Composition for preventing or treating alopecia

Abstract

The invention relates to a pharmaceutical composition for preventing or treating alopecia, the pharmaceutical composition is prepared by matching three active ingredients of moringa seed element, kinsenoside and serenoa serrulata extract according to a specific proportion, and pharmacodynamic research proves that the composition can obviously promote and improve the proliferation activity of human papilla cells, and has the efficacy of preventing or treating alopecia. In addition, in an animal model of alopecia, the effect is obviously better than that of an existing anti-alopecia product such as minoxidil. Compared with an existing anti-alopecia product, the anti-alopecia composition has the following remarkable advantages: 1) the effect of preventing or treating alopecia can be realized by adopting a simplified formula, and mutual interference among complex components is avoided; 2) the composition provided by the invention has an excellent effect obviously better than that of the existing mainly used anti-alopecia products, by adopting the technical scheme provided by the invention, a promising treatment choice is provided for the alopecia problem which puzzles people for a long time, and the composition has a wide clinical application prospect.

Description

Technical Field

[0001] The present invention belongs to the field of medical technology, and in particular relates to a composition for preventing or treating hair loss. Background Art

[0002] With improved living standards and a growing focus on personal appearance, hair loss is a growing concern, affecting people of all ages, genders, and regions. Globally, androgenic alopecia is the most common type of hair loss, along with other conditions such as alopecia areata. In terms of age distribution, hair loss can occur at any age. While the prevalence of hair loss is relatively low among children, some are also severely affected. The prevalence of hair loss gradually increases with age. Hair loss is more prevalent in middle-aged and elderly people due to declining physiological functions and fluctuating hormone levels. Androgenic alopecia begins to manifest and worsens after puberty. Significant gender differences exist between different types of hair loss. Androgenic alopecia is more common in men, characterized by a receding hairline and progressive thinning and thinning of hair on the top of the head, known as male pattern baldness. Women, on the other hand, are more susceptible to female pattern baldness, which typically causes thinning of hair on the top of the head, while the hairline on the front of the head generally remains unchanged.

[0003] Currently, different hair loss treatments have been developed, but each has varying degrees of defects and deficiencies, including the following.

[0004] (1) Drug treatment: Minoxidil, finasteride, or anti-androgen drugs are commonly used to treat hair loss. Topical minoxidil is a commonly used drug for treating hair loss, showing some efficacy in treating androgenic alopecia and alopecia areata, and can promote hair growth. However, its effectiveness is relatively weak, and patients need to use it long-term (usually for more than 3-6 months to see significant results). Some users experience irritation reactions such as scalp itching, redness, and scaling. A few may also develop hirsutism, which is increased hair growth in other parts of the body. Oral finasteride is primarily used to treat androgenic alopecia. By inhibiting the activity of 5α-reductase, it reduces the production of dihydrotestosterone, prevents hair follicle atrophy and hair loss, and can fundamentally improve hair loss symptoms. However, it requires long-term use and is prone to relapse after discontinuation. It may also cause side effects such as decreased libido, erectile dysfunction, and decreased semen volume. Anti-androgen drugs mainly include spironolactone, cyproterone acetate, etc., which are used to treat androgenic alopecia in women. However, these drugs may cause adverse reactions such as menstrual disorders, breast tenderness, and decreased libido. Long-term use may also have a certain impact on liver and kidney function.

[0005] (2) Laser Therapy: This primarily includes low-level laser therapy (LLLT) and fractional laser therapy (FLT). LLLT is believed to promote the re-entry of catagen hair follicles into the growth phase and prolong the growth phase. However, the effectiveness varies from person to person, and some may not see significant improvement. Furthermore, laser treatments take a long time to manifest, typically requiring multiple treatments for optimal results. The treatment process is cumbersome, and the equipment is relatively expensive, making treatment relatively expensive. FLT delivers a precise laser pulse beam that evenly illuminates the scalp, stimulating the body's natural healing process. However, it may cause minor burns, redness, swelling, and blisters. Improper or excessive treatment increases the risk of skin damage. Post-treatment skin may become sensitive and susceptible to infection, requiring careful care and protection from direct sunlight.

[0006] (3) Microneedle Therapy: Microneedle therapy stimulates the scalp, inducing a post-injury self-repair cascade and promoting the release of growth factors and cytokines, thereby promoting hair growth. However, this treatment may cause infection, bleeding, skin irritation, and allergic reactions, especially if proper disinfection measures are not followed or the procedure is performed improperly. Furthermore, the effectiveness of microneedle therapy for hair growth varies from person to person, and not everyone will see significant results. Recovery time is required after treatment, which may affect daily life.

