RU2252015C1 - Preparation for biological skin rejuvenation - Google Patents

Abstract

FIELD: cosmetology.

SUBSTANCE: the present innovation deals with preparations that improve the state of patient's skin. The suggested preparation for biological skin rejuvenation contains emulsion of perfluorocarbons and organosilicon compound, at their ratio being (30:70) to (70:30) vol.%, moreover, one should, also, apply the mixture of organosilicon compounds. The suggested preparation enables to affect deep and surface layers of skin for persons of any age groups and it shifts metabolic processes in cutaneous tissues towards the predominance of those processes that are peculiar for juvenile tissues.

EFFECT: higher efficiency of rejuvenation.

2 cl, 10 ex

Description

The invention relates to the field of cosmetology and dermatology and relates to cosmetic preparations that improve the condition of the skin.

Numerous cosmetic preparations intended for skin care are known, which have a different composition and have a beneficial effect on the skin, improving metabolic processes in the skin tissues and slowing down the aging process.

Described, in particular, a cream for dry skin containing spermaceti, wax, cocoa butter, lanolin, soybean oil, mayonnaise, distilled water. When using this cream, the skin becomes smooth, acquires a more youthful and fresh look, and the emerging wrinkles are smoothed out. The use of this cream is especially effective for the age group of 25-35 years (RF patent No. 2034588, class A 61 K 7/00, 1995).

A cosmetic product is proposed that contains wax, anhydrous lanolin, soybean oil, paraffin, diluted lactic acid, lavender oil and distilled water, which helps restore skin turgor, smooths wrinkles, acquires a healthy, fresh look, which was most pronounced in people aged 35-42 years and to a lesser extent in people of a more mature age (RF patent No. 2034530, class A 61 K 7/00, 1995).

The aforementioned cosmetics, as well as a number of other cosmetic preparations of a similar action, contribute only to visually noticeable, favorable changes in the physical condition of the skin, manifested in a decrease in the number and severity of wrinkles, in the acquisition of a skin with a healthier color and appearance inherent in younger skin, and their use is less effective for adults. The described sources do not contain an indication of a change in skin tissues under the influence of the described means of any biological indicators associated with age-related changes, and do not speak of the physiological effect of rejuvenation.

It is known a cosmetic product containing a stabilized emulsion of perfluorocarbons, which, when exposed to skin tissue, along with other beneficial effects determined by the specific composition of the product, causes biochemical changes that lead to a shift in the metabolic processes occurring in the skin tissues, towards the predominance of processes characteristic of the tissue physiologically younger age (RF patent No. 21979790, class A 61 K 7/00, 1996).

One of the disadvantages of the described perfluorocarbon emulsion is the high volatility of the main component, perfluorocarbons. Therefore, when applying a well-known cosmetic product to the skin at the first stage, perfluorocarbons penetrate the upper layers of the skin, after which part of the perfluorocarbons evaporates, cooling the skin surface and reducing the biological activity of the drug, while the remaining part penetrates into the deeper layers of the skin, where perfluorocarbons manifest its positive properties.

The scientific, technical and patent literature describes a large number of emulsions of organosilicon compounds obtained using various emulsifiers. As well as perfluorocarbon emulsions, they have the ability to supply oxygen to the skin. Describes a tool for the treatment of all types of baldness and skin regeneration, including chloromethylsilatran, dimexide and vegetable oil (RF patent No. 2097017, class A 61 K 7/06, 1997). It is noted that the product has regenerating, whitening properties, improves trophism, skin elasticity. Mentioned cosmetic product, as well as the first two, contributes only to visually noticeable, favorable changes in the physical condition of the skin.

The applicant has not found sources of information that would indicate the use of emulsions of organosilicon compounds alone or in combination with other products as a means for biological skin rejuvenation.

The disadvantage of all emulsions of organosilicon compounds is the difficulty in obtaining a stable emulsion with particle sizes less than 2 microns, since the large particle size (over 2 microns) adversely affects the stability of the emulsions and their effectiveness. In particular, to obtain an emulsion of MIRASIL DME 2 organosilicon compounds, a special emulsion stabilizer was used, a natural succinoglycan biopolymer — a polysaccharide obtained by fermentation of microorganisms “Agrobacterium tumefacient”, which made it possible to obtain an emulsion in combination with standard emulsifiers such as sodium laureth sulfate with a particle size of 2 μm (Prospectus of the company "Rhodia", France, 1998).

