Cosmetic composition for the scalp, use and method for treating the scalp

WO2025059735A1PCT designated stage expired Publication Date: 2025-03-27NATURA COSMETICOS SA
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Patent Information

Application Number
PCT/BR2023/050310
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Filing Date
2023-09-18
Publication Date
2025-03-27

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Abstract

The present invention relates to a cosmetic composition, particularly in the form of a serum for application to the scalp, comprising Astrocaryum murumuru in sufficient quantity to provide benefits to the scalp and hair, as well as to its related uses and methods.
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Description

COSMETIC COMPOSITION FOR THE SCALP, USE AND METHOD FOR TREATMENT OF THE SCALP FIELD OF THE INVENTION [1] The present invention relates to a cosmetic composition, particularly in the form of a serum, for application to the scalp, comprising Astrocaryum murumuru, in a quantity sufficient to promote benefits to the scalp and hair, as well as related uses and methods. BACKGROUND OF THE INVENTION [2] The scalp is the part of the skin where the largest amount of hair, in terms of density, is concentrated. The skin on the scalp has specific characteristics that differentiate it from the rest of the body. For example, it has an intermediate thickness, between the skin on the eyelids, which is the thinnest, and that on the nape of the neck, which is the thickest. It is home to approximately 150,000 hair follicles, each with a hair shaft and a sebaceous gland. It is, therefore, a site of intense metabolic activity in sebum production and in the hair cycle, encompassing the anagen, catagen, and telogen phases of hair. [3] In general, changes in the scalp, whether due to injuries, flaking or even diseases, which may be of genetic, metabolic, systemic or infectious origin, can even compromise the quality of the hair. [4] An undernourished scalp, lacking natural hydration and repair factors, is expected to produce dull, rough, naturally more porous hair strands that require cortex and cuticle repair. In this sense, the main complaints observed in hair are rough texture, dullness, and fragility—hair that requires softness, shine, and repair from the root of the hair. [5] In addition to recommendations for stress management, a balanced diet and the use of regular massages to activate blood circulation, several products focusing on the scalp have been developed. [6] In general, available products are aimed at acting directly on damaged hair strands or are intended for application to the scalp to prevent hair loss. In these cases, these products generally use a complex combination of active ingredients, most of which include active ingredients of synthetic origin. [7] Furthermore, the particularities of the scalp make it impossible for ingredients classically known for providing benefits to the skin in general, whether of natural or synthetic origin, to be researched for the development of products for the scalp. [8] Astrocaryum murumuru, known as murumuru, has been researched for skin treatment products. For example, international publication WO14053038, by Natura Cosméticos SA, deals with cosmetic and / or pharmaceutical compositions comprising a plant lipid, which provide benefits to the skin, proven by biological mechanisms associated with skin treatment in general. [9] Patent reference CN102198064, from Tianjin Tiens Biolog Dev Co, presents a specific hair treatment composition and a method of preparing the same, which specifically uses murumuru butter. It is observed that the reference correlates with hair treatment associated with dandruff, directly related only to the scalp microbiota.

[0010] Thus, the need for new cosmetic compositions that can provide direct benefits to the scalp, such as revitalization, repair and deep hydration of this characteristic region of the skin, as well as providing additional benefits to the hair, such as anti-hair loss, anti-thinning, growth stimulation, and hair growth persists in the state of the art. fuller-bodied, repairing the strands including the cortex and cuticles from their origin (i.e., root to tip), promoting more complete strands, with uniform texture, softness and shine from their origin. SUMMARY OF THE INVENTION

[0011] In a first aspect, the present invention relates to a cosmetic composition, particularly in the form of a serum, for application to the scalp, comprising Astrocaryum murumuru, in a quantity sufficient to promote benefits to the scalp and hair.

[0012] In a second aspect, the present invention contemplates the use of Astrocaryum murumuru in the preparation of cosmetic compositions for treating the scalp and hair strands.

