RU2500385C1 - Biologically active additive for preparing cosmetic products - Google Patents

Abstract

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetology and represents a biologically active additive for preparing a cosmetic products, containing oxygenated dextran of molecular weight 35-70 kDa, and a cosmetically acceptable excipient with the ingredients of the additive are found in specific proportions, wt %.

EFFECT: invention provides more effective inhibition of the process of senescence ensured by improved anti-inflammatory and phagocytic activity of the biologically active additive.

2 cl, 4 ex, 1 tbl

Description

The invention relates to the field of cosmetology and can be used in the manufacture of various cosmetics, which have the ability to normalize the functional condition of the skin due to the prevention of inflammatory phenomena caused by various adverse environmental factors.

Currently, there is a wide range of various medical and cosmetic products. The basic cosmetic composition (cream, lotion, mask, etc.) in this case is supplemented with some biologically active substance, which gives the cosmetic composition as a whole a specific therapeutic and prophylactic specificity. In some compositions, in addition to the biologically active substance, various moisturizers, antioxidants, solubilizing agents and transdermal delivery agents are added in order to enhance the therapeutic and prophylactic properties of the entire cosmetic composition.

Known biologically active additive (BAA) for cosmetics, which is a product obtained by mixing in equal volumes of the secretion of the salivary glands and the contents of the esophagus of medical leeches. This dietary supplement significantly stimulates protein metabolism, reduces the total lipid content in the skin, has a pronounced antioxidant and antiheriartic effect, has the ability to stimulate phagocytosis and DNA supermethylation, without showing irritating and allergenic effects on the skin (patent RU No. 2238718 C2, publ. 10/27/2004).

Known biologically active additive for cosmetics, which represents the larvae of drones of bees (drone brood), and a cosmetic cream based on it, providing a higher nutritional and regenerative effect. The cream contains a base, crushed insect larvae, biologically active substances of plant and animal origin with the following quantitative ratio of cream components, wt.%: Bee drones larvae (drone brood) 0.5-3.5, biologically active substances of plant and animal origin, including vegetable oils and bacteriostatic additives, or vegetable oils, bacteriostatic and tonic additives, or vegetable oils, bacteriostatic and sedative additives, not more than 24.0, the basis is the rest e (Patent RU 2129858 C1, publ. 10.05.1999).

Known biologically active additive containing at least 10 wt.% Chitosan gel or chitosan suspension with a size of spherical nanogranules of not more than 100 nm (patent RU 2209069 C1, publ. July 27, 2003).

Known biologically active additive for cosmetics, containing a mixture of Tambucan therapeutic mud, sapropel or preparations obtained from them, blue clay and kaolin, taken in a certain ratio, having antibacterial, absorbable, immunostimulating and anti-aging properties (patent RU 2180213 C1, publ. 03/10/2002).

Known biologically active additive for cosmetics, with a high regenerating ability, containing edible xylotrophic fungi either in the form of native mycelium obtained by the method of deep cultivation, or in the form of 5-25% aqueous-alcoholic extract from native mycelium of mushrooms. As xylotrophic fungi, Lentinus edodes, Pleurotus ostreatus, Flammulina velutipes, Ganoderma lucidum, Grifola frondosa, Pholiota nameko (patent RU 2232571 C1, publ. 20.07.2004) can be used.

However, the known additive has a low regenerative ability and has poorly expressed anti-inflammatory and antioxidant properties.

Known biologically active additive for cosmetics with anti-inflammatory and regenerative properties, which is a growth stimulator of bacterial cultures obtained from the culture fluid of bacteria E. Coli and Bifidobacterium adolescentis (patent RU 2180576 C2, publ. 10.12.1999),

Known biologically active additive for cosmetics from Jerusalem artichoke using various parts of the plant and their final forms of the following chemical composition: water, 2.0-14%; carbohydrates 14-90%; protein 1.0-20%; fats 0.1-12.0%; ash residue 3-16%. Supplements from Jerusalem artichoke have a healing effect on the skin through the presence of biological activity affecting the immune system, which allows you to selectively prepare cosmetics with therapeutic and prophylactic properties. In dietary supplements in high concentrations there are natural polysaccharides of predominantly inulin nature, which are the main biologically active substance (patent RU 2162684 C1, publ. 02/10/2001).

The main disadvantage of the above-mentioned known dietary supplements for cosmetics is that they have mild anti-inflammatory properties, and their active components are “living” natural substances that retain their activity for only a short time, and therefore cosmetic compositions based on them have extremely limited shelf life.

The closest to the claimed biologically active additive - the prototype, is an additive that stimulates microcirculation in the tissues of the skin, characterized in that it includes a cosmetically and / or dermatologically acceptable excipient and dextran sodium sulfate, taken in an amount of 1-10% (patent RU 2371170 C2, published on October 27, 2009).