[0007] (IV) Tissue engineering scaffolds: Tissue engineering scaffolds and artificial skin platforms based on macromolecules have shown certain potential in hair loss treatment research, but most of them are currently in the experimental research stage. In addition, they have problems such as insufficient mechanical properties, complex preparation process, difficult to control degradation rate, possible immune response, and difficulty in large-scale production. They are still a long way from widespread clinical application.

[0008] (5) Traditional Chinese Medicine Treatment: Some traditional Chinese medicine formulas or plant extracts have been reported to promote hair growth. However, the composition of traditional Chinese medicine is complex, and the mechanism of action is not yet fully understood. Allergic reactions may occur, and long-term and excessive use of some traditional Chinese medicine ingredients may burden liver and kidney function. Furthermore, the effectiveness of traditional Chinese medicine treatment varies from person to person, requiring long-term and consistent use, and the onset of effect is relatively slow.

[0009] (6) Hair Transplantation: Hair transplantation is a new, clinically proven technology for the effective treatment of permanent hair loss. However, it is costly and can lead to complications such as infection, bleeding, swelling, scarring, inconsistent hair growth direction and angle, hair frizziness, and transplant failure. For severe hair loss, multiple surgeries may be required to achieve the desired results. Furthermore, the recovery period is long, lasting approximately 1-3 months.

[0010] Therefore, given that existing treatment options are not ideal, patients with hair loss are in urgent need of a new, safe and effective treatment option for hair loss, including therapeutic drugs, treatment methods, etc. Summary of the Invention

[0011] In order to solve the problems existing in the aforementioned prior art, the applicant has provided a solution for treating hair loss as described in the present invention after research.

[0012] In a first aspect of the present invention, a composition for preventing or treating hair loss is provided, comprising the following components calculated in parts by weight: 55-75% moringa seed extract, 8-15% anoectochiloside, and 15-25% saw palmetto extract.

[0013] Preferably, the weight percentage of the moringa seed extract is 60-70%, the weight percentage of anoectochiloside is 10-12%, and the weight percentage of the saw palmetto extract is 17-22%.

[0014] Preferably, the weight percentage of the moringa seed extract is 62-68%, the weight percentage of anoectochiloside is 9-14%, and the weight percentage of the saw palmetto extract is 18-21%.

[0015] Preferably, the weight percentage of the moringa seed extract is 64-66%, the weight percentage of anoectochiloside is 9-14%, and the weight percentage of the saw palmetto extract is 18-21%.

[0016] According to the first aspect provided by the present invention, the composition for preventing or treating hair loss further comprises an auxiliary material acceptable in the pharmaceutical or cosmetic field.

[0017] The composition for treating hair loss provided according to the first aspect of the present invention may also be composed of the components in parts by weight.

[0018] In a second aspect of the present invention, a composition for preventing or treating hair loss is provided, the composition comprising moringa seed extract, anoectin, and saw palmetto extract, wherein the molar ratio of moringa seed extract, anoectin, and saw palmetto extract is 5-20:1.5-6:1-4.

[0019] Preferably, the molar ratio of moringa seed, anoectin and saw palmetto extract is 10-15:1.5-4.5:2-4.

[0020] More preferably, the molar ratio of moringa seed, anoectin and saw palmetto extract is 10:1.5:3.

[0021] In a third aspect of the present invention, provided is use of the composition provided by the present invention in the preparation of a medicament or cosmetic for preventing, treating, alleviating or reversing hair loss.

[0022] Preferably, the drug is a skin external preparation, and the skin external preparation is selected from one or more of aerosols, ointments, liquids, emulsions, patches, powders for spreading, oils, creams and gels.

[0023] Preferably, the cosmetic is a cosmetic for hair or scalp.

[0024] Preferably, the cosmetics include but are not limited to one or more of shampoo, conditioner, hair treatment cream, hair lightener, hair mask, hair milk, hair lotion, hair root nutrient solution, scalp care solution, scalp essence, scalp nutrient solution, scalp ampoule, scalp essence or ointment.

[0025] The CAS number of the moringa seed extract used in the present invention is 73255-40-0. The CAS number of the anoectin used in the present invention is 151870-74-5. The CAS number of the saw palmetto extract used in the present invention is 84604-15-9.

