Composition to prevent and / or treat white stretch marks

The use of a composition containing palmitoyl tripeptide-5 addresses the inadequacies of existing treatments for white stretch marks by specifically targeting the lesions' biochemical and histological changes, achieving effective prevention and treatment with minimal side effects.

FR3126876B1Active Publication Date: 2025-04-11LSI SILDERMA LTD
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Patent Information

Application Number
FR2021009660
Authority / Receiving Office
FR · FR
Patent Type
Patents
Current Assignee / Owner
Filing Date
2021-09-15
Publication Date
2025-04-11
Estimated Expiration
2041-09-15

AI Technical Summary

Technical Problem

Existing treatments for white stretch marks are not satisfactory due to their lack of specificity and often result in undesirable side effects, making them unsuitable for all types of subjects, including pregnant women.

Method used

A composition comprising palmitoyl tripeptide-5 as a dermatological active ingredient, which is applied topically or through transcutaneous injection, to prevent and treat white stretch marks by targeting the specific biochemical and histological changes associated with these lesions.

Benefits of technology

The composition effectively prevents the appearance and development of white stretch marks, reducing their surface area and improving their visual appearance, with no observed side effects, making it suitable for all subjects, including pregnant women.

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Abstract

Composition comprising, as a dermatological active ingredient, palmitoyl tripeptide-5, for use in the prevention and / or treatment of white stretch marks
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Description

Title of the invention: Composition for preventing and / or treating white stretch marks Technical field of the invention

[0001] The present invention relates to the field of prevention and / or treatment of stretch marks, more specifically white stretch marks. More particularly, the invention relates to a composition comprising, as dermatological active ingredient, palmitoyl tripeptide-5, for use in the prevention and / or treatment of white stretch marks.

[0002] The present invention also relates to a cosmetic method for applying said composition to prevent and / or treat white stretch marks. Technological background

[0003] Stretch marks are benign skin lesions that appear, for example, during pregnancy, adolescence, or following rapid weight gain, particularly on the stomach, buttocks, thighs or breasts.

[0004] Clinically, two physiological forms of stretch marks are distinguished: red stretch marks and white stretch marks. These physiological forms correspond to different stages of development of the dermal lesion. Red and white stretch marks are characterized by different histological and biochemical characteristics and a different pathophysiological state.

[0005] In the initial evolutionary stage, the erythema is in its acute phase, in the form of red stretch marks.

[0006] Red stretch marks are visible as red or purplish, or even purple, linear streaks on the skin. In fact, red stretch marks are characterized by an increase in microvascularization, which contributes to their red, erythematous color. Histologically, red stretch marks present dermal edema with a predominance of fine dermal elastic fibers, thinning the dermis. Biochemically, red stretch marks are characterized by an alteration of collagen and elastic fibers, highlighting structural changes.

[0007] Over time, the erythema enters the chronic cicatricial phase, in the form of white stretch marks.

[0008] The white stretch mark is visible in the form of atrophic tissue, generating a permanent wrinkled, often linear, hypo-pigmented, depressed and flaccid mark, which is visually close to a scar.

[0009] Biochemically, the appearance of white stretch marks results from a decrease in the expression of genes, such as procollagen type I and III, elastin and fi bronectin, caused in particular by an alteration of the fibroblast mechanism. Indeed, fibroblasts, residents of the dermis, ensure its coherence and flexibility, in particular through the signaling pathway of the growth factor TGF-[3. The latter is the main regulator of the extracellular matrix.

[0010] Histologically, at the level of the epidermis, white stretch marks are characterized by atrophy with loss of epidermal ridges, and a reduction in melanocytes. At the level of the dermis, white stretch marks present collagen and dense elastic fibers, packed and aligned parallel to the dermal epidermal junction, and reduced micro-vascularization leading to their pale color.

[0011] Stretch marks are common, unsightly skin conditions that cause discomfort in those affected.

[0012] This is why it is important to find solutions to treat stretch marks and prevent their appearance or development.

[0013] Several treatments for stretch marks exist today, without distinction between red and white stretch marks, although they are histologically and biochemically different. The lack of specificity of existing treatments, depending on the type of stretch mark, means that these existing treatments are not satisfactory.

