccharides or their derivatives, e.g.
- Hyaluronic acid, xanthan gum, hydroxypropylmethylcellulose particularly advantageously from the group of polyacrylates, preferably a polyacrylate from the group of so-called carbopols, for example Carbopols types 980, 981, 1382, 2984, 5984, each individually or in combination.
- carbopols for example Carbopols types 980, 981, 1382, 2984, 5984, each individually or in combination.
- Gels used in the present invention usually contain low C number alcohols, e.g. Ethanol, isopropanol, 1, 2-propanediol, glycerol and water or an above-mentioned oil in the presence of a thickener which is preferably silica or an aluminosilicate in oily-alcoholic gels, in aqueous-alcoholic or alcoholic gels, preferably a polyacrylate.
- a thickener which is preferably silica or an aluminosilicate in oily-alcoholic gels, in aqueous-alcoholic or alcoholic gels, preferably a polyacrylate.
- Solid pens contain eg natural or synthetic waxes, fatty alcohols or Fatty acid ester.
- liquid oils eg paraffin oils, castor oil, isopropyl myristate
- semi-solid constituents eg petrolatum, lanolin
- solid constituents eg beeswax, ceresin and microcrystalline Waxes or ozokerite
- high-melting waxes eg carnauba wax, candelilla wax
- Suitable propellants for sprayable from aerosol containers cosmetic and / or dermatological preparations in the context of the present invention the usual known volatile, liquefied propellants, such as hydrocarbons (propane, butane, isobutane) are suitable, which can be used alone or in mixture with each other. Also, compressed air is advantageous to use.
- hydrocarbons propane, butane, isobutane
- PEG-40 Stearates 0.80 1.00 1.00 1.00
- Methyl Methacrylate Crosspolymer 1 0 1, 0
- Nylon 12 1.0 1.0 1.0 1.0 1.0
- Glyceryl stearates self-emulsifying 2 2 1, 5 1, 5
- Phenoxyethanol 0.35 0.25 0.3 0.3
- Glyceryl stearate self-emulsifying 1.0 1.0 1.0 1.0
- Phenylbenzimidazole sulfonic acid 1.0 1.0 - 1.0
- Cetylstearyl alcohol 5.0 3.5 4.0 3.0
- Caprylic acid / capric acid triglycerides 2.0 2.5 1, 0 2.0
- Methylisothiazolinone 0.05 - -
Abstract
Description
Claims
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102012210399A DE102012210399A1 (de) | 2012-06-20 | 2012-06-20 | Kosmetische und dermatologische Zubereitung enthaltend eine oder mehrere Substanz(en), die das Gen / Protein für den Rezeptor Endo180 modulieren |
PCT/EP2013/060840 WO2013189694A2 (de) | 2012-06-20 | 2013-05-27 | Kosmetische und dermatologische zubereitung enthaltend eine oder mehrere substanz(en), die das gen / protein für den rezeptor endo180 modulieren |
Publications (1)
Publication Number | Publication Date |
---|---|
EP2863878A2 true EP2863878A2 (de) | 2015-04-29 |
Family
ID=48520968
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP13725161.7A Ceased EP2863878A2 (de) | 2012-06-20 | 2013-05-27 | Kosmetische und dermatologische zubereitung enthaltend eine oder mehrere substanz(en), die das gen / protein für den rezeptor endo180 modulieren |
Country Status (3)
Country | Link |
---|---|
EP (1) | EP2863878A2 (de) |
DE (1) | DE102012210399A1 (de) |
WO (1) | WO2013189694A2 (de) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP6781549B2 (ja) * | 2016-01-21 | 2020-11-04 | 丸善製薬株式会社 | Endo180産生促進剤 |
JP7455344B2 (ja) | 2018-04-03 | 2024-03-26 | 丸善製薬株式会社 | Endo180産生促進剤 |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6063390A (en) * | 1998-08-07 | 2000-05-16 | Chesebrough-Pond's Usa Co., A Division Of Conopco, Inc. | Cosmetic effervescent cleansing pillow |
FR2813195B1 (fr) * | 2000-08-29 | 2003-04-04 | Serobiologiques Lab Sa | Utilisation d'extraits de la plante cassia alata dans des produits de soin |
FR2877219B1 (fr) * | 2004-10-28 | 2007-03-09 | Fatima Basri | Composition utilisee en cosmetique ou en pharmacologie pour stimuler la synthese du collagene |
DE102005056393A1 (de) * | 2005-11-24 | 2007-05-31 | Grünenthal GmbH | Multicyclische Verbindungen in druckempfindlichen Klebstoffen |
DE102008034944B4 (de) * | 2008-07-26 | 2017-03-16 | Arivine Pharma Ag | Mikroemulsion |
-
2012
- 2012-06-20 DE DE102012210399A patent/DE102012210399A1/de not_active Withdrawn
-
2013
- 2013-05-27 WO PCT/EP2013/060840 patent/WO2013189694A2/de active Application Filing
- 2013-05-27 EP EP13725161.7A patent/EP2863878A2/de not_active Ceased
Non-Patent Citations (2)
Title |
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None * |
See also references of WO2013189694A2 * |
Also Published As
Publication number | Publication date |
---|---|
WO2013189694A3 (de) | 2014-06-26 |
DE102012210399A1 (de) | 2013-12-24 |
WO2013189694A2 (de) | 2013-12-27 |
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