[0026] The present invention relates to a pharmaceutical composition for preventing or treating hair loss. The composition comprises three active ingredients: moringa seed extract, anoectin, and saw palmetto extract, combined in a specific ratio. Pharmacodynamic studies have demonstrated that the composition significantly enhances the proliferation activity of human dermal papilla cells and demonstrates significantly superior efficacy to existing anti-hair loss products, such as minoxidil, in animal models of hair loss. Compared to existing anti-hair loss products, the present invention offers the following significant advantages: 1) a streamlined formula is employed to prevent or treat hair loss, avoiding interference between complex ingredients; and 2) the composition exhibits superior efficacy significantly superior to currently used anti-hair loss products. The technical solution provided by the present invention provides a promising treatment option for the long-standing problem of hair loss, with broad prospects for clinical application. BRIEF DESCRIPTION OF THE DRAWINGS

[0027] Figure 1 This figure shows the cytotoxicity of a combination of moringin, kinsenoside, and saw palmetto extract at varying molar concentrations on human dermal papilla cells (results are shown as mean ± SD, N = 6, *p < 0.05 and **p < 0.01 indicate significant differences compared with the control group). Moringin represents moringin, kinsenoside represents kinsenoside, sawpalmetto represents saw palmetto extract, and control represents the control group.

[0028] Figure 2 The results show the effects of different drug combinations on the growth morphology (left) and proliferation activity (right) of human dermal papilla cells (results are shown as mean ± SD, N = 6, *p < 0.05 indicates a significant difference compared with the control group). Mor represents moringin, Kin represents anoectin, Sap represents saw palmetto extract, and Control represents the control group.

[0029] Figure 3The effects of different drug combinations on the expression of VEGF (left) and AR (right) genes in human dermal papilla cells are shown (results are shown as mean ± SD, N = 6, *p < 0.05 indicates a significant difference compared with the model group). Mor represents moringa seed extract, Kin represents anoectin, Sap represents saw palmetto extract, and Model represents the model group (i.e., the baseline level of the model group itself).

[0030] Figure 4 This figure shows the effects of different drug combinations on the rate of hair regeneration (top) and quality (hair length and weight, lower left and lower right, respectively) on the backs of mice with androgenetic alopecia. The positive drug group is minoxidil (results are shown as mean ± SD, N = 5, *p < 0.05 indicates a significant difference compared with the positive drug group). Control represents the blank control group, Model represents the model group, Minoxidil represents the minoxidil positive control group, Mor represents moringa seed extract, Kin represents anoectin, and Sap represents saw palmetto extract. DETAILED DESCRIPTION

[0031] In order to make the objectives, technical solutions and effects of the present invention clearer and more specific, the present invention is further described in detail below with reference to the accompanying drawings and examples. It should be understood that the specific embodiments described herein are only used to explain the present invention and are not intended to limit the present invention.

[0032] In the following examples and comparative examples, where specific conditions are not specified, the experiments were conducted under conventional conditions or those recommended by the manufacturer. Reagents and instruments used, where the manufacturer is not specified, are commercially available. The experimental methods and detection methods used in the following examples, unless otherwise specified, are conventional experimental methods and detection methods known in the art.

[0033] This example used a CCK-8 assay (Cell Counting Kit-8, C0037, Shanghai Biyuntian Biotechnology Co., Ltd.) and followed the product instructions to investigate the effects of different molar concentrations of a combination of moringa (Mor), anoectin (Kin), and saw palmetto extract (Sap) on the proliferation activity of human dermal papilla cells. Moringa (Mor), anoectin (Kin), and saw palmetto extract (Sap) were all purchased from commercial sources. Moringa was purchased from Chengdu Zhizhihua Pure Biotechnology Co., Ltd. (Cat. No. PCS-3232, CAS No. 73255-40-0), anoectin was purchased from Chengdu Ruifensidedan Biotechnology Co., Ltd. (Cat. No. J-091, CAS No. 151870-74-5), and saw palmetto extract was purchased from Shanghai MacLean Biochemical Technology Co., Ltd. (Cat. No. S967402-500g, CAS No. 84604-15-9). The specific steps are as follows.

