RU2376974C2 - Transdermal gel for face 'stvolin" - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention relates to medicine, in particular to cosmetology. As biologically active additive gel contains suspension of niosomes with size up to 100 Nm with included in them extract of stem cells of pig's placenta, hyaluronic acid, oil of avocado, base includes acrylate emulsion of copolymer (Salcare SC80™), cyclometicon (DC 345™), preservative, odorant and low mineralised spring water for intensified nutrition, moistening and regeneration of skin.

EFFECT: intended for intensified moistening, nutrition, regeneration, increasing of tonus and elasticity of face skin by means of biologically active substances (BAS), included in transdermal carriers - niosomes.

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Description

The invention relates to medicine, in particular to cosmetology. Transdermal gel is intended for regeneration, enhanced moisturizing, nutrition, increasing the tone and elasticity of the skin of the face with the help of biologically active substances (BAS), which are included in the transdermal carriers - niosomes.

The skin on the face is very different in structure from the rest of the skin of a person, here it is very thin, more oily and requires special care. At any age, it is necessary to cleanse, nourish, moisturize and protect the skin of the face from the harmful effects of the environment.

Known gel for facial skin care (RF Patent No. 2142269, publ. 10.12.1999, Bull. No. 34) containing an extract from antlers of reindeer, carbomers or Sacap, or Sacap-R, 2,2'-2 ' '-Nitrilotriethanolyl, or sodium hydroxide, or aqueous ammonia, glycerin or propylene glycol, bronitrol or bronopol, PEG-40 hydrogenated castor oil, perfume and drinking water. The gel has a rejuvenating, moisturizing property, nourishes, increases its elasticity.

The disadvantage of the gel is the use of bronopol, which is in contact with the components of the product with the formation of toxic nitrogen oxides, as well as aqueous ammonia, which impairs the organoleptic characteristics of the gel.

Known cosmetic gel for the face (RF Patent No. 2102975, publ. 01/27/1998, Bull. No. 3), which contains as biologically active substances the sodium salt of deoxyribonucleic acid, a gelling copolymer based on acrylic acid, distilled glycerin or 1.2 -propylene glycol, ethyl alcohol, triethanolamine, a plasticizer selected from the group consisting of perfume oil, butyl stearate, isopropyl myristate, isopropyl palmitate, perfume, preservative, dye, and water up to 100.0. The cosmetic gel also contains polyethylsiloxane liquid and hydroxyethylated lanolin. The gel has anti-geriatric, anti-inflammatory, hydratant, antioxidant effects.

With all its advantages, the gel has its drawbacks: it contains lanolin, which is a potential allergen, and ethyl alcohol, which dries the skin.

Closest to the claimed invention is a cosmetic gel for skin care of the face (RF Patent No. 2245707, publ. 02/10/2005, Bull. No. 4), containing a gel-forming component - a copolymer of acrylic acid - carbopol, pH regulator - triethanolamine, preservative, perfume, biologically active additive and water, while fullerenes or shungite water, wheat germ oil, tocopherol acetate (vitamin E), vitamin A, vitamin F, water, components are taken in a certain quantitative content as a biologically active additive. The gel has anti-inflammatory, moisturizing and antioxidant effects while oxygenating the skin. The gel tones, softens and nourishes the skin, improves skin respiration, is not toxic, does not cause allergic reactions.

The disadvantage of the gel is insufficient transdermal transfer of biologically active substances (BAS) due to the lack of penetration enhancers and transdermal carriers.

The purpose of the invention is the regeneration, hydration, nutrition, increase the tone and elasticity of the skin of the face with biologically active substances included in the transdermal carriers - niosomes.

Niosomes are vesicles consisting of a shell in the form of a water-insoluble double layer of a nonionic emulsifier (surfactant), which is a group of dimethicone copolyols that are esters of a polyethylene glycol and a polydimethylsiloxane base and a biologically active substance enclosed inside a capsule. Thus, dimethicone copolyols are a hybrid of silicon and carbon. Unlike liposomes made on the basis of phospholipids, niosomes have a number of advantages for the delivery of biologically active substances. The presence of the Si-O covalent bond in the hydrophobic part of the emulsifier polydimethylsiloxane base molecule, which has great elasticity and reactivity, allows the targeted delivery of a wide range of biologically active substances using reactive sites and their targeted release from the vesicles. These properties allow the use of niosomes for interstitial delivery of biologically active substances (antibiotics, vitamins, plant and animal extracts).