The objective of the present invention is to develop a cosmetic product for the biological rejuvenation of the skin with a stable composition with increased effectiveness due to the simultaneous effect on the deep and surface layers of the skin, which would be equally effective for people of any age groups.

The problem was solved as a result of research conducted by the applicant, which showed that such a tool for biological skin rejuvenation is a cosmetic product containing an emulsion of perfluorocarbons and organosilicon compounds in effective amounts.

Moreover, as shown by the applicant’s studies using a highly sensitive thermal imaging technique, when exposed to the skin of the proposed cosmetic product, it is distributed evenly over the entire depth of the skin due to the rapid penetration of perfluorocarbons into the deeper layers of the skin and the action of organosilicon compounds exclusively in the surface layers of the skin.

According to the applicant, the different penetration depths of the components can be explained by the different hydrophobicity of perfluorocarbons and organosilicon compounds (perfluorocarbons are more hydrophobic), and hydrophobicity is one of the main characteristics that affect the distribution of matter in the stratum corneum (Arct J., Gronwald M., Kasiura K Possibilities for the prediction of an active substance penetration through epidermis. IFSCC Magazine 2001; 4 (3): 179-83).

In addition, as the studies of the applicant have shown, when exposed to the skin of individuals of different age groups, the proposed cosmetic product can have an equally effective, but different in nature effect, which is determined mainly by the corresponding ratio of perfluorocarbons and organosilicon compounds in it.

So, for persons of the age group of 25-35 years, it is preferable to affect the surface layers of the skin and, accordingly, the increased content of organosilicon compounds in a cosmetic product, and the above ratio is ~ 30: 70 vol. %, which provides a stable effect of reducing skin wilting and preventing aging.

For persons of the age group of 45-55 years and older, preferably a higher content of perfluorocarbons in the cosmetic product to enhance the effect on the deeper layers of the skin, and the above ratio is ~ 70: 30 vol. % In this case, the rejuvenation effect for more mature skin is more pronounced and occurs sooner, which is probably due to the fact that perfluorocarbons possess not only oxygen transport, but also other positive biological properties, for example, membranotropic ones (E.I. Maevsky, “Perfluorinated carbon in biology and medicine ”, Pushchino, 1981, 76-92).

In this case, the emulsion of perfluorocarbons and organosilicon compounds refers to physicochemical dispersed systems.

As an emulsion of perfluorocarbons and organosilicon compounds, an emulsion of both individual perfluorocompounds and individual organosilicon compounds, and an emulsion of several perfluorocompounds and several organosilicon compounds, as well as mixture variants, can be used.

An emulsion of perfluorocarbons and organosilicon compounds is prepared as follows.

Perfluorocarbon (or a mixture of perfluorocarbons) and an organosilicon compound (or a mixture thereof) and water are mixed with an emulsifier solution, for example proxanol (a block copolymer of ethylene and propylene oxides). The mixture is intensively mixed in an ultra-mixer (type Ultra-Turex). The resulting mass is homogenized in a high pressure homogenizer at a pressure of up to 600 atm. The perfluorocarbon portion of the mixture may include perfluorinated aliphatic and cyclic hydrocarbons, perfluorinated amines, perfluoropolyesters, perfluorooctyl bromide, or mixtures thereof. The boiling point of perfluorocarbons is 150-200 ° C. The organosilicon part of the mixture may include cyclomethicones, dimethicones, mixtures thereof or other organosilicon compounds with a boiling point above 100 ° C.

As a preservative, Germaben-2 can be used in an amount of 0.8-1.0%.

The concentration of emulsifier - a block copolymer of ethylene oxide and propylene (proxanol) is usually 3-10%. The ratio of perfluorocarbons and organosilicon compounds in the mixture can vary over a wide range from 90-10 to 10-90 vol.%. The concentration of the mixed emulsion introduced into the cosmetic is usually 30-70 vol.% (Preferably 50-60 vol.%). The particle size of the emulsion in this case is 0.1-0.3 microns.

