WO2020055278A1

WO2020055278A1 - Composition against ageing of the intimate area skin

Info

Publication number: WO2020055278A1
Application number: PCT/RS2018/000015
Authority: WO
Inventors: Amira Fazlagic
Original assignee: Amira Fazlagic
Priority date: 2018-09-14
Filing date: 2018-09-26
Publication date: 2020-03-19
Also published as: RS20181082A1; RS58997B1; EP3849672A1

Abstract

The present invention relates to a cosmetic agent, a composition against ageing of the intimate area skin, as well as the use of the composition. Active ingredients of the composition are encapsulated in liposomes.

Description

Composition against ageing of the intimate area skin

Description of the invention

The present invention relates to a cosmetic agent, a composition against ageing of the intimate area skin, and the use thereof. The present invention belongs to the following classes of the International Patent Classification A6lKlb, A61K8/14, A61Q19/08, A61Q90/00,

A61Q19/00.

Technical problem

A technical problem solved by the present invention is the obtaining of a composition intended for intimate area skin care and prevention of ageing, i.e. loss of elasticity. The present invention provides a pH value of the intimate area of 3.8-4.5, provides a reduction of the possibility of infection, an increase in the sensation of skin hydration, facilitation of intimate relations, depigmentation.

Background art

European Patent No. EP2648739 relates to a multi-purpose gel for the dryness of the vagina with direct and delayed effect. The gel comprises colostrum fraction enriched with immunoglobulin, growth factors, chemotactic factors, and antimicrobial/antiviral factors. This gel is used in the treatment of vaginal dryness and an anti-ageing effect is not indicated.

The International Patent Application Publication WO 2017/069793 relates to the compositions of the vaginal gel and methods for use thereof. The gel listed in this international application solves the problem of vaginal dryness. The anti-ageing effect is not attributed to the gel, but is indicated only as one of the effects of vitamin E. This application addresses the problem of vaginal dryness by a viscous pharmaceutical composition containing a water-soluble gel containing niacin and/or L-arginine. L-arginine is listed as an ingredient or as an alternative ingredient of the gel.

In the art, there are vaginal preparations used for the treatment of vaginal dryness, but none of them deals with the problem of ageing of the intimate area. The preparations of the prior art are applied vaginally, while the composition according to the present application is applied to the skin of the intimate area outside. Treatment that involves the application of the composition to the intimate area outside, rather than vaginal application, is more acceptable to women. The present composition prevents changes in the skin, thereby contributing to improved circulation, reduced pigmentation, skin hydration, and through circulation, gives effects in the vagina. The composition according to the present application prevents the skin from thinning by stabilizing the DNA strands of the skin cells and by stimulating microcirculation with antimicrobial activity and under the conditions of a well-defined pH value (pH 3.8-4.5). Also, none of the preparations known in the art has this specific combination of ingredients. This composition provides the pH value of the intimate area of 3.8-4.5, thus reducing the possibility of infection, in addition, the sensation of skin hydration increases, intimate relations are facilitated, depigmentation is achieved. The pH value of female intimate area increases, by ageing, up to pH 6. The present composition affects the alteration of the pH of the intimate area skin by readjusting the pH to the optimal value i.e., 3.8-4.5, preferably 4.0-4.4.

The composition can be used for showering (cleanses the skin, hydrates the skin...), instead of the lubricant, it reduces scar tissue and has a hypoallergenic effect.

Different clinics around the world are dealing with anti-ageing treatment of the intimate zone, but they address the issue by surgical procedures or by injecting, for example, hyaluronic acid.

In the art, there is no anti-ageing treatment that is non-invasive. Also, when the treatment is less invasive, it is more likely that it will be accepted by women. There are no defined intimate area skin care preparations on the market, and in particular, there are no preparations with these active substances in the liposomal form in one preparation with arginine concentration up to about 20%.

The present invention advantageously avoids the leakage effect of the composition, since the composition is not in the form of an aqueous solution, but is enclosed by liposomes.

Disclosure of the invention

The term "intimate area/zone" refers to the female external reproductive organs and the perineum, i.e. labia majora and labia minora, the clitoris, the vaginal opening and the perineum.

