Composition for preventing or treating alopecia comprising a tubulin inhibitor
By using microtubule inhibitors such as ABT-751, TN-16, punabulin, and compressortin-A4, apoptosis of dermal papilla cells is inhibited, the growth phase is prolonged, and the problem of hair loss in modern society is solved, achieving significant hair regrowth and hair growth effects.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- CUEPEAK BIO CO LTD
- Filing Date
- 2025-01-06
- Publication Date
- 2026-07-31
AI Technical Summary
In modern society, due to environmental pollution, strong ultraviolet radiation and physiological factors, hair loss is a common problem among people of all ages. Existing technologies are unable to effectively inhibit hair loss and promote hair growth.
Microtubule inhibitors, such as ABT-751, TN-16, punabulin, and compressortin-A4, are used to promote hair growth by inhibiting apoptosis of dermal papilla cells, prolonging the growth phase, and shortening the resting and shedding phases.
It significantly increases hair regrowth, inhibits hair loss, promotes hair growth, and increases hair density.
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Figure CN122497501A_ABST
Abstract
Description
Technical Field
[0001] This invention relates to compositions containing microtubule inhibitors as active ingredients for inhibiting hair loss, promoting hair growth, or promoting hair growth.
[0002] Furthermore, the present invention relates to pharmaceutical compositions comprising microtubule inhibitors as active ingredients for inhibiting hair loss, promoting hair growth, or promoting hair growth.
[0003] Furthermore, the present invention relates to a quasi-pharmaceutical composition comprising a microtubule inhibitor as an active ingredient for inhibiting hair loss, promoting hair growth, or promoting hair growth.
[0004] Furthermore, the present invention relates to cosmetic compositions containing microtubule inhibitors as active ingredients for inhibiting hair loss, promoting hair growth, or promoting hair growth.
[0005] Furthermore, the present invention relates to products for hair or scalp containing microtubule inhibitors as active ingredients. Background Technology
[0006] Human hair primarily serves a defensive function, protecting the scalp from external stimuli such as ultraviolet rays. Secondly, it contributes to an aesthetically pleasing appearance. However, due to environmental pollution, strong ultraviolet radiation, and physiological factors like stress and hormonal imbalances in modern society, hair loss is increasingly common. Unlike in the past when it was limited to adult men, hair loss now affects people of all ages and genders. Therefore, the demand for materials to prevent or treat hair loss is extremely urgent.
[0007] As the physiological organ responsible for hair generation, the hair follicle repeats the hair growth cycle, thus relating to hair growth, maintenance, and shedding. This growth cycle is divided into the following phases: hair formation after birth, the anagen phase (active hair growth), the catagen phase (hair regression), the telogen phase (hair telogen remaining until shedding), and the exogen phase (hair loss). Numerous studies have shown that the activity of these hair follicles is manifested through hair papilla cells, particularly their proliferation and differentiation, which are primarily related to the hair growth cycle and hair formation. During the anagen phase, active hair growth, hair papilla cell proliferation and differentiation occur actively, while during the catagen, telogen, and exogen phases, when hair growth is interrupted and shedding occurs, cells undergo apoptosis. Therefore, hair growth and hair loss are closely related to the proliferation and apoptosis of dermal papilla cells. Inducing the proliferation of dermal papilla cells to prolong the growth phase or inhibiting cell apoptosis to shorten the regression, resting, and shedding phases has become a solution for improving and treating hair loss.
[0008] Hair loss is characterized by the loss of more than 100 hairs per day, with a decrease in hair in the anagen (growth) phase and an increase in hair in the catagen (transitional) or telogen (resting) phase. As hair loss progresses, the proportion of hair in the telogen phase increases sharply, while the proportion of hair in the anagen phase decreases accordingly. Hair loss can generally be classified into hereditary androgenetic alopecia (baldness), alopecia areata, tinea capitis caused by fungal infection, telogen effluvium, trichotillomania, and hair growth disorders. Among these, the most common types of hair loss include male pattern baldness (male pattern baldness), female pattern baldness, alopecia areata, and telogen effluvium. There are various causes of hair loss. The occurrence of baldness is usually attributed to genetic factors and androgens (male hormones). It is speculated that some cases of female pattern baldness also occur through the same pathway as male pattern baldness, but the clinical manifestations differ. Alopecia areata is speculated to be caused by autoimmune diseases. Telogen effluvium is a temporary form of hair loss that typically occurs after severe psychological or physical stress, such as from endocrine disorders, nutritional deficiencies, medications, childbirth, fever, or surgery. It is caused by some hairs failing to complete their full growth phase (anagen phase) and prematurely entering the telogen phase, subsequently falling out. Summary of the Invention
[0009] Technical issues Therefore, the inventors confirmed that tublin inhibitors have the effect of inhibiting hair loss, promoting hair growth, or promoting hair growth, thus completing this invention.
[0010] Therefore, the object of the present invention is to provide a composition for inhibiting hair loss, promoting hair growth, or promoting hair growth.
[0011] Furthermore, the purpose of this invention is to provide a quasi-pharmaceutical or cosmetic composition for inhibiting hair loss, promoting hair growth, or promoting hair growth.
[0012] Furthermore, the object of the present invention is to provide a product for hair or scalp.
[0013] Technical solution To achieve the aforementioned objective, the present invention provides a composition comprising a microtubule inhibitor as an active ingredient for inhibiting hair loss, promoting hair growth, or promoting hair growth.
[0014] Furthermore, the present invention provides a pharmaceutical composition comprising a microtubule inhibitor as an active ingredient for inhibiting hair loss, promoting hair growth, or promoting hair growth.
