Cosmetic preparation for skin care

EP4465956A4Pending Publication Date: 2026-01-21UNIV MIKOLAJA KOPERNIKA
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Patent Information

Application Number
EP2022922390
Authority / Receiving Office
EP · EP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2022-01-18
Filing Date
2022-04-30
Publication Date
2026-01-21

AI Technical Summary

Technical Problem

Current cosmetic preparations lack selective efficacy in addressing the proliferation of normal cells while effectively inhibiting neoplastic skin lesions, particularly in skin types with lesions caused by epidermal resection, and do not adequately enhance the skin's barrier function against UV radiation and free radicals.

Method used

A cosmetic preparation containing 0.125% to 0.250% gallic acid, combined with humectants like glycerin or propylene glycol, phenoxyethanol, methyl glucose sesquearate, cetyl alcohol, vegetable oils, and squalane, which selectively impacts cell proliferation and enhances skin barrier function, specifically inhibiting human melanoma cell growth while promoting fibroblast proliferation.

Benefits of technology

The preparation achieves a two-fold increase in fibroblast proliferation and significant inhibition of human melanoma cell proliferation, offering enhanced anti-radical protection and improved skin barrier function, suitable for all skin types including those with neoplastic lesions.

✦ Generated by Eureka AI based on patent content.

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Abstract

The cosmetic preparation for skin care is characterized by the fact that it contains: from 0.125% to 0.250% gallic acid from 3% to 5% humectant, preferably glycerin or propylene glycol from 1% to 1.5% phenoxyethanol 4% to 6% methylglucose sesquistearate from 3% to 5% cetyl alcohol from 14% to 17% of vegetable oil, preferably sunflower or rapeseed or linseed oil, or from nut seeds or from fruit or fruit seeds 7-9% squalane the rest up to 100% is water.
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Description

[0001] Cosmetic preparation for skin care

[0002] The subject of the invention is a cosmetic preparation for the care of the skin.

[0003] The skin is a natural barrier that protects our body against harmful external factors. It is exposed to year-round UV radiation reaching the Earth. Lack of proper prophylaxis against the harmful effects of this radiation may lead to skin lesions, including cancerous ones.

[0004] Known from Pat.198268, there is a herbal composition consisting of at least three plants, containing active substances in the form of carotenoids, iridoids, especially aucubin and catalpol, and polyphenols, especially phenolic acids and flavonoids, where these plants are present in supplementary amounts to obtain a mixture of 0.3 to 1 per 100 g, 5% carotenoids, 0.5 to 1.0% iridoids, 0.5 to 4.0% polyphenols.

[0005] The cosmetic preparation of active substances is known from US6989150, both as such and in combination with other active substances which protect the skin particularly effectively against the aggression of free radicals. The preparation consists of quebracho bianco bark extract, which contains: at least 90 wt%. proanthocyanidin oligomers, silkworm extract, which contains the peptide cecropin, amino acids and a mixture of vitamins, non-ionic, cationic or anionic hydrogel, phospholipids, yeast breakdown product and cyclodextrins. According to the invention, the preparation may contain additional active substances, such as plant extracts of acerola, seaweed, citrus, bitter orange, cherries, papaya, tea, coffee beans, peel and angelica. The preparations synergistically increase the anti-radical protection factor to 10,000. Cosmetic compositions containing these preparations have the anti-radical protection factors from 40 to 400, depending on the portion of the preparation.

[0006] The eutectic of gallic acid and glycine is known from CN 113233976 A, as well as from a whitening cream containing eutectic, eutectic of gallic acid and glycine added to the cosmetic, where the rate of gallic acid dissolution is increased due to eutectics and the gallic acid absorption capacity and the whitening healing effect of the cosmetic are improved.

[0007] The cosmetic and pharmaceutical use of gallic acid and gallic acid derivatives is known from CN106456478A. The invention relates to a compound, a salt of a compound, a derivative of a compound or a salt of a derivative, wherein the compound is selected from gallic acid, its gallic acid hydrolyzing polymers, hexahydroxydiphenic acid, its hexahydroxy diphenic acid hydrolyzing polymers, ellagic acid, ellagic acid hydrolyzing polymers thereof, galotannins, elagitans and their cosmetic use to stimulate or repair the barrier function of the epidermis and their pharmaceutical functions to treat damage caused by conditions such as Crohn's disease.