[0013] In a third aspect, the present invention relates to a cosmetic treatment method comprising applying a cosmetic composition comprising Astrocaryum murumuru to the scalp to promote benefits to the scalp and hair. BRIEF DESCRIPTION OF THE FIGURES

[0014] Figure 1 shows a comparison of the quantification of representative images of the increase in BMP4 synthesis in human skin fragments incubated with the product according to the present invention for 72 hours. The measurement was performed using the Image J program, and the quantification unit is square pixel.

[0015] Figure 2 (A) to (I) presents the results of atomic force microscopy. (A) to (C) present the results for zone 1, (D) to (F) for zone 2 and (G) to (I) for control, at t0, t90 and t150, respectively. DESCRIPTION OF THE INVENTION

[0016] The present invention relates to a cosmetic composition comprising Astrocaryum murumuru capable of promoting benefits to the scalp and, consequently, to the hair.

[0017] The cosmetic composition according to the present invention, particularly provided in the form of a serum, comprises from about 0.01 to about 5% of Astrocaryum murumuru, relative to the total weight of the composition, preferably in the form of butter.

[0018] The direct benefits to the scalp and, consequently, to the hair strands, are achieved by modulating genes involved in the formation and development of the hair follicle and hair fiber, as well as in hair protection against oxidative stress and scalp health.

[0019] The cosmetic composition according to the present invention, particularly in the form of a serum, comprising Astrocaryum murumuru, preferably in the form of a butter, provides healthier scalp and hair by modulating at least one of the genes BMP4, CASK, ITGB4 and / or SOD2. Thus, it is also an aspect of the present invention a cosmetic composition according to the present invention comprising Astrocaryum murumuru to modulate at least one of said genes BMP4, CASK, ITGB4 and / or SOD2, particularly the BMP4 gene.

[0020] The cosmetic composition according to the present invention promotes an increase of at least 90% in BMP4, responsible for cell growth and differentiation, as well as for inducing differentiation of keratinocytes in the bulb matrix and the formation of the hair follicle and hair fiber.

[0021] According to the present invention, Astrocaryum murumuru, preferably in the form of butter, has been shown to be capable of acting in the region of the dermal papilla and bulb, inducing the differentiation of keratinocytes to improve the quality of the hair fiber, through the gene modulation of BMP4 (increased expression), which represents the main marker for the mechanism of hair formation, due to its characteristic of modulating the keratinocyte life cycle.

[0022] Furthermore, the cosmetic composition according to the present invention promotes an increase of at least 74% in CASK, which acts on development of the hair follicle, in the differentiation of keratinocytes and in the formation of the hair follicle.

[0023] Furthermore, the cosmetic composition according to the present invention provides an increase of at least 216% in ITGB4, associated with the embryonic processes of follicle formation, as well as maintenance and protection of the follicle (dermis-epidermis junction), which denotes scalp health.

[0024] The cosmetic composition according to the present invention also provides an increase of at least 91% in SOD2, responsible for protection against external aggressions and oxidative stress and hair protection.

[0025] This surprising action in the modulation of genes associated with scalp mechanisms, particularly ITGB4, SOD2, BMP4 and CASK, provides benefits of comprehensive repair of the scalp and hair, deep hydration of the scalp, providing repair of the cortex and cuticles from their origin (root to tip) and more intact hair, with uniform texture, softness and shine from their origin.

[0026] The cosmetic composition according to the present invention is prepared with cosmetically acceptable excipients, particularly for the preservation of a serum composition.

[0027] In a second aspect, the present invention contemplates the use of Astrocaryum murumuru, preferably in the form of butter, in an amount ranging from approximately 0.01 to approximately 5%, in relation to the total weight of the composition, in the preparation of cosmetic compositions for treating the scalp and, consequently, the hair strands.

[0028] In a third aspect, the present invention relates to a cosmetic treatment method that consists of applying a cosmetic composition comprising Astrocaryum murumuru to the scalp to promote benefits to the scalp and hair.