The skin of an intimate area that includes the female external reproductive organs has a number of specificities and specific issues that are expressed only in this area. This area of the skin has its own specific pH of 3.8-4.5 which is lower than the pH of the other parts of the skin, in order to represent defense against various infections. Also, in this zone, epithelium alters from the keratinized stratified squamous, to the stratified squamous, and that line of epithelium alteration represents the risk point for the action of adverse agents, toxins and microbes. This area of the skin is highly exposed to mechanical lesions and damage of the surface parts of the skin. Every use of toilet, every sexual relation, produces small micro- lesions that disrupt skin pH and structure, resulting in loss of advantageous properties of the skin, such as elasticity, hydration and compactness. The childbirth itself involves the creation of serious and unpleasant scars in this zone, and so far there was no continuous treatment upon the completion of the healing phase available for these scars. Alteration of skin properties of this zone, i.e. ageing thereof, pH alteration and the reduction of thickness and elasticity lead to a direct negative impact on the female reproductive and general health. The present treatment provides optimal pH and serves as the first defense against infections, and active ingredients that are incorporated into phospholipid liposomes lead to increased tissue circulation, considerable elimination of free radicals in cells, stabilization of DNA strands of the cells and high hydration. These improvements of skin metabolism in this area results in cessation of feeling of dryness, reduction of infections, and leads to easier and more pleasant sexual relations.

Adverse factors such as micro-lesions, difficult maintenance of the pH of the intimate area, exposure to infections, scars, all affect the intimate area skin and lead to faster ageing thereof.

This composition provides the pH value of the intimate area of 3.8-4.5, thus reducing the possibility of infection, in addition, the sensation of skin hydration increases, intimate relationships are facilitated, depigmentation is achieved. By ageing, the pH value of female intimate area increases up to pH 6. The present composition affects the alteration of the pH of the intimate area skin by readjusting the pH to the optimal value i.e., 3.8-4.5, preferably 4.0- 4.4.

The problem of the present invention is solved by a composition comprising: L-arginine, turmeric, hyaluronic acid or a salt thereof, lactic acid and vitamin E as active ingredients encapsulated in liposomes.

The present composition may further comprise lecithin, glycerol and/or one or more preservatives, e.g., potassium sorbate and/or sodium benzoate.

The present composition may additionally contain vitamin C, niacin and/or lysine. In our product, L-arginine, a white turmeric derivative, hyaluronic acid or a salt thereof, lactic acid and tocopherol (vitamin E) are present.

The present composition contains up to about 20% arginine, which is accomplished by the use of liposomes within which the active substances of the present composition are contained. The use of liposomes allows the active ingredients to reach the stratum comeum of the skin, rather than the circulation.

In a preferred embodiment, the composition is in the form of a gel.

The effect of L-arginine on the skin has been confirmed by many scientific papers and it has been found that it stimulates circulation in the skin, stimulates the growth hormone effects, stimulates fibroblasts and prevents skin thinning. It also prevents the action of free radicals before they damage the DNA strand, thereby prolonging the life of the cells. L-arginine also helps in wounds healing and is used in some cosmetic treatments for facial skin care, but what makes our preparation unique is the L-arginine concentration of about 20%, which is not present in any known skin care product.

It has been proven that Turmeric has an effect on the prevention of pigmentation of the skin, has significant antimicrobial effect and is one of the strongest antioxidants.

Hyaluronic acid is known and widely used in cosmetics as an important skin hydration factor and collagen stimulator.

Tocopherol is a very common ingredient in the preparation that increases the activity of the enzymes in skin cells, hydrates skin and has an antioxidant effect.

Lactic acid is very important in this preparation because it enables achieving ideal pH, but it also has a positive effect on the exfoliation of dead skin layers, the reduction of pigmentation and the strengthening of the skin texture.