[0008] The aim of the invention is to develop such a cosmetic preparation with the addition of gallic acid that will allow for a selective effect on the proliferation of normal cells and melanomas and will be intended for all skin types, including the skin of people with skin lesions caused by epidermal resection in order to remove neoplastic skin lesions. This objective has been achieved in the cosmetic preparation obtained according to the following invention and with the described method of its preparation.

[0009] The essence of the invention is a cosmetic preparation for skin care, characterized by the content of 0.125% to 0.250% gallic acid, from 3% to 5% humectant, preferably glycerin or propylene glycol, from 1% to 1.5% phenoxyethanol, from 4% to 6% methyl glucose sesquearate, 3% to 5% cetyl alcohol, 14% to 17% vegetable oil, preferably sunflower or rapeseed or linseed or nut kernel or fruit or fruit kernel oil, 7-9% squalane. The rest up to 100% is water.

[0010] It is preferable to add gallic acid to the aqueous phase to prepare the emulsion. The invention is presented in the examples, which do not limit the invention, but represent its most preferred variants. The invention fulfills all ranges of the listed ingredients. Example I. A cosmetic emulsion was prepared containing in the fat phase 5% methyl glucose sesquearate (INCI: Methyl Glucose Sesquistearate), 4% cetyl alcohol (INCI: Cethyl Alcohol), 8% squalane (INCI: Squalane), 15% sunflower oil (INCI: Helianthus Annus Seed Oil); in the water phase, while 3% glycerin (INCI: Glycerin), 0.250% gallic acid (INCI: Gallic Acid), 1% Euxyl PE 9010 (INCI: Phenoxyethanol, Ethylhexylglycerin), and water (INCI: Aqua) supplemented to 100%.

[0011] For a solution of gallic acid in water with a concentration of 0.250%, cell tests were performed using the human fibroblast line and the human melanoma line.

[0012] Cellular studies were also performed on the emulsions obtained according to the description of the invention.

[0013] The human fibroblast line (passage 2) (NHDF) and the human melanoma line (MNT-1) were cultured in MEM (Minimum Essential Medium Eagle), respectively, supplemented with 10% inactivated bovine serum, 2 mM L-glutamine and 1% streptomycin / penicillin solution for human fibroblasts and MEM medium enriched with 20% inactivated bovine serum, 10% AIM-V ™ medium, 2 mM L-glutamine, 10 mM HEPES, 1% NEAA (non- esential amino acids) and 1% streptomycin / penicillin solution for melanoma cells.

[0014] Cultures were carried out in bottles in an incubator maintaining a constant temperature of 37 ° C and a constant concentration of 5% CO2. After a confluent culture (70-80%) was obtained, the medium was removed, the cells were washed twice with warm 1 x PBS buffer (pH 7.4) and incubated for approximately 1 minute with 1-2 ml of trypsin / EDTA solution (1 x). The detached cells were gently pipetted with an aliquot of fresh medium. Part of the suspension was allocated to the proliferation experiment in the presence of gallic acid (concentration range: 0.15%, 0.03%, 0.0625%, 0.125%, 0.25%, 0.5%) versus the control (cells in the presence of the appropriate culture medium). The cells were seeded in a 96-well plate (0.15x105 cells / well) and allowed to remain there for 24 hours for the cells to adhere to the medium. After this time, the cells were incubated with gallic acid in the above concentration range for 96 hours (well solution volume: 200 pl) and the proliferation was assessed with the MTT test based on tetrazolium salt (thiazole blue formazan), which is converted by active mitochondrial dehydrogenase to water-insoluble formazan crystals. After incubation, the medium was removed from the cells and 100 pl of a mixture of MTT and the medium (1 : 10) was added, followed by incubation for 3 hours (37 ° C, 5% CO2). Then, 100 pl of acid isopropanol (isopropanol containing 0.04N HC1) was added to each of the wells and the resulting formazan crystals were pipetted to obtain the same dispersion. The dye optical density was measured at 595 nm using a BioTek ELx808 ™ plate reader (BioTek Instruments, Inc., Winooski, VT, USA).