[0029] The following examples, without imposing any limitation, are particular embodiments of the present invention, as well as demonstrate that the cosmetic composition according to the present invention: - activates the hair's reconstruction power from its origin; - promotes more repaired strands from the cuticle to the cortex from its origin; - deeply moisturizes the scalp; - intensifies the production of shielded wires that are more resistant to breakage; - provides natural shielding of the strands; - protects and intensifies keratin production; - provides a healthier cuticle and cortex, prepared to face the daily damage that the hair is exposed to; - results in shiny, vital strands from birth; - stimulates the formation of strands that are more resistant to daily damage; - promotes hair with more mass (keratin quality), armored cuticles and less susceptible to breakage; - stimulates the formation of high-quality keratin for greater resistance to daily damage, meaning hair with more mass, armored cuticles and less susceptible to breakage; - stimulates the formation of a strand with a high-quality structure for resistance to daily damage, that is, hair with more mass, armored cuticles and less susceptible to breakage; - stimulates the renewal of the scalp and follicles, restoring the vitality and softness of the scalp and hair, so that the scalp is healthier, protected for shiny hair that is easier to comb; - promotes complete reconstruction of both the scalp and hair strands, restoring hair health and allowing them to form with more intact cuticles and cortex that are prepared for external damage; - restores the natural shine of the hair; - activates the self-shielding of the wires, promoting wires that are more resistant to physical, chemical and thermal damage; - activates the hair's reconstruction power from its origin, in order to restore the hair and the hair bulb, for the growth of healthier and more resistant hair; - provides deeply restored hair from the inside out; - results in hair with a more uniform, healthy and shiny texture; - promotes the restoration and reconstruction of hair strands from the root; - results in higher quality strands, that is, strands with less porosity from birth; - the strands grow shinier, softer and more uniform; - Improves cuticle texture from the root; and - provides nutrition from root to tip, that is, more nutrition from the origin of the hair.

[0030] Based on the evaluation of the following tests, it can be concluded that the use of the composition according to the present invention can improve scalp health and impact new hair growth. The formation of better-quality keratin and a reduction in hair roughness were observed. These benefits are primarily modulated by the BMP4 gene (related to follicle development and hair growth). EXAMPLES Example 1A - Serum composition according to the present invention Example 1 B - Serum composition according to the present invention Example 1C - Serum composition according to the present invention Example 2 - Ex vivo evaluation of BMP4 protein synthesis

[0031] Bone morphogenetic proteins (BMPs) comprise a group of more than 20 proteins belonging to the transforming growth factor (TGF)-[3 superfamily. Among their functions, they stand out as powerful regulators of skin development and as controllers of epidermal homeostasis, hair follicle growth and melanogenesis.

[0032] In melanogenesis, bone morphogenetic protein 4 (BMP4) can act as an autocrine inhibitor of melanogenesis. The BMP-4 effect is mediated by transcriptional and post-transcriptional events, leading to partial repression of the tyrosinase promoter, as well as decreased tyrosinase mRNA stability and levels. Regarding skin aging, BMP4 also plays a fundamental role in tissue maintenance. The protein is closely linked to the process of skin stem cell proliferation and is absolutely necessary for proper differentiation into various lineages of ultimately differentiated skin cells. Since inappropriate biological activities of skin stem cells induce wrinkle formation, appropriately acting BMPs tend to inhibit this undesirable process.

[0033] In this study, the capacity of the composition according to the present invention (as per example 1) on the synthesis of BMP4 in human skin fragments was evaluated. Incubation of ex vivo skin fragments

[0034] After the surgical procedure performed by the ophthalmic plastic surgery clinical staff, eyelid fragments were placed in vials containing 0.9% saline solution until the time of the experiment. Biological samples were removed from the saline solution, immersed in 70% ethanol for 15 seconds, and washed twice in fresh saline solution. The fragments were transferred to a petri dish containing culture medium for treatment with the composition according to the present invention for 72 hours in a humidified atmosphere, 37°C, 5% CO2. The product was applied to the skin at a rate of 2 mg / cm 2 Immunofluorescence evaluations

[0035] After 72 hours of incubation with the composition according to the present invention, the ex vivo skin fragments were fixed in 4% paraformaldehyde (pH 7.4) for 24 hours and cryoprotected in 30% sucrose solution for 48 hours. Then, serial sections of 10 pm were collected directly on silanized slides with the aid of a cryostat (Leica - CN1850).