The inventors of the present invention incorporated all of these ingredients into phospholipid liposomes which were used as carriers of the active substances. Phospholipid liposomes have the same structure as the cell membrane, so they adhere to it, and have the effect of preventing the loss of water from the cells. Also, their structure allows the transport of active substances into the deeper layers of the skin where they actually achieve their biological activity and allow large molecules, such as hyaluronic acid, to be absorbed and transported through the cell membrane which is otherwise impossible to achieve by other types of carriers. As will be further described in the examples section, the present composition represents a combination of ingredients that gives a synergistic effect over to the individual ingredients in relation to the following biophysical parameters of the subjects skin: EC-as measure of skin moisture, TEGV-trans-epidermal water loss as a measure of barrier properties of the skin, the surface lipid content, El-erythema index, and MI-melanin index.

Detailed description of the invention

Example 1

A composition against ageing of the intimate area skin was prepared in the form of an intimate liposomal gel with the following composition: Ingredients per 50 CC (All material is of food quality grade)

The ingredients from the above table are incorporated in liposomes. Liposomes were formed automatically by mixing phospholipids from lecithin with a solution of L-arginine in water. The system was formed using high shear mixing and high pressure production processes. (source: Liposomes, a practical approach, edited by Vladimir P. Torchilin et al, Oxford university press, second edition). Example 2

The liposomal intimate gel described in Example 1 was applied to women aged 25 to 70 years in the gynecological ordination Medison plus, Belgrade, Serbia, under the control of Dr Sci med. Amira-Mima Fazlagic. Over the course of two years, this gel was tested in 80 women and in the younger group there was a significant improvement of the blood circulation sensation in the intimate area and the improvement of sensitivity during intimate relations, and in the older group there was a significant increase in the hydration and the blood circulation sensation in the intimate area. In the group of women from 55 to 70 years, after the regular use of the preparation, the tissue quality improved and the intimate relationships that were previously impossible due to dryness were enabled.

The study was carried out in the Medison plus ordination in Zemun between October 2016 and January 2018. There were selected 80 gynecologically healthy women, sexually active, of different lifespan, who used the preparation daily for 30 days, and subsequently the control examination was performed and they filled out the questionnaire. The pH of the intimate area skin was tested before and after 30 days from the beginning of the use of the preparation. The pH was measured at the vagina opening (introitus) using the pH control gloves CarePlan VpH from manufacturer INVERNESS MEDICAL GMBH.

Optimal pH of the intimate area skin is 4.0-4.4.

Number of subjects by age groups who had an optimal pH at the beginning of the study, expressed in percentages:

The total number of subjects of all age groups with normal pH before the use of the preparation was 30.

The total number of subjects with normal pH of the intimate area skin after 30 days of daily use of the preparation was 66 (Fig. 1). Number of subjects by age groups with normal pH of the intimate area skin after 30 days of daily use of the preparation: A sensation of better hydration of the intimate area skin after 30 days of daily use of the preparation by age groups:

A graphic representation of the sensation of better hydration after 30 days of use of the preparation is given in Fig. 2.

The total number and percentage of subjects of all age groups in relation to sensation of better hydration of the intimate area after 30 days of daily use of the preparation: Fig. 3.

Improvement of the quality of intimate relations after 30 days of daily use of the preparation is shown in Fig. 4 and in the following table, which contains the number and percentage of women with improvement of the quality of intimate relations. At the beginning of the study, of all 80 subjects, 30 had normal pH of the intimate area skin (4.0-4.4), representing 37.5% of the total number. After 30 days of daily use of the preparation, 82.5% of all subjects had normal pH of the intimate area skin. This result shows a statistically significant change in the achievement of normal pH by using the preparation. The most pronounced effect was achieved in older age groups where, due to loss of estrogen, the greatest problem with optimal pH value occurs. The sensation of better hydration of the intimate area skin after 30 days of daily use of the preparation with the descriptive grade "slight" and "significant" was determined in 63 subjects, i.e. in 79% of subjects, of which 33 experienced "significant" improvement, i.e. 41%. These data show great statistical significance. The study of the improvement in the quality of intimate relationships after 30 days of daily use of the preparation showed that 64 subjects experienced "slight" and "significant" improvement in the quality of intimate relationships, which makes 80% of the total number of subjects, of which "significant" improvement experienced 26 subjects, i.e. 32.5%. These results also indicate great statistical significance.