[0014] In the current market, we distinguish between mechanical and chemical techniques for treating stretch marks.

[0015] Among the mechanical techniques, we will cite for example micro-dermabrasion, radiofrequency, treatment by fractional laser, diode laser, xenon chloride excimer laser, vascular laser, intense pulsed light, infrared, UV light, but also percutaneous collagen induction therapy, or platelet-rich plasma.

[0016] However, these techniques have several undesirable side effects, including post-inflammatory hyperpigmentation, transient hyperpigmentation, the appearance of erythema, edema, skin intolerance or bruising. In addition, these techniques are not all suitable for all types of subjects, such as pregnant women, who are nevertheless greatly affected by the appearance of stretch marks.

[0017] Among the chemical techniques by topical application, we can cite for example the chemical peel, involving the application of trichloroacetic acid or glycolic acid. However, the chemical peel is not satisfactory for treating stretch marks, in particular white stretch marks. The chemical peel also has undesirable side effects such as post-inflammatory hyperpigmentation. Sometimes, to increase its effectiveness, the chemical peel with glycolic acid is carried out in combination with tretinoin, which is not recommended during pregnancy and breastfeeding. Thus, the chemical peel with glycolic acid combined with tretinoin does not allow to treat all subjects with stretch marks.

[0018] Other chemical compounds, applied topically in combination with skin massage, are known to treat stretch marks in general. Examples include creams containing hyaluronic acid or extracts of Centella asiatica, and the application of sweet almond oil or olive oil. However, to date, the chemical action on stretch marks has not been separated from the mechanical effect linked to repeated skin massage.

[0019] Thus, anti-stretch mark cosmetic compositions, with known chemical action, do not provide full satisfaction in preventing or treating white stretch marks, in particular because of the side effects.

[0020] There therefore remains a need to develop new compositions, to treat and / or prevent the formation and development of white stretch marks, which can be easily used by all types of subjects including pregnant women.

[0021] Description of the invention

[0022] Surprisingly, the Applicant has found that the use of a composition comprising palmitoyl tripeptide-5 makes it possible to overcome the aforementioned drawbacks in order to prevent and / or specifically treat white stretch marks.

[0023] For this purpose, the present invention relates to a composition comprising, as dermatological active ingredient, palmitoyl tripeptide-5, for use in the prevention and / or treatment of white stretch marks.

[0024] The term “dermatological active ingredient” means a compound intended to be applied to the skin and which has biological properties that underlie a physiological effect. The active ingredient is to be distinguished from the “excipients” of the composition.

[0025] The term "excipient" means all compounds which give the composition its physicochemical properties, such as its consistency, its galenic and its capacity to deliver said dermatological active ingredient while being inert with respect to its physiological effect.

[0026] The expression "prevention of white stretch marks" means avoiding the appearance of new white stretch marks on the surface of the skin.

[0027] The expression "treatment of white stretch marks" means limiting their development, growth and extent on the surface of the skin.

[0028] According to a preferred embodiment of the composition of the invention, said palmitoyl tripeptide -5 represents between 0.01% and 0.1%, preferably 0.025% by mass relative to the total mass of the composition.

[0029] Palmitoyl tripeptide-5 has the advantage of being easily formulated into a composition, of being non-cytotoxic, biocompatible and accepted by current cosmetic product regulations. In addition, the action of palmitoyl tripeptide-5, even at concentrations below 0.1%, shows satisfactory results. factants, against white stretch marks, as indicated below.

[0030] According to a preferred embodiment of the invention, the composition comprises as the only dermatological active ingredient, said palmitoyl tripeptide -5.

[0031] Preferably, said palmitoyl tripeptide -5 consists of a valine-lysine-valine tripeptide, it advantageously makes it possible to treat and / or prevent white stretch marks.

[0032] According to a preferred embodiment, the composition used to prevent and / or treat white stretch marks is in a galenic form suitable for topical use. In other words, said composition is in a galenic form which allows the dermatological active ingredient to act locally, by targeting white stretch marks, in particular at the site of application of the composition to the skin.

[0033] Preferably, the composition used to prevent and / or treat white stretch marks is in a dosage form suitable for cutaneous administration. In other words, the composition is administered to the surface of the skin. In this case, the dosage form may be, for example, a cream, a gel, an oil, a lotion, an ointment, a mousse.