[0034] (1) Experimental preparation: Human hair follicle dermal papilla cells (DPCs) were prepared and cultured using a culture medium consisting of DMEM / F12, 1% non-essential amino acids, 15% fetal bovine serum, and 1% streptomycin. (2) Cell separation and culture in well plates: DPCs with a confluency of more than 80% were selected, the cells were digested into a cell suspension, and the assay medium (composed of DMEM / F12, 1% non-essential amino acids, 10% fetal bovine serum, and 1% streptomycin) was added and the density was adjusted to 1×10 4 cells / ml, and then add the cell suspension to a 96-well plate, 100 ml / well (set up 6 replicate wells for each group, make two plates) and then place in a cell culture incubator for 12 hours; (3) Experimental grouping scheme: According to the composition and concentration of different compositions in Table 1, a blank control group (drug-free, i.e., experiment number 1 in Table 1) and a drug group (drug composition and concentration refer to experiment numbers 2-25 in Table 1) were prepared using the test culture medium, and two culture time points of 24 hours and 48 hours were set.

[0035] (4) CCK-8 assay: After the cell culture reaches the time point in step (2), the supernatant is aspirated and discarded, and 100 ml of the assay medium containing different drug concentrations in step (3) is added. The culture is continued for 24 hours and 48 hours. After the time point is reached, the supernatant is aspirated and discarded, and the assay medium containing 10% CCK-8 is added. The culture is continued for 3.5 hours, and the absorbance value at 450 nm is measured using a microplate reader.

[0036] (5) Crystal violet staining: discard the culture medium containing CCK-8, gently wash the cells twice with preheated PBS to remove residual reagents; add 4% paraformaldehyde (or cold methanol) to each well to cover the cells, fix at room temperature for 15 minutes, and then discard the fixative; add 0.1% crystal violet staining solution (dissolved in 10% ethanol) to each well to cover the cells, stain at room temperature for 20 minutes, then discard the staining solution, gently rinse with deionized water until the background is colorless, and then observe the cell staining morphology under a microscope.

[0037] The results are as follows Figure 1 and as shown in Table 1.

[0038] like Figure 1 As shown, within the Mor concentration range below 2.5 μM, cell viability exhibited a dose-dependent increase. At 5 μM, there was no significant difference compared to the blank control group. However, as the concentration continued to rise, Mor exhibited significant cytotoxicity. At 0-5 μM molar concentrations, cell viability remained stable, with no significant differences observed. However, at concentrations above 10 μM, Mor exhibited dose-dependent cytotoxicity. Similarly, Sap had little effect on the viability of human dermal papilla cells at concentrations below 10 μM. However, at concentrations of 20 μM, Sap began to exhibit significant cytotoxicity.

[0039] Experiment number Moringa oleifera seed extract (mM) Anoectochiloside (mM) Saw Palmetto Extract (mM) Cell viability (OD) 1 0 0 0 1.242 2 0 1.5 1 1.011 3 0 3 2 1.203 4 0 4.5 3 1.117 5 0 6 4 0.986 6 5 0 1 1.224 7 5 1.5 2 1.298 8 5 3 3 1.313 9 5 4.5 4 1.252 10 5 6 0 1.147 11 10 0 2 1.323 12 10 1.5 3 1.516 13 10 3 4 1.338 14 10 4.5 0 1.272 15 10 6 1 1.108 16 15 0 3 1.078 17 15 1.5 4 1.146 18 15 3 0 1.276 19 15 4.5 1 1.023 20 15 6 2 0.965 21 20 0 4 0.822 22 20 1.5 0 0.753 23 20 3 1 0.966 24 20 4.5 2 0.878 25 20 6 3 0.633 Table 1 shows the results of an orthogonal assay for the proliferation activity of a combination of three drug ingredients at five concentration levels (three factors, five levels) after 48 hours of co-culture with human dermal papilla cells. Based on the data in Table 1, calculations show that the range of effect of moringa seed extract on cell activity is 0.501, the range of effect of anoectin on cell activity is 0.251, and the range of effect of saw palmetto extract on cell activity is 0.072. Moringa seed extract has the greatest impact on cell activity, followed by anoectin.

[0040] according to Figure 1 The effect of moringa on cell activity is mainly manifested as toxic side effects at high doses, while the combined use of anoectin and saw palmetto extract at a certain dose concentration can antagonize the cytotoxicity of moringa and show a trend of promoting cell growth. For example, in experimental group No. 12, when the concentration of moringa was 10 mM, its main effect on cell growth was inhibition ( Figure 1 ), but after adding 1.5 mM aostemoside and 3 mM saw palmetto extract, the cell activity was significantly improved and was better than that of the blank group (No. 1), while pure aostemoside and saw palmetto extract did not show obvious cell proliferation promoting effect at this concentration, which means that aostemoside and saw palmetto extract mainly achieve the effect of improving cell proliferation by antagonizing the cytotoxicity of moringa seed extract.