This goal is achieved due to the fact that the biologically active substances included in the vesicles - niosomes, are able to penetrate into the deeper layers of the skin, overcoming the stratum corneum of the epidermis, and provide the necessary therapeutic effect.

In relation to the prototype in composition, the inventive transdermal gel for face “STVOLIN” has the following distinctive features.

A correctly selected “delivery system” of a biologically active substance (BAS) through the skin of a person largely determines the effectiveness and safety of a cosmetic product. A high degree of selectivity of the action of biologically active substances (BAS) can be achieved by using bilayer silicone vesicles as transdermal carriers of NIOSOM. All biologically active substances of the gel are microencapsulated in vesicles up to 100 nm in size, consisting of a bimolecular layer of PEG-12 Dimethicone.

The resulting vesicles have increased stability over time and a standardized size of up to 100 nm, which allows you to freely transfer biologically active substances through the stratum corneum (Stratum Corneum) deep into the dermis.

The gel contains an extract of regional stem cells from pig placenta, which has unique properties: the presence of growth factor (bFGF), cytamines, cytokines - signal peptides that provide for the regeneration (renewal) of cells and tissues; the presence of a wide range of vitamins A, D, E, F, K, Q ₁₀ , supporting the flow of biochemical processes in the skin.

The use of the extract of regional stem cells from pig placenta as the main biologically active substance in the gel allows you to enhance its effect: accelerate the renewal of skin cells due to cell division of collagen, elastin and keratinocytes. Its action is based not on external effects on skin cells, but on signaling mechanisms of intercellular interaction.

The development of a modern formulation of a cosmetic product depends on the final purpose of its use, therefore, a rational solution is a formulation that would emphasize the action of the main active active component - an extract of regional stem cells from pig placenta. The optimal structure to ensure uniform distribution of the extract is a gel, in contrast to a conventional emulsion, requiring a large amount of ballast substances (for example, saturated lipids).

To enhance the nutritional and moisturizing properties of the gel, avocado oil (Persea gratissima) is included in the formulation, which also has excellent regenerative properties, complementing the action of stem cell extract. Due to unsaponifiable components (phospholipids, tocopherols, sterols (β-sitosterol, campesterol, avenasterin, squalene) and a high content of polyunsaturated fatty acids (oleic, palmitic, linoleic, palmitoleic), it well restores the structure of the epidermis and improves the moisture-holding properties of the skin.

Avocado oil has a high viscosity, therefore, to improve the spreadability of the gel on the surface of the skin and eliminate its stickiness, DC 345 ™ cyclomethicone was introduced into the formulation (Dow Corning, USA). The use of cyclomethicones based on cyclopentasiloxane improved the organoleptic characteristics of the gel.

Low molecular weight hyaluronic acid (Hyalyronic acid, LMW), which is a structural part of the epidermis, can give the gel moisturizing properties. One molecule of hyaluronic acid can hold up to 100 water molecules. Hylauronic acid forms a film on the surface of the skin that holds water and transmits oxygen, thereby moisturizing the skin due to internal reserves of the body.

The fragrance of the German company Curt Georgi ^® (Germany) gives a pleasant aroma to the gel. To preserve the gel, a water-soluble preservative Kathon CG ™ (Great Britain) is introduced.

The aqueous anionic acrylate emulsion of the Salcare SC 80 ™ copolymer (INCI: Steareth-lOAllyl Ether / Acrylates Copolymer), which is a carbomer, was chosen as the basis for the gel. Salcare SC80 ™ is compatible with a wide range of cosmetic components. Typically, carbomers are in the form of a white fine powder (Carbopol ™, Cosmedia SP ™), which must first be subjected to the stage of swelling and dispersion. Salcare SC80 ™ is easy to use due to its emulsified form, which allows you to quickly get a clear gel.

The possibility of carrying out the claimed invention is confirmed by examples of specific performance.

Example 1

STVOLIN transdermal gel for face contains as a biologically active additive a 5.0% suspension of niosomes up to 100 nm in size with the included extract of regional stem cells from pig placenta, hyaluronic acid, avocado oil, and the base consists of an acrylate emulsion of a copolymer, cyclomethicon , triethanolamine, Kathon CG ™ preservative, perfume and low mineralized spring water.