The resulting emulsion is a white creamy stable mass, which when diluted with water 10 times gives a clear opalescent liquid of a bluish color, which further confirms the submicron dimensions of the emulsion.

Water emulsions of a mixture of perfluorocarbons and organosilicon compounds can be most widely used, but other media, for example, glyceric or water-glyceric ones, can also be used.

As you know, one of the main indicators affecting the effectiveness of the emulsion used for cosmetics is the oxygen content in it.

Table 1 shows the oxygen content in the emulsions studied by the applicants (studies were carried out using a Lexington, USA, LEXO2-CON-T volumetric oxygen analyzer at a temperature of 37 ° C and an oxygen barometric pressure of 735 mm Hg).

The following emulsions were studied.

No. 1

A mixture of perfluorocarbons:

Perfluorodecalin (PFD) 59.5 ml

P-216 perfluoropolyether (PE) 10.5 ml

Emulsifier (Proxanol P-268) (BS) 7.0 g

Preservative (Hermaben-2) 1.0 g

Water up to 100 ml

Number 2

Organosilicon compound -

Dimethicone (DM) 70.0 ml

Emulsifier (Proxanol P-268) 7.0 g

Preservative (Hermaben -2) 1.0 g

Water 100 ml

No. 3

A mixture of perfluorocarbons:

Perfluorodecalin 29.8 ml

P-216 perfluoropolyether 5.7 ml

Organosilicon compound -

Dimethicone 35.5 ml

Emulsifier (Proxanol P-268) 7.0 g

Preservative (Hermaben -2) 1.0 g

Water 100 ml

Number 4

A mixture of perfluorocarbons:

Perfluorodecalin 40.0 ml

Perfluorotripropylamine 10.0 ml

Organosilicon compound -

Cyclomethicone 20.0 ml

Emulsifier (Proxanol P-286) 10.0 g

Preservative (Hermaben -2) 1.0 g

Water up to 100 ml

Number 5

Perfluorodecalin 49.0 ml

Dimethicone 21.0 ml

Emulsifier (Proxanol P-268) 7.2 g

Preservative (Hermaben-2) 1.0 g

Water up to 100 ml

Number 6

Perfluorodecalin 21.0 ml

Dimethicone 49.0 ml

Emulsifier (Proxanol P-268) 7.2 g

Preservative (Hermaben-2) 1.0 g

Water up to 100 ml

As can be seen from the data in table 1, the oxygen content in the mixed emulsions No. 3, 4, 5, and 6 remains high and varies depending on the ratio of perfluorocarbons and organosilicon compounds.

In order to confirm that the use of mixed emulsions of perfluorocarbons and organosilicon compounds in cosmetic products shifts the metabolic processes in the skin tissues more sharply towards the predominance of processes characteristic of tissues of a younger age, and this shift is faster and more pronounced for mature skin, the applicant The effect of perfluorocarbon emulsions, emulsions of organosilicon compounds and mixed emulsions on the state of collagen fibers in the skin of rats of different ages was studied.

Emulsions No. 1-6 were applied over 30 days to certain areas of the skin of the tail of rats of three age groups (2, 5, 15 months). At least 10 animals were represented in each group. Collagen was isolated from tails by a known method, which was dissolved in 0.5 M acetic acid and the process of collagen fibril melting was studied using differential scanning calorimetry (DSC).

Collagen - (from Greek kolla - glue, genes - giving birth) - fibrillar secretory protein, the main structural component of connective tissue - skin, bones, ligaments, tendons, blood vessel walls.

Collagen forms fibers that intertwine like threads in tissue and create a framework into which new cells can grow. In this way, the firmness and elasticity of body tissues, including skin, is ensured.

Collagen undergoes the aging process in the body over time, due to the formation of cross-links between its fibers. Due to these transverse bridges, collagen is gradually broken down. Cross-links are stable, interfere with the natural breakdown and renewal of collagen fibers, reduce their flexibility, elasticity and elasticity. Aging, diseases and injuries enhance these processes, which primarily affect the skin, which is manifested in its wrinkled and flabby appearance.