[0041] Figure 2 The effects of different drug formula combinations of pure moringa (10 μM), moringa (10 μM) + anoectin (1.5 μM), moringa (10 μM) + saw palmetto extract (3 μM), and moringa (10 μM) + anoectin (1.5 μM) + saw palmetto extract (3 μM) on the growth morphology and proliferation activity of human dermal papilla cells were studied. Figure 2 It can be observed that after 24 hours of co-culture of cells with the drug formula, the cell adhesion density of the Moringa oleifera seed extract group was significantly lower than that of the control group, and a large number of cells showed shrinkage and deformation. After 48 hours, the cell density increased but was still significantly lower than that of the control group. Similarly, the cell adhesion density and proliferation activity of the Mor+Kin and Mor+Sap groups were not significantly different from those of the Mor group. However, the Mor+Kin+Sap group was able to effectively promote the proliferation of human dermal papilla cells, and the cell adhesion morphology and adhesion density were better than those of the control group.

[0042] Further RT-PCR detection of VEGF and androgen receptor (AR) gene expression in dermal papilla cells treated with different drug formula combinations was performed. Figure 3 As shown, it can be seen that the Mor and Mor+Kin groups can promote the expression of AR, but have no significant effect on the expression of VEGF. The Mor+Sap group can promote the expression of VEGF, but has no significant effect on the expression of AR. Mor+Kin+Sap showed a significant effect in promoting the expression of AR and VEGF. The above results indicate that specific drug formulations help reduce the toxic effects on human dermal papilla cells and promote their growth and proliferation by regulating the normal response of dermal papilla cells to androgens and improving the cell microenvironment.

[0043] The effects of the positive drug minoxidil and the present drug formulation on hair regeneration were compared in an androgenic alopecia mouse model, wherein the Mor+Kin+Sap composition used was the experimental group No. 12 in Example 1. The results are shown in FIG. Figure 4 As shown in the figure, compared with the model group, the hair on the back of the mice in the minoxidil group began to grow on the 14th day, and by the 21st day, the hair had covered most of the exposed skin. However, there was no significant improvement in hair weight and average length compared with the model group. In contrast, the Mor+Kin+Sap group had a small amount of hair on the skin surface on the 7th day, and the hair was completely covered on the 21st day. The hair weight and average length were significantly improved compared with the minoxidil group, and no side effects were found. This shows that the drug formula has a better effect in promoting hair regeneration.

[0044] The embodiments of the present invention are described in detail above, but the present invention is not limited to the described embodiments. It is apparent to those skilled in the art that various changes, modifications, substitutions, and variations of these embodiments may be made without departing from the principles and spirit of the present invention, and the changes still fall within the scope of protection of the present invention.

Claims

1. A composition for preventing or treating hair loss, comprising the following components in parts by weight: 55-75% moringa seed extract, 8-15% anoectin, and 15-25% saw palmetto extract.

2. The composition according to claim 1, wherein the weight percentage of moringa seed is 60-70%, the weight percentage of anoectochiloside is 10-12%, and the weight percentage of saw palmetto extract is 17-22%.

3. The composition according to claim 2, wherein the weight percentage of moringa seed is 62-68%, the weight percentage of anoectochiloside is 9-14%, and the weight percentage of saw palmetto extract is 18-21%.

4. A composition for preventing or treating hair loss, comprising moringa seed extract, anoectin, and saw palmetto extract, wherein the molar ratio of the moringa seed extract, the anoectin, and the saw palmetto extract is 5-20:1.5-6:1-4.

5. The composition according to claim 4, wherein the molar ratio of the moringin, the anoectin, and the saw palmetto extract is 10-15:1.5-4.5:2-4.

6. Use of the composition according to any one of claims 1 to 5 in the preparation of a medicament or cosmetic, wherein the medicament or cosmetic is used to prevent, treat, alleviate or reverse hair loss.

7. The use according to claim 6, wherein The medicine is a skin external preparation.

8. The use according to claim 7, wherein The skin external preparation is one or more of aerosol, ointment, lotion, emulsion, patch, powder, oil, cream and gel.

9. The use according to claim 6, wherein The cosmetic is a cosmetic for hair or scalp.

10. The use according to claim 9, wherein The cosmetics are one or more of shampoo, conditioner, hair treatment cream, hair lightener, hair mask, hair milk, hair lotion, hair root nutrient solution, scalp care solution, scalp essence, scalp nutrient solution, scalp ampoule, scalp essence or scalp ointment.

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