The disadvantage of dietary supplements is the lack of anti-inflammatory properties.

The aim of the present invention is the creation of a biologically active additive for cosmetics based on a polysaccharide with a local anti-inflammatory effect.

EFFECT: increased effectiveness of a skin aging-inhibiting action due to the use of a biologically active supplement with anti-inflammatory and phagocytic activity.

This goal is achieved by the proposed biologically active additive containing oxidized dextran with an average molecular weight (m.M.) of 35 to 70 kDa and a cosmetically acceptable filler in the following components, in wt.%.

Oxidized Dextran with M.M. 35-70 kDa 0.5-5.0 cosmetically acceptable excipient up to 100

The inventive additive can be introduced into any cosmetic composition, both in the form of an aqueous solution, and in the form of a dry powder to achieve the claimed concentrations.

As a cosmetically acceptable excipient, water, physiological or buffer solution, microcrystalline cellulose can be used.

The main component of the proposed dietary supplement is oxidized dextran, which is an oxidized form of polysaccharide with the ability to stimulate the cellular immunity, in particular, phagocytosis.

It can be obtained by known methods based on the chemical or radiation oxidation of dextran. In particular, oxidized dextran can be obtained chemically, for example, by separating dextran fractions from the commercial preparation Reopoliglukin, subsequent oxidation of dextran with sodium periodate and precipitation of oxidized dextran with ethanol (patent RU 2087146, publ. 08.20.1997). Modifications of this method are known, characterized by the use of additional methods for purifying oxidized dextran from impurities (patent RU 2163120, publ. 02.20.2001). Potassium permanganate is also used as an oxidizing agent for dextran (EA patent No. 011718, publ. 04/28/2009).

Variants of cosmetic compositions containing the claimed dietary supplement are given in examples 1-4.

Example 1. Cosmetic cream containing, in wt.%:

Oxidized Dextran with M.M. 35-70 kDa 0.5-5.0 Lanolin 6.0-7.0 Spermaceti 3.0-4.0 Olive oil 20.0-25.0 Benzyl alcohol 1.5-2.0 Perfumery fragrance 0.5-1.5 Water rest

Example 2. Cosmetic mask containing, in wt.%:

Oxidized Dextran with M.M. 35-70 kDa 0.5-5.0 Olive oil 15.0-17.0 Cacao butter 6.0-8.0 Beeswax 2.0-5.0 Perfumery fragrance 0.1-0.5 Water rest

Example 3. Cosmetic milk containing, in wt.%:

Oxidized Dextran with M.M. 35-70 kDa 0.5-5.0 Olive oil 10.0-15.0 Soybean oil 12.0-13.0 Cedar oil 11.0-16.0 Beeswax 1.0-2.0 Water rest

Example 4. Face lotion containing, in wt.%:

Oxidized Dextran with M.M. 35-70 kDa 0.5-5.0 2-bromo-2-nitropropanediol-1,3 0.03-0.04 Perfumery fragrance 0.3-0.5 Water rest

The anti-inflammatory properties of the claimed biologically active additives were investigated on the model of “formalin” paw edema in mice. The experiments were performed on 90 Balb / C mice of both sexes weighing 20 ± 1.3 g. The tested cosmetic compositions containing the inventive biologically active additive (examples 1 and 4) were applied with light grinding to the sole of the paws of experimental animals daily for 10 days before induction acute inflammatory edema at a dose of 0.02 g. In control groups, solutions of sodium dextran sodium sulfate or physiological saline corresponding to concentrations were applied for 10 days. The induction of acute inflammatory edema was caused by subplanar administration of 0.05 ml of a 1% formalin solution. After administration of formalin solution, paw edema developed after 4 hours, as evidenced by a significant increase in its volume. The results of the study are presented in the table, where * - differences with the control (before the introduction of formalin solution) are significant (p <0.05)

As can be seen from the presented results, 4 hours after the introduction of formalin, the paw volume in experimental animals of the control group increased by an average of 66.9% (p <0.05). In mice that received test cosmetic compositions containing the claimed biologically active additive for 10 days, after administration of formalin, the paw volume of experimental animals increased on average only by 37.5-48.7% (p <0.05), and with an increase in the content of oxidized dextran in the cosmetic composition, the anti-inflammatory effect is also enhanced, as evidenced by the lesser severity of edema.

Additionally, the anti-inflammatory properties of the tested samples were studied on a model of erythema caused by UV irradiation of a 2 × 2 cm skin area in 45 albino guinea pigs. The tested compositions in the amount of 0.5 g were applied and rubbed until completely dry on the shaved area of the skin 1 hour before UV irradiation and 1 hour after UV irradiation. Cutaneous erythema induction was induced using UV radiation with a wavelength of 290-320 nm. The degree of erythema that occurred was evaluated after 24 hours on a 5-point scale. The results are presented in the table.