[0034] According to another embodiment, the composition, used to prevent and / or treat white stretch marks, is in a galenic form suitable for a transcutaneous route of administration. In other words, the composition is applied through the skin, by subcutaneous injection, for example with a needle containing the composition in liquid form, for example in the form of a solution.

[0035] Preferably, the composition used to prevent and / or treat white stretch marks is in the form of a cream, gel, oil, lotion, solution, ointment, foam, emulsion. This galenic form has the advantage of allowing easy and targeted application to white stretch marks.

[0036] According to a particular embodiment, the composition according to the invention is a cosmetic composition.

[0037] In other words, the invention therefore relates to a cosmetic use of palmitoyl tripeptide -5, as a dermatological active ingredient, for preventing and / or treating white stretch marks.

[0038] According to a particular embodiment, the invention relates to a composition, used to prevent and / or treat white stretch marks, which comprises in mass percentage relative to its total mass, equal to 100%: - between 70% and 80% water; - between 1% and 10% glycerin; - between 1% and 10% caprylic and / or capric triglyceride; - between 1% and 10% of isostearyl neopentanoate; - between 1% and 10% sorbitan stearate between between between 1% and 10% polysorbate 60; 1% and 10% dimethicone; 1% and 10% cetyl alcohol; between 0.5% and 5% pentylene glycol; between 0.1% and 1% beeswax; between 0.1% and 1% chlorphenesin; between 0.1% and 1% sodium benzoate; between 0.1% and 1% alkyl acrylate / C10-30; between 0.05% and 0.5% cymene 5-ol; between 0.01% and 0.1% palmitoyl-tripeptide-5; between 0.001% and 0.01% sodium hydroxide; and between 0.0005% and 0.005% citric acid.

[0039] The present invention also relates to a cosmetic method for the prevention and / or treatment of white stretch marks, according to which a composition according to the invention is applied to the white stretch marks. In the case of application of the composition of the invention by cutaneous administration, a light massage allows its penetration into the different layers of the skin so that the dermatological active ingredient, in this case palmitoyl-tripeptide-5, reaches the epidermis, the dermis, or even the hypodermis. In the case of application of the composition by transcutaneous route, the targeted injection of the composition allows the palmitoyl-tripeptide-5 to be released directly into the epidermis, the dermis, or even the hypodermis.

[0040] According to a preferred embodiment of the cosmetic process of the invention, said composition is applied twice a day, preferably once in the morning and once in the evening, to the white stretch marks, once the skin has been cleansed. Thus, this application method allows the physiological effect of palmitoyl-tripeptide-5 to be obtained on the white stretch marks, both during the day and during the users' sleeping period. Consequently, this dosage makes it possible to be effective over the 24 hours of the day in the prevention and / or treatment of white stretch marks.

[0041] According to another embodiment of the cosmetic process of the invention, an effective amount of said composition of the invention is applied to the white stretch marks.

[0042] The term "effective quantity" means the necessary quantity of the composition to be applied to white stretch marks to obtain a significant physiological effect which prevents their appearance and / or treats them by slowing down their development.

[0043] According to a preferred embodiment, between 0.02 and 0.04 mL of the composition of the invention is applied / cm2 of skin concerned.

[0044] It is clear from the above that the composition comprising palmitoyl-tripeptide-5, advantageously cosmetic, makes it possible to prevent and / or specifically treat white stretch marks.

[0045] Consequently, the composition of the invention makes it possible to prevent the formation and development of white stretch marks. The use of the composition of the invention makes it possible to eliminate the unsightly appearance of white stretch marks and to reduce their growth and extension on the surface of the skin.

[0046] Other characteristics and advantages of the invention will emerge from the detailed description which follows of the non-limiting embodiments of the invention, with reference to the appended figure, in which:

[0047] - [Fig.l] represents the evaluation of the improvement of the dermal surface of the white stretch marks, observed after 30 days, 60 days or 90 days of cutaneous application of the composition according to the invention.

[0048] Example of realization

[0049] In this example, the composition according to the invention, for its use in the prevention and / or treatment of white stretch marks, is of formula 1.