This study showed that the use of the present preparation brings significant positive qualitative changes for the intimate health of women and the improvement of the overall quality of life.

Example 3

Examination of efficacy of the preparation on the healthy skin of the subjects-volunteers by prof dr. Jvana Arsic, Faculty of Pharmacy, University of Nis

The efficacy was studied after the application of the preparation on the healthy skin of the subjects-volunteers.

A long-term study of the efficacy of the preparation on healthy skin was carried out (4 weeks of application).

In vivo testins of efficacy on healthy skin

In vivo testing of the efficacy of the samples was performed in a long-term, double-blind study by measuring the biophysical parameters of the skin of the subjects (EC-as measure of skin moisture, TEGV-trans-epidermal water loss as a measure of barrier properties of the skin, the surface lipid content, El-erythema index and MI-melanin index ). Study protocol

The study included healthy subjects. The study was conducted in August and September 2018.

Subjects were told not to use any skin care products in the examined area (skin of the inner side of the forearm) in the course of the study, nor one week before the start of the study. The tested preparation was applied, as well as a preparation containing individual active principles at the same concentration as the tested product.

After the initial measurement (before the start of the study, basal values), the volunteers were instructed to apply the preparation at home once a day, in the evening, after showering on the area of the marked skin surface for 4 weeks. Measurements were made before the start of the application (basal values), as well as after 1, 2, and 4 weeks of application. Also, the measurements were made 4 days after completing the application.

In accordance with the obtained results, we conclude that the investigated preparation statistically significantly increases the skin moisture after 7 days of application (in relation to the basal value) and the hydration level is maintained at a statistically significant level throughout the test period (4 weeks of application). All the time during the test period, the preparation had a statistically significant effect on TEGV in terms of its decrease in relation to basal value, which indicates a positive effect on the barrier properties of the skin. The surface lipid content is increased on the skin treated with the tested preparation from the 7^th day of application, during the entire period of administration, indicating the formation of a thin phospholipid film on the surface of the skin as a result of the application of liposomes to the skin. The increase in MI and El indicates the anti-irritant effect of the examined preparation. All the measured parameters showed statistically significantly better results for the examined preparation compared to the preparations containing individual active principles, significantly better results than a sum of the effects of individual preparations, indicating the synergistic effect of the selected active principles.

Claims

1. A composition comprising L-arginine, turmeric, hyaluronic acid or salt thereof, lactic acid and vitamin E encapsulated in liposomes.

2. The composition of claim 1, characterized in that it additionally comprising lecithin, glycerol and/or one or more preservatives, e.g., potassium sorbate and/or sodium benzoate.

3. The composition according to any one of the preceding claims, characterized in that it comprises up to about 20% L-arginine.

4. The composition according to any one of the preceding claims, characterized in that it comprises the following ingredients incorporated in liposomes:

INGREDIENT AMOUNT PER 50 CC PERCENTAGE

L-Arginine HC1 10 g 20%

(contains 83% L-arginine)

Lecithin (GMO-free Soy) 10 g 20%

Glycerol 7 g 14%

Tetrahydrocurdrocurcuminoids 500 mg 1%

(or Tetrahydrodiferuloylmethane)

Sodium hyaluronate 100 mg 0,2%

Potassium-sorbate (preservative) 100 mg 0,2%

Sodium benzoate (preservative) 50 mg 0,1%

Alpha-Tocopherol (antioxidant) 0,001% 0,001%

Lactic Acid QS QS

Water (aqua purificata) ad 50 CC ad 100%

5. The composition according to any one of the preceding claims, further comprising vitamin C, niacin and/or lysine.

6. The composition according to any one of the preceding claims, characterized in that it is in the form of a gel.

7. The use of the composition according to any of the preceding claims for the cosmetic treatment of the intimate area.

8. The use according to claim 7 against the ageing of the intimate area.

9. The use according to claim 7 for achieving a pH 3.8-4.5 of the intimate area.

10. The use according to claim 9 for achieving a pH 4.0-4.4 of the intimate area.

11. The use according to claim 7 against the pigmentation of the intimate area skin.

12. The use according to claim 7 as a lubricant for the intimate area.