[0036] At the end of the section collection, they were washed with 0.1 M PB and incubated overnight with the primary antibody BMP4 (Abeam, ab39973). Subsequently, they were washed again with 0.1 M PB and incubated for 1 hour with the Goat anti-mouse secondary antibody (Invitrogen; A11055). At the end of these steps, a new incubation (1 minute) with DAPI (4'-6-Diamidino-2-Phenylindole; DNA marker) was performed, followed by three 5-minute washes with 0.1 M PB.

[0037] Then, the slides were mounted in a specific mounting medium and analyzed under a fluorescence microscope (Leica - DM 1000) with using LAS Software (Leica Application Suite). The parameter evaluated was the fluorescence intensity emitted by the labeling with a specific antibody. Data analysis

[0038] Analysis of variance (ANOVA) was used for statistical analysis. The paired t-test was used when the analysis of variance detected significant differences between groups. In all groups studied, P values ​​less than 0.05 were considered statistically significant.

[0039] Figure 1 shows the results of measuring BMP4 synthesis in human skin fragments from three different patients treated with the composition according to the present invention for 72 hours, compared to the control (untreated) under the same conditions. When compared to the control, the composition according to the present invention showed a positive modulatory action on BMP4 synthesis, promoting a 90% increase.

[0040] According to the results presented, it is concluded that the composition according to the present invention demonstrated the ability to positively modulate the synthesis of BMP4, in human skin fragments, when compared to the control group, promoting an increase of 90%. Example 3 - Leather irritation test

[0041] For the present study, nineteen patients completed the study. Mean age: 45 ± 12 years; Phototype: 89% phototype III and 11% phototype IV; Gender: 89% female and 11% male.

[0042] The study was carried out for about five months.

[0043] After recruitment, patients were instructed to discontinue use of any topical scalp and hair products 48 hours before the study began. On the day of the study, patients who came to the laboratory received explanations from the researcher about the study procedures, legal and ethical aspects, risks and benefits, and support. physician and reimbursement methods for participation expenses. The subjective analysis methodology for clinical efficacy was performed by the dermatologist at the beginning of the study and after 90 and 150 days of use of the product under investigation.

[0044] The patient applied the composition according to the present invention daily to the entire scalp, massaging it in at night with his fingertips to distribute it evenly and facilitate its penetration. He was asked not to rinse and to let it dry.

[0045] According to the study protocol and procedures used to evaluate the efficacy of the product under investigation, it was possible to verify that the composition according to the present invention reduced erythema in 53% of the research subjects after 150 days of use.

[0046] There was no variation in the irritation, burning sensation, or itching parameters. This indicated that the composition according to the present invention did not cause these symptoms and protected the scalp, preventing the appearance of any signs or symptoms of sensitivity and / or irritation.

[0047] The composition according to the present invention reduced scalp flaking in 32% of the research subjects after 150 days of use.

[0048] Regarding erythema, it was observed that after 90 days of use of the composition according to the present invention there was a 3.1% reduction in erythema, with a responsiveness of 5% and after 150 days there was a 3.1% reduction in erythema, with a responsiveness of 53%.

[0049] Regarding scaling, some of the participants had mild to moderate flaking, and after 90 and 150 days the condition improved. After 90 days of using the composition according to the present invention, there was a 37.5% improvement in scaling, with a 16% responsiveness, and after 150 days, there was an 87.5% improvement in flocculation, with a 32% responsiveness.