[0050] Formula 1 comprises in mass percentage relative to its total mass, equal to 100%: 75.471426% water; - 5.1% glycerin; - 4% caprylic and / or capric triglyceride; - 3.75% isostearyl neopentanoate; - 3% sorbitan stearate; - 2.5% polysorbate 60; - 2% dimethicone; - 1.5% cetyl alcohol; - 1% pentylene glycol; - 0.75% beeswax; - 0.3% chlorphenesin; - 0.3% sodium benzoate; - 0.2% alkyl acrylate / Cl0-30; - 0.1% cymene 5-ol; - 0.025% palmitoyl-tripeptide-5; - 0.002574% sodium hydroxide, and - 0.001% citric acid.

[0051] In formula 1 above, all compounds are considered as formulation excipients, except palmitoyl-tripeptide-5 which consists of the only dermatological active ingredient.

[0052] Evaluation of the efficacy and tolerance of the application of a cosmetic composition according to the above-mentioned formula 1 for treating white stretch marks

[0053] To evaluate the efficacy and tolerance of application of the composition of the invention, 27 individuals applied, morning and evening, for 90 days, to an area of ​​cleansed skin with existing white stretch marks, either a composition according to the invention or a “placebo” composition.

[0054] In the study protocol, the individuals consisted of both men and women. For each of them, no treatment against their white stretch marks was carried out in the 4 weeks before the start of the study protocol, in order to avoid any interactions or effects linked to previous treatments.

[0055] The cosmetic composition according to the invention is of formula 1 and comprises palmitoyl-tripeptide-5. The “placebo” composition is of formula identical to formula 1, but without palmitoyl-tripeptide-5.

[0056] In each individual, the “placebo” composition was applied to a first half of the area consisting of white stretch marks, and the composition of the invention to the other half of said area. The cutaneous application to the different areas of white stretch marks was accompanied by a light massage to promote penetration into the skin of each of the two compositions. On average, between 0.02 and 0.04 mL of composition / cm2 of skin with white stretch marks was applied.

[0057] The evolution of the surface area of ​​the white stretch mark lesions was evaluated after 30 days, 60 days and 90 days of applications, for the area treated with the composition of the invention compared to the area treated with the placebo composition.

[0058] Table 1 below shows the average percentage of improvement observed on the surface of each of the white stretch marks evaluated, as a function of the number of days of treatment and for each of the compositions tested.

[0059] The analysis of the surface area of ​​white stretch marks is a planimetric analysis, carried out with the ImageJ software, which allows, over time, to evaluate the surface area of ​​a given white stretch mark, in relation to its initial pre-protocol starting surface. The initial starting surface area occupied by a given stretch mark on the skin corresponds to a reference surface area defined as being 100%.

[0060] A reduction in the skin surface area occupied by a given white stretch mark, over time, results in a percentage of improvement in the dermal lesion which is positive and increasing.

[0061] On the contrary, an increase in the surface area of ​​skin occupied by a given white stretch mark, over time, results in a percentage of improvement in the dermal lesion which is decreasing, low, or even negative.

[0062] [Tables 1] % improvement in the area of ​​the white stretch mark lesion Number of days of treatment With the composition of the invention of formula 1 With the "placebo" composition 30 days 16.63% -6.07% 60 days 36.69% -1.12% 90 days 45.96% 3.98%

[0063] This table 1 shows that the application of the composition of formula 1 of the invention significantly improves the white stretch mark lesion considered on the surface of the skin, whereas this is not the case with the “placebo” composition.

[0064] The results show, for example, that after 90 days of treatment with the composition of the invention, on average over all the initial white stretch marks considered, the white stretch marks lose up to 45.96% of their surface area, compared to the surface area they initially occupied on the skin before treatment. The area of ​​skin over which they initially extended has decreased. The use of the composition of the invention therefore results in a significant reduction in the extent of white stretch marks on the skin. Thus, the presence of palmitoyl-tripeptide-5 plays its role as a dermatological active ingredient in the composition of the invention by improving the condition and extent of the surface area occupied by the white stretch mark lesions.