From the presented data it is seen that the concentration of oxidized dextran in the cosmetic composition is less than 0.5% significantly reduces the anti-inflammatory properties of the claimed biologically active additives. At the same time, the concentration of oxidized dextran in excess of 5.0%, regardless of its average molecular weight, may make it difficult to obtain stable emulsions such as oil / water and water / oil (the effect of coagulation and delamination of creams and emulsions). Thus, the claimed range of concentrations of oxidized dextran is optimal, and the claimed range of average molecular weights of oxidized dextran is determined by its availability, as it is produced in industrial volumes.

The study of the immunomodulatory action of the claimed dietary supplement was carried out according to the known method (Chernushenko EF, Kolosova LS Immunological studies in the clinic. Kiev, 1978).

The inventive dietary supplement was applied to the skin of 30 adult non-linear male rats on a normal diet daily for 45 days at a concentration of 0.5% (n = 10) and 5.0% (n = 10). As a control, 0.85% NaCl solution (saline; n = 10) was applied to animals. After this period, animals were sampled and the phagocytic activity of neutrophils was studied. The phagocytic index (PI) and the percentage of phagocytosis (F) were analyzed. FI when using a 0.5% aqueous solution of the inventive dietary supplement was 8.3 ± 0.3, when using a 5.0% solution - 24.5 ± 0.8, in the control - 1.8 ± 0.7 . The percentage of phagocytosis when using a 0.5% aqueous dietary supplement solution was 79.5 ± 6.3, when using a 5.0% aqueous solution - 96.7 ± 4.6, in the control - 45.4 ± 6.3 .

The leukocyte phagocytosis indicator is one of the criteria for assessing the body's resistance to infections. Phagocytes are the most important component of the body's immune defense. Thus, the claimed dietary supplement, increasing the phagocytic index and the percentage of phagocytosis, demonstrates an immunostimulating (stimulating phagocytosis) effect.

The novelty of the claimed technical solution follows from the following:

1. The immunoactive properties of dextran, including its oxidized forms, are known only for its parenteral route of administration, and it is not obvious that when applied topically, the oxidized forms of dextran will have anti-inflammatory properties and stimulate phagocytosis.

2. With the selected technological parameters, cosmetic compositions containing the inventive biologically active additive have a distinct local anti-inflammatory effect.

3. The anti-inflammatory properties of the claimed biologically active additives are manifested regardless of the type of cosmetic composition in which it is included (creams, lotions, masks, etc.)

The proposed biologically active additive based on oxidized dextran expands the range of anti-inflammatory components for the cosmetic industry and gives practical results for use in cosmetics, expressed in the acquisition of therapeutic and preventive properties by cosmetics.

Table No. Experience Series The thickness of the paws of experimental mice, mm (M ± m) The magnitude of the edema,% of ref. UV erythema, points Before administration of formalin solution 4 hours after the introduction of formaldehyde solution one Cream with oxidized dextran, m.M. 35 kDa, the content of 0.5 wt.% (Composition according to example 1) 2.34 ± 0.19 3.7 ± 0.2 * 48.7 four 2 Oxidized Dextran Lotion, M.M. 70 kDa, content of 2.5 wt.% (Composition according to example 4) 2.3 ± 0.07 3.4 ± 0.16 * 47.8 3 3 Cream with oxidized dextran, m.M. 70 kDa, the content of 5.0 wt.% (Composition according to example 1) 2.2 ± 0.07 2.95 ± 0.3 * 37.5 one four Oxidized Dextran Lotion, M.M. 35 kDa, the content of 5.0 wt.% (Composition according to example 4) 2.1 ± 0.07 2.9 ± 0.2 * 38.1 2 5 Cream, basic composition (composition according to example 1) 2.2 ± 0.12 3.89 ± 0.4 * 76.8 four 6 Lotion, base composition (composition according to example 4) 2.3 ± 0.07 3.78 ± 0.18 * 64.3 four 7 Control: isotonic sodium chloride solution 2.2 ± 0.07 3.67 ± 0.21 * 66.9 5 8 Control: 0.5% sodium sulfate dextran solution 2.23 ± 0.07 3.9 ± 0.3 * 72.6 four 9 Control: 5.0% sodium sulfate dextran solution 2.3 ± 0.09 3.69 ± 0.28 * 60,4 four

Claims (2)

1. Biologically active additive for the manufacture of cosmetics, containing dextran and a cosmetically acceptable excipient, characterized in that as dextran it contains oxidized dextran with a molecular weight of 35-70 kDa with the following components, wt.%:
oxidized dextran 0.5-5.0 cosmetically acceptable excipient up to 100 2. The dietary supplement according to claim 1, characterized in that as a cosmetically acceptable filler, it contains water, physiological or buffer solution, microcrystalline cellulose.