[0050] From these results it is possible to conclude that the composition according to the present invention helps to improve the health of the scalp, since it is capable of reducing flaking. Example 4 - Hair fiber test

[0051] The objective of this study was to evaluate the lifting of the cuticle and the roughness of the hair fiber after the application of the composition according to the present invention using the atomic force microscopy technique.

[0052] Five research patients completed the study. Mean age: 48 ± 11 years; Phototype: 100% phototype III; Gender: 100% female.

[0053] The study was carried out for about five months.

[0054] After recruitment, patients were instructed to discontinue use of any topical scalp and hair products 48 hours before the study began. On the day of the study, patients who presented to the laboratory received explanations from the researcher about the study procedures, legal and ethical aspects, risks and benefits, medical support, and reimbursement options for participation expenses.

[0055] To assess hair roughness, strands were collected from the root and three regions of the strands were analyzed by atomic force microscopy: Zone 1 - Keratinization Zone, Zone 2 - 1.5 cm of hair shaft growth and Zone 3 - half length (control region).

[0056] Apply daily to the entire scalp, and at night, massage with your fingertips to distribute evenly and facilitate product penetration. Do not rinse and allow to dry. Recommended use is once a day.

[0057] According to the protocol and procedures used in this study, it was possible to conclude that in zone 2 (1.5 cm of hair shaft growth), after 90 and 150 days, the strands presented significantly (P<0.05) lower roughness values ​​when compared to the strands in the initial condition. Furthermore, after 90 days the composition according to the present The invention showed an improvement in roughness values ​​of 14.5%, reaching 24.2% and after 150 days it showed an improvement in roughness values ​​of 21.4%, reaching 35.3%.

[0058] In zone 1 (keratinization zone), after 90 and 150 days, the strands presented significantly (P<0.05) lower roughness values ​​when compared to the strands in the initial condition. Furthermore, after 90 days, the experimental product showed an improvement in roughness values ​​of 11.3%, reaching 17.3%, and after 150 days, it showed an improvement in roughness values ​​of 12.5%, reaching 19.5%.

[0059] The comparison between zone 2 (1.5 cm of hair shaft growth) and zone 3 (control region) showed a significant reduction in the roughness values ​​of zone 2 when compared to zone 3 (control) after 90 and 150 days of domestic use.

[0060] Surprisingly, the composition according to the present invention showed improvement in wire roughness from atomic force microscopy.

[0061] Roughness is an important attribute for the surface and evaluates the mechanical / structural perspective of the hair, in this case it is the newly formed hair, not being a modification resulting from deposition in the hair, but rather from gene / protein modulation in the scalp, leading to the formation of a healthier hair.

[0062] This evaluation was carried out by evaluating different parts of the wire.

[0063] In zone 1 (keratinization zone or growth zone), there was an improvement in roughness, with a more uniform shape of the hair fiber being observed, which will result in a less rough hair strand in the future. The results are illustrated in Figure 2 (A), (B), and (C), where after 90 days there was an 11% improvement in roughness, reaching 17.3%, and after 150 days there was a 12% improvement in roughness, reaching 19.5%.

[0064] In zone 2 (distal region - proximal to the bulb), the keratin is already fully formed, making it the best region for evaluating roughness. The results are presented in Figure 2 (C) to (E), which showed a 14.5% improvement in roughness after 90 days, reaching 24.2%, and a 21.4% improvement after 150 days, reaching 35.3%.

[0065] In the control, shown in figure 2 (F) to (I), where there is no possibility of the composition according to the present invention acting, the roughness remained, as it is very far from the hair bulb.

[0066] Comparing zone 2 with the control zone, the results from zone 2 are statistically significant (P<0.05). Example 5 - hair integrity by differential scanning calorimetry (DSC).

[0067] The aim of this study was to evaluate the protection of the keratin structure of the hair fiber through DSC (differential scanning calorimetry).

[0068] Twenty research patients completed the study. Mean age: 43 ± 12 years; Phototype: 75% phototype III and 25% phototype IV; Gender: 100% female.

[0069] The study went on for about five months.