In studies, a temperature range was determined in which collagen melts and the parameter T _{1/2 is} calculated, which characterizes the number of cross-links and increases with age. The results are presented in table 2.

An analysis of the data obtained allows us to conclude that the use of mixed emulsions compared with emulsions containing perfluorocarbons and emulsions containing organosilicon compounds more sharply shifts the value of the parameter T _1/2 towards indicators characteristic of younger skin, and this the shift is more pronounced for older animals. Moreover, mixed emulsions with a high content of perfluorocarbons are preferably used for more mature skin.

To assess the intensity of biochemical processes in the skin, the intensity of incorporation of labeled ³ H-thymidine into rat skin cells was studied, which reliably reflects the severity of DNA biosynthesis (cell division). The results are shown in Table 3. It is possible to note a decrease in the intensity of DNA synthesis with the age of the animals and a significant and sharper shift of this indicator for mixed emulsions compared to other studied emulsions in the direction of the characteristic for younger animals. Moreover, emulsions No. 4 and No. 5 show a more pronounced shift for more mature skin.

Table 4 presents the dynamics of changes in the synthesis of basic proteins, which most adequately reflects the physiological state of skin tissue. For this purpose, the inclusion of ³ H-amino acids in vivo and ¹⁴ C-amino acids in vitro into the skin tissue was evaluated.

For this purpose, 0.2 ml of emulsion was applied to the hairless area of the skin of rats with an area of 5 cm2 for 30 days, then labeled amino acids were injected into the animals and the necessary parameters were determined. From the results it follows that with age, changes in the intensity of protein biosynthesis occur. However, the use of cosmetics containing an emulsion of perfluorocarbons and organosilicon compounds shifts these indicators to values characteristic of a physiologically younger age. Moreover, this shift is sharper compared to emulsions containing pure perfluorocarbons or pure organosilicon compounds. In mixed emulsions, changes occur in different ways: an increase in the content of perfluorocarbons (emulsions No. 4 and 5) leads to more effective changes in the skin of animals of a more mature age, and an increased content of the organosilicon fraction (emulsions No. 3 and 6) is more effective for young skin.

Figure 1 shows in graphical form the data presented in table 3. It can be seen that the greater the absolute value of the changes in the intensity of synthesis during aging, the faster the skin ages. Given this, we can recommend emulsions No. 3, 4, 5, with a higher content of perfluorocarbons for mature skin, and emulsion No. 6 with a high content of organosilicon compounds - for young skin.

Cosmetics prepared on the basis of a mixed emulsion may or may not contain any additional biologically active substances. In other words, the appropriate product can be intended either exclusively for biological rejuvenation of the skin, or it can exhibit other useful qualities along with this effect, depending on the known properties of biologically active substances of different directions added to the composition of the product. In particular, vitamin preparations or other substances that positively affect the metabolic processes in the skin tissues and enhance the anti-aging effect can be introduced into the composition of the product.

On the other hand, excipients such as antioxidants, stabilizers, colorants, flavors, and the like may also be included in the composition of the product with mixed emulsions.

Using a thermal imaging technique, the effect of emulsions containing perfluorocarbons, emulsions containing organosilicon compounds and mixed emulsions on the penetration of biologically active substances into the skin tissue was studied.

Finalgon, a vasodilator and local heating agent, was used as a biologically active substance. Studies were performed on volunteers (3 women and 2 men). The inner side of the forearm of both hands was examined, since this surface has the most stable mechanical and temperature parameters. At the same time, the reaction of the skin and blood vessels was recorded.

The studies were carried out using a thermal imaging system with a spatial resolution of 320 × 240 elements along the image field, with a sensitivity limited by temperature noise of no worse than 0.02 ° C, in the range from 10-50 ° C, the measurement speed was 25 frames per second. Digital data was recorded in real time.

Figure 2 shows a graph of the effect of the composition of the emulsions on the penetration of biologically active substances into the skin.