[0015] Statistical analysis was performed by analysis of variance, ANOVA using GraphPad Prism 7.05 software (La Jolla, CA, USA). Differences from the controls of * p <0.05, ** p <0.01 and *** p <0.001 were considered as statistically significant. The results were obtained in six replicates and presented as mean + standard deviation (SD).

[0016] Figure 1. Cell proliferation (% relative to control) obtained as a result of contact of cells with various concentrations (0.015%; 0.03%; 0.0625%; 0.125%; 0.25%; 0.5%) with cells of the human fibroblast line .

[0017]

[0018] Figure 2. Cell proliferation (% relative to control) obtained by contacting cells with various concentrations (0.015%; 0.03%; 0.0625%; 0.125%; 0.25%; 0.5%) with the human melanoma line.

[0019] The results show the differentiation of cell proliferation of different lines depending on the concentration of gallic acid (Figures 1 and 2). On their basis, 0.25% gallic acid addition was selected as active substance and emulsions were prepared. Cellular studies of the prepared emulsions showed a two-fold increase in proliferation of the human fibroblast lineage with inhibition of proliferation of the human melanoma lineage.

[0020] Example II.

[0021] The cosmetic preparation for skin care contains:

[0022] 0.125% gallic acid

[0023] 3% humectant in the form of glycerin

[0024] 1% phenoxyethanol

[0025] 4% methylglucose sesquistearate

[0026] 3% cetyl alcohol

[0027] 14% sunflower vegetable oil

[0028] 7% squalane the rest up to 100% is water.

[0029] Example III.

[0030] The cosmetic preparation for skin care contains:

[0031] 0.250% gallic acid

[0032] 5% humectant in the form of propylene glycol

[0033] 1.5% phenoxyethanol in the form of propylene glycol

[0034] 6% methylglucose sesquistearate

[0035] 5% cetyl alcohol

[0036] 17% of rapeseed vegetable oil

[0037] 9% squalane the rest up to 100% is water.

[0038] Example IV.

[0039] The cosmetic preparation for skin care contains:

[0040] 0.190% gallic acid

[0041] 4% humectant in the form of glycerin

[0042] 1.2% phenoxyethanol 5% methylglucose sesquistearate

[0043] 4% cetyl alcohol

[0044] 15.9% of rapeseed vegetable oil

[0045] 8% squalane the rest up to 100% is water.

[0046] Example V.

[0047] The cosmetic preparation for skin care contains:

[0048] 0.21% gallic acid

[0049] 4.5% humectant in the form of glycerin

[0050] 1.4% phenoxyethanol in the form of Euxyl PE 9010, which is a mixture of phenoxyethanol and ethylhexylglycerin

[0051] 4.2% methylglucose sesquistearate

[0052] 3.1% cetyl alcohol

[0053] 16.7% of rapeseed vegetable oil

[0054] 7.3% squalane the rest up to 100% is water.

Claims

Patent claim1. The cosmetic preparation for skin care that contains: from 0.125% to 0.250% gallic acid from 3% to 5% humectant, preferably glycerin or propylene glycol from 1% to 1.5% phenoxyethanol4% to 6% methylglucose sesquistearate from 3% to 5% cetyl alcohol from 14% to 17% of vegetable oil, preferably sunflower or rapeseed or linseed oil, or oil from nut seeds or from fruit or fruit seeds7-9% squalane the rest up to 100% is water.

Citation Information

Patent Citations

  • Antibacterial or antiseptic

    JP2020083771A

  • Pharmaceutical composition for wound healing containing gallic acid, derivatives thereof or pharmaceutically acceptable salts thereof as an active ingredient

    KR1020170034808A

  • Cosmetic composition comprising a natural organic oil and polymethylmethacrylate particles

    WO2014184228A1