[0065] It should be noted that no side effects were observed during the entire period of application of the composition of formula 1 or the placebo composition. By "side effect" is meant burning, irritation, itching or any other type of modification of the skin at the surface of application of the composition of the invention. Thus, palmitoyl-tripeptide-5, as a dermatological active ingredient, in association with the excipients, is well tolerated in cutaneous application.

[0066] In addition to the planimetric analysis of the surface occupied by a white stretch mark given by the software, a visual evaluation of the lesion on the area treated with the composition of the invention was carried out on each patient. The visual evaluation, after 30, 60 and 90 days of application, is determined by indicating a score ranging from 1 to 4 for the visual appearance of the white stretch mark. The term "visual appearance" of a white stretch mark is understood to mean its length, its width, the intensity of the white color, its total surface area.

[0067] A score of 1 means a slight visual improvement in the appearance of the white stretch mark, of the order of 0 to 25% compared to the initial white stretch mark without treatment.

[0068] A score of 2 means a moderate visual improvement, of the order of 25 to 50% compared to the initial appearance of the white stretch mark without treatment.

[0069] A score of 3 means a satisfactory visual improvement, of the order of 50 to 75% compared to the initial appearance of the white stretch mark without treatment.

[0070] A score of 4 means an excellent visual improvement, greater than 75% compared to the initial appearance of the white stretch mark without treatment.

[0071] [Fig.l] summarizes the scores evaluated for each individual, as a function of the number of days of treatment, after application, morning and evening, of the composition of the invention of formula 1 on an area of ​​skin presenting white stretch marks.

[0072] The results show that after 30 days of application of the composition of the invention, 1 / 3 of the patients (10 individuals) present a moderate visual improvement and more than half of the patients (15 individuals) present a slight improvement in the dermal lesion of the white stretch mark evaluated.

[0073] Similarly, after 60 days of application, almost 2 / 3 of the patients (17 individuals) present a moderate dermal improvement of the white stretch mark lesion, and 1 / 4 of the patients (7 individuals) present a satisfactory visual improvement of the white stretch mark dermal lesion.

[0074] After 90 days of application, the results show that more than half of the people (16 individuals) have a satisfactory visual improvement of the stretch marks and two people have an excellent visual improvement of the white stretch mark lesion.

[0075] In other words, the results of [Fig.l] show that, over time, the application of the composition of formula 1 according to the invention improves the visual score of the surface condition of the dermal lesion causing the white stretch mark.

[0076] Thus, the composition of the invention has the effect of improving the condition and visual appearance of existing white stretch marks. The composition of the invention also makes it possible to prevent the appearance of new white stretch marks, but also to slow down the development of existing ones, by reducing the overall surface area they occupy on the skin.

[0077] In addition to its demonstrated efficacy even at low concentrations, palmitoyl-tripeptide-5, as a dermatological active ingredient in a composition for white stretch marks, is easy to formulate.

[0078] The use of palmitoyl-tripeptide-5, in a composition for preventing and / or treating white stretch marks, is also easy to implement and inexpensive.

[0079] Thus, the composition of the invention, for preventing and / or treating white stretch marks, comprising as dermatological active ingredient, palmitoyl-tripeptide-5 consists of an effective, inexpensive solution, usable by all types of subject, easy to implement to prevent and / or treat white stretch marks in a targeted manner.

Claims

Claims

1. Composition comprising palmitoyl tripeptide-5 as the sole dermatological active ingredient, which represents between 0.01% and 0.1% by mass relative to the total mass of the composition for use in the prevention and / or treatment of white stretch marks.

2. Composition, for its use, according to the preceding claim, characterized in that said palmitoyl tripeptide -5 represents 0.025% by mass relative to the total mass of the composition.

3. Composition, for its use, according to any one of the preceding claims, characterized in that it is presented in a galenic form suitable for topical use.

4. Composition, for its use, according to any one of the preceding claims, characterized in that it is presented in a form suitable for a cutaneous route of administration.

5. Composition, for its use, according to any one of the preceding claims, characterized in that it is in the form of cream, gel, oil, lotion, solution, ointment, mousse, emulsion.

6. Composition, for its use, according to any one of the preceding claims, characterized in that it is a cosmetic composition.

7. Cosmetic process for the prevention and / or treatment of white stretch marks, according to which: a composition according to any one of claims 1 to 6 is applied to the white stretch marks.