The studies recorded the nature of the changes in time that occur when applying finalgon to the skin in the following cases:

- row 1 - emulsion No. 3 (control) without finalgon

- row 2 - emulsion No. 1 + finalgon

- row 3 - pure ointment of finalgon (control)

- row 4 - emulsion No. 2 + finalgon

- row 5 - mixed emulsion No. 3 + finalgon

As can be seen in the graph (despite the differences in the types of skin, age and gender of the subjects, the type of curves is identical), the use of mixed emulsions contributes to a greater increase in skin temperature, which indicates the effective penetration of biologically active substances into the skin, and, therefore, we can most likely assume enhancing the action of other biologically active substances traditionally introduced into cosmetics of this orientation.

The essence of the proposal is illustrated by the following examples, which should not be construed as limiting the inventive concept.

Example 1. To a mixture of 240 ml of a 30% solution of Proxanol P-268 and 10 g of the preservative Hermaben-2, 298 ml of perfluorodecalin, 57 ml of P-216 perfluoropolyether and 375 ml of dimethicone are slowly added with vigorous stirring. The volume of the mixture was adjusted to 1000 ml with distilled water and subjected to three cycles of homogenization on a high-pressure homogenizer at a pressure of up to 600 atm. The resulting emulsion is a white, stable, creamy mass.

After periodic application of the emulsion to healthy, but dry, mature skin for a month, the appearance of the skin significantly improved, the number of wrinkles decreased, the skin became more elastic. Dry skin has disappeared.

Example 2. 50 g of the emulsion obtained in example 1 is slowly added to 50 g of a 1% carbopol gel 2010. The mixture is thoroughly mixed, the fragrance is added and mixed again. With periodic application of the obtained gel to the skin affected by neurodermatitis, itching immediately disappeared, subjective sensations improved. After a month's use of the gel, the skin acquired a healthy appearance and color, characteristic of young and healthy skin.

Example 3. 50 g of the emulsion obtained in example 1 is slowly added to a mixture of 30 g of 1% carbopol gel 2010 and a solution of 3 g of oak bark extract in 17 ml of water. Perfume is added and the mixture is thoroughly mixed. Get a cream gel to care for oily skin. After applying the cream gel on the young skin for a month, lipid metabolism improves, the oily sheen disappears, and inflammation and the appearance of acne are prevented.

Example 4. 50 g of the emulsion obtained in example 1 is slowly added to a mixture of 20 g of a 1% carbopol gel 2010 and a fat component containing 2 g jojoba oil, 2 g avocado oil, 4 g of a 20% solution of Proxanol P- 268, 1 g of emulsion wax and 21 g of water. Perfume is added and the mixture is thoroughly mixed. The resulting cream gel is intended to care for dry and normal young skin. After application for a month, skin turgor improves, the skin softens and takes on a healthier and younger look.

Example 5. To a mixture of 240 ml of a 30% solution of Proxanol P-268 and 10 g of Hermaben preservative, 490 ml of perfluorodecalin and 210 ml of dimethicone are slowly added with vigorous stirring. The volume of the mixture was adjusted to 1000 ml with distilled water and subjected to three cycles of homogenization on a high-pressure homogenizer at a pressure of up to 600 atm. The resulting emulsion is a stable white creamy mass and is intended for introduction into cosmetic compositions for the care of mature and aging skin.

Example 6. Dissolve 3 g of a fat-soluble UV-filter of benzophenone-3 in 10 ml of olive oil, to the resulting solution add a solution of 3 g of a UV-filter of benzophenone-4 in 10 ml of water, 10 ml of a 20% solution of Proxanol-P-268, then add 2.5 g of emulsion wax. The mixture is heated with stirring to 80 ° C. The resulting mass is added to a mixture of 40 g of the emulsion as described in Example 5. 3.5 g of titanium dioxide and 24 g of 1% carbopol gel 2010 are added. Perfume is added and the mixture is thoroughly mixed. The obtained photoprotective cream gel has a high SPF factor (more than 25) and provides effective skin protection from sunlight, has low water washability and does not require the use of additional cosmetics, and also allows, despite the action of UV rays, to provide the skin with a healthy look: freshness, firmness and elasticity.