The phases of preparation and formulation of the gel are presented in table 1.

Phase A is prepared at room temperature by mechanical mixing of the following components in a mixer: Salcare SC80 ™ copolymer acrylate emulsion, DC 345 ™ cyclomethicone, Curt Georgi ™ perfume, Kathon CG ™ preservative and low-mineralized spring water.

Phase B, containing a suspension of niosomes up to 100 nm in size, is manufactured separately and introduced into phase A with vigorous stirring. The niosome suspension contains avocado oil, regional stem cell extract from pig placenta, and hyaluronic acid.

The preparation of a suspension of niosomes consists in intensive mechanical stirring of the PEG-12 Dimethicone organosilicon surfactant in the corresponding oils and extracts. PEG-12 Dimethicone is added to the mixture of oil and extracts in an amount of 4% of the volume. The result is stable niosome vesicles capable of penetrating deep into the dermis.

The method of preparation of the extract of regional stem cells from pig placenta consists in the following operations: washing of pork placental tissue, trypsinization of placental tissue (treatment with trypsin enzyme to separate tissue cells), isolation of regional stem cells, growth on nutrient media (increase in cell mass), cell disintegration and water-salt extraction (2.5% NaCl solution).

To stabilize the concentration of hydrogen ions (pH) to 6.6-7.2 and form a gel structure, phase B, triethanolamine, is introduced. This component is introduced into the mixture last for the mixture to turn into a gel; in this case, the pH shifts to the alkaline side and interacts with the acrylate emulsion.

The prepared gel was applied to previously cleaned skin 1 time a day before bedtime. After 10 days of using the gel, the technical result was evaluated: the degree of keratinization and moisture. The maximum increase in the degree of keratinization was 10% and the moisture content of 5% with a suspension of niosomes of 5%.

Example 2. It is carried out analogously to example 1, only a suspension of niosomes is introduced in an amount of 15%, which includes an extract of regional stem cells from pig placenta, avocado oil and hyaluronic acid. The maximum increase in the degree of keratinization was 30% and the degree of moisture 30% of the initial values.

Example 3. It is carried out analogously to example 1, only a suspension of niosomes is introduced in an amount of 30%, which includes an extract of regional stem cells from pig placenta. The maximum increase in the degree of keratinization was 31% and the moisture content was 32% of the initial values.

Thus, the optimal delivery system is a suspension of niosomes in an amount of 15% containing the extract of stem cells, hyaluronic acid and avocado oil (example 2). A further increase in the percentage of niosomes did not lead to a significant increase in the degree of keratinization and hydration of the skin. The designed gel has passed clinical trials in the regional dermatovenerological dispensary and at the Department of Dermatovenerology and Cosmetology of the Stavropol State Medical Academy (protocol No. 27 of 10/17/2006).

As a result of the studies, the optimal percentage of niosomes in the inventive transdermal gel for the face “STVOLIN” was selected, which allows to obtain the maximum increase in the degree of keratinization of skin hydration (table 2). The claimed content of all components in the formulation of the transdermal gel for the face "STVOLIN" optimally ensures the achievement of the desired effect.

Thus, the inventive transdermal gel for face “STVOLIN” regenerates, intensely moisturizes and nourishes the skin, and also increases the tone and elasticity of the skin of the face. The desired therapeutic and cosmetic effect is achieved through the use of transdermal carriers of biologically active substances - niosomes.

Claims (1)

A transdermal gel for the face containing a jelly-forming substance, pH-triethanolamine regulator, dietary supplement, base, preservative, perfume, water, characterized in that it contains as a biologically active additive a suspension of niosomes up to 100 nm in size with the included extract of regional stem cells of pig placenta , hyaluronic acid, Avocado oil, as a preservative Kathon CG ™, and is based on an acrylate emulsion copolymer (Salcare SC80 ™), cyclomethicone (DC 345 ™) and low-mineralized spring water with the following content NTV, wt.%:
Niosome suspension containing avocado oil, stem cell extract, hyaluronic acid 5.0-30.0 Salcare SC80 ™ Acrylate Emulsion 3.0-3.5 Cyclomethicone DC 345 ™ 10.0-15.0 Triethanolamine 2.0-2.5 Fragrance Curt Georgi ™ 0.5-0.6 Kathon CG ™ Preservative 0,0004-0,0006 Low mineralized spring water up to 100.0