[0070] Hair fibers were randomly collected for DSC analysis at baseline (t0) and after 150 days of product use (t150). Thermal analyses were performed in triplicate by DSC, totaling 3 data sets per treatment.

[0071] The sample was applied daily to the entire scalp, massaging it in at night with fingertips to distribute it evenly and facilitate penetration. The product was applied once a day.

[0072] According to the results, when comparing the data on the enthalpy of degradation of a-keratin (deltaHD) in the initial condition and after 150 days of using the products, respectively (for each patient in the research), after 150 days of using the product, 90% of the researched showed an increase of the enthalpy of degradation of a-keratin (deltaHD) compared to hair fibers in the initial condition (tO). After 150 days of use of the product, 10% of patients showed no significant differences in the enthalpy of degradation of a-keratin (deltaHD) values ​​compared to hair fibers in the initial condition (tO).

[0073] Also according to the results, when comparing the data on the degradation temperature of a-keratin (TD) in the initial condition and after 150 days of use of the products, respectively (for each patient in the research), it was observed that after 150 days of use of the product, 30% of the respondents showed an increase in the degradation temperature of a-keratin (deltaD) in relation to the hair fibers in the initial state (tO). After 150 days of use of the product, 70% of the respondents did not show significant differences in the degradation temperature (TD) of a-keratin in comparison with the hair fibers in the initial condition (tO).

[0074] The objective of this test was to evaluate the protection of the alpha-keratin structure in the hair fiber based on the amount of energy required to break the structure.

[0075] No cosmetic composition capable of improving the quality of newly formed keratin has been identified in the state of the art. In general, scalp care products refer to general care, involving factors such as scaling, redensification (increasing the number of hairs), and preventing hair loss.

[0076] It was therefore found that after 150 days, 90% of participants demonstrated an increase in the variation of energy required for keratin degradation, which means that the keratin formed has better quality compared to T0.

[0077] The man of technique will be able to readily evaluate, through the teachings contained in the text and the examples presented, the advantages of invention and propose variations and equivalent alternatives for implementation, without departing from the scope of the invention, as defined in the attached claims.

Claims

CLAIMS 1. COSMETIC COMPOSITION FOR THE SCALP characterized by comprising Astrocaryum murumuru and cosmetically acceptable excipients.

2. COMPOSITION, according to claim 1, characterized by comprising from about 0.01 to about 5% of Astrocaryum murumuru relative to the total weight of the composition.

3. COMPOSITION, according to claim 2, characterized by Astrocaryum murumuru being in the form of butter.

4. COMPOSITION, according to any one of claims 1 to 3, characterized by being in serum form.

5. COMPOSITION, according to any one of claims 1 to 4, characterized by modulating at least one of said genes BMP4, CASK, ITGB4 and / or SOD2.

6. COMPOSITION, according to claim 5, characterized by modulating the BMP4 gene.

7. COMPOSITION, according to any one of claims 1 to 4, characterized by increasing the BMP4 modulation by at least 90%, the CASK modulation by at least 74%, the ITGB4 modulation by at least 216% and / or the SOD2 modulation by at least 91%.

8. USE of the composition as defined in any one of claims 1 to 7, characterized by being for promoting complete repair of the scalp and hair, deep hydration of the scalp, repair of the cortex and cuticles from their origin, more intact hair strands, with uniform texture, softness and shine from their origin.

9. Use of Astrocaryum murumuru characterized by the fact that it is in the preparation of a cosmetic composition for the treatment of the scalp.

10. USE, according to claim 9, characterized by being useful in the complete repair of the scalp and hair, deep hydration of the scalp, repair of the cortex and cuticles from their origin, resulting in healthier hair strands with a uniform texture, softness, and shine from their origin.

11. USE, according to claim 9, characterized in that the amount of Astrocaryum murumuru varies from about 0.01 to about 5% relative to the total weight of the composition.

12. METHOD FOR SCALP TREATMENT characterized by comprising applying a cosmetic composition comprising Astrocaryum murumuru to the patient in need.

Citation Information

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