Example 7. To a mixture of 240 ml of a 30% solution of Proxanol P-268 and 10 g of Hermaben preservative, 490 ml of perfluorodecalin and 210 ml of dimethicone are slowly added with vigorous stirring. The volume of the mixture is adjusted to 1000 ml with distilled water and subjected to three homogenization cycles on a high-pressure homogenizer at a pressure of up to 600 atm. The resulting emulsion is a stable white creamy mass and is intended for introduction into cosmetic compositions for the care of mature and aging skin.

Example 8. To a mixture of 240 ml of a 30% solution of Proxanol P-268 and 10 g of Hermaben preservative, 490 ml of dimethicone and 210 ml of perfluorooctyl bromide are slowly added with vigorous stirring. The volume of the mixture is adjusted to 1000 ml and subjected to three homogenization cycles on a high pressure homogenizer at a pressure of up to 600 atm. The resulting emulsion is a stable white creamy mass and is intended for introduction into cosmetic compositions for skin care of a person 25-35 years old.

Example 9. Prepare the fat component by mixing with heating 60 g of a 20% solution of Proxanol P-268, 5 g of pepper oil extract, 5 g of petroleum jelly, 1.6 g of emulsion wax until a homogeneous mass is obtained. To a 500 g gel of carbopol-940 gel is added the fat component, 30 g of alcohol tincture of pepper, 16 g of alcohol extract of kelp, 100 g of the emulsion obtained in Example 7, 0.7 g of cato is added, perfume is added and the mixture is mixed. The total weight is adjusted with water to 1000 g, the pH of the resulting gel for the body with an anti-cellulite effect of 6.5-7.5 (if necessary, correlates with triethanolamine). It is especially effective for middle and mature skin, it shows not only anti-cellulite effect, but also stimulates the metabolism in skin tissues, giving it firmness and elasticity.

Example 10. Mix 25 g of alcoholic extract of birch buds, 30 g of water-alcohol-glycerin extract of wheat germ, 20 g of a 20% solution of Proxanol P-268, 100 g of the emulsion obtained in example 8 and containing 250 ml of dimethicone, 240 ml of cyclomethicone, preservative and perfume are added, adjusted with distilled water to 1000 g. The mixture is mixed and a tonic for normal skin is obtained. Regular use of the tonic to care for young skin prevents its premature aging and ensures its healthy appearance.

According to the applicant, the foregoing allows us to conclude that the increase in the effect of directing and shifting the activity of metabolic processes in skin tissues towards processes characteristic of physiologically younger skin tissues under the influence of mixed oxygen-carrying emulsions was not known and did not follow from a known level of knowledge. Moreover, this shift is sharper compared to emulsions containing pure perfluorocarbons or pure organosilicon compounds. Moreover, in mixed emulsions, changes in the skin occur in different ways: an increase in the content of perfluorocarbons leads to changes in the skin of people of a more mature age, and an increased content of the organosilicon fraction is more effective for young skin.

The applicant has shown and proved that the high efficiency of cosmetics containing mixed emulsions of perfluorocarbons and organosilicon compounds is due to the fact that when exposed to the skin of such cosmetics, they are distributed evenly over the entire depth of the skin due to the rapid penetration of perfluorocarbons into the deeper layers of the skin and the action of organosilicon compounds exclusively in the surface layers of the skin.

Visible persistent manifestations of the true effect of rejuvenation consisted in the prolonged acquisition by the skin of a condition inherent in younger healthy skin. Regardless of the age of the patient who applied cosmetic preparations containing mixed emulsions, and the initial state of the skin, the treated skin areas had the appearance characteristic of tissues of a younger age. It should be especially noted that using various ratios of perfluorocarbons and organosilicon compounds in emulsions, it is possible to effectively achieve a rejuvenating effect for people of any age, which is especially important for young people, since the use of mixed emulsions instead of, for example, currently used perfluorocarbons significantly reduces the cost of cosmetics.

Claims (3)

1. The tool for the biological rejuvenation of the skin containing an emulsion of perfluorocarbons, characterized in that it further comprises an organosilicon compound. 2. The tool according to claim 1, characterized in that the ratio of the content of organosilicon compounds and perfluorocarbons in it is from (30:70) to (70:30) vol.%. 3. The tool according to claims 1, 2, characterized in that a mixture of organosilicon compounds is used.

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