[0015] Furthermore, the present invention provides a quasi-pharmaceutical composition comprising a microtubule inhibitor as an active ingredient for inhibiting hair loss, promoting hair growth, or promoting hair growth.
[0016] Furthermore, the present invention provides a cosmetic composition containing a microtubule inhibitor as an active ingredient for inhibiting hair loss, promoting hair growth, or promoting hair growth.
[0017] Furthermore, the present invention provides a product for hair or scalp containing a microtubule inhibitor as an active ingredient.
[0018] Furthermore, the present invention provides a method for inhibiting hair loss, promoting hair growth, or alleviating hair loss symptoms, including the step of administering a microtubule inhibitor to an individual in need.
[0019] The effects of the invention In animal models, the application of the tubulin inhibitors of this invention, particularly ABT-751, TN-16, Plinabuline, and Combretastatin A4, has confirmed significantly increased hair regrowth, inhibition of hair loss, and promotion of hair growth compared to the control group. Therefore, the tubulin inhibitors of this invention can be effectively used as pharmaceuticals or cosmetics for hair loss or hair growth. Attached Figure Description
[0020] Figure 1 Photographs showing the results of observing the hair growth effect when microtubule inhibitors were applied to an animal model (hos:HR-1 mice). Figure 1It can be confirmed that, compared with the control group without the compounds, mice treated with ABT-751, TN-16, punabulin, and compressortin-A4, which are microtubule inhibitors, showed a significant increase in hair regrowth.
[0021] Figure 2 A graph showing the results of quantitatively measuring the number of hairs per unit area (hair density) after applying a microtubule inhibitor. Figure 2 The chart shows that, compared with the control group, the group that applied the microtubule inhibitor had a significant increase in hair density. Best practice
[0022] The present invention will now be described in detail.
[0023] The present invention provides a composition comprising a microtubule inhibitor as an active ingredient for inhibiting hair loss, promoting hair growth, or promoting hair growth.
[0024] Furthermore, the present invention provides a method for inhibiting hair loss, promoting hair growth, or alleviating hair loss symptoms, including the step of administering a microtubule inhibitor to an individual in need.
[0025] Microtubule inhibitors are a group of drugs that regulate or inhibit the function of tubulin, a major structural element of microtubules. As part of the cytoskeleton, which plays an important role in cells, microtubules are essential structures for cell division, cell migration, and intracellular transport.
[0026] In this invention, unlike previous functions, the microtubule inhibitors have shown hair growth efficacy in animal models.
[0027] In this invention, for example, the microtubule inhibitor may be BT-751, TN16, Compressorin-A4 or Punabulin, but the type is not limited.
[0028] The ABT-751 can be represented by the following compound I.
[0029] Compound I The compound I is the compound with CAS registration number 141430-65-1, which is ABT-751 (N-[2-[(4-hydroxyphenyl)amino]pyridin-3-yl]-4-methoxybenzenesulfonamide).
[0030] ABT-751 is a compound that targets microtubules. It has been reported that this drug has shown activity in inhibiting the growth of cancer cells by suppressing cell division in specific cancer cells.
[0031] The TN16 can be represented by the following compound II.
[0032] Compound II Furthermore, the compound II is the compound with CAS registration number 33016-12-5, which is TN-16 (3-[1-(phenylamino)ethylidene]-5-(phenylmethyl)-2,4-pyrrolidinedione).
[0033] TN-16 is a novel microtubule inhibitor with antitumor activity. It is synthesized by modifying tenuazonic acid (3-acetyl-5-sec-butyltetramic acid), a natural antibiotic isolated and identified from cultures of *Alternaria tenuis*. Although TN-16 was found to possess potent anticancer activity as early as 1967, no more potent agents have been discovered through subsequent studies. Furthermore, in 1983, it was determined that TN-16's mechanism of action is to inhibit microtubule formation by binding to sensitive sites.
[0034] In this invention, Compressorin-A4 is known to inhibit microtubule polymerization by binding to tubulin, induce apoptosis by disrupting the cytoskeleton within cancer cells, and has shown anti-angiogenic effects as a candidate anticancer agent.
[0035] Furthermore, in this invention, punabulin, known as a microtubule inhibitor, acts as an anti-angiogenic agent, simultaneously targeting cancer cells and blood vessels to inhibit the growth of cancerous tissue.
[0036] The microtubule inhibitors of the present invention are a concept that includes all pharmaceutically acceptable salts, isomers or derivatives thereof, and analogs that exhibit the same or similar effects.
[0037] In this invention, pharmaceutically acceptable salts refer to salts commonly used in pharmaceutical systems, such as: inorganic ionic salts prepared from calcium, potassium, sodium, and magnesium; inorganic acid salts prepared from hydrochloric acid, nitric acid, phosphoric acid, bromic acid, iodic acid, perchloric acid, and sulfuric acid; organic acid salts prepared from acetic acid, trifluoroacetic acid, citric acid, maleic acid, succinic acid, oxalic acid, benzoic acid, tartaric acid, fumaric acid, mandelic acid, propionic acid, citric acid, lactic acid, glycolic acid, gluconic acid, galacturonic acid, glutamic acid, glutamate, glutaric acid, glucuronic acid, aspartic acid, ascorbic acid, carbonic acid, vanillic acid, and hydroiodic acid; sulfonates prepared from methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, and naphthalenesulfonic acid; amino acid salts prepared from glycine, arginine, and lysine; and amine salts prepared from trimethylamine, triethylamine, ammonia, pyridine, and methylpyridine, etc. However, this is not a limitation.
[0038] The microtubule inhibitors may be derived from extracts, produced biologically, or synthesized chemically, and their source and preparation method are not limited.
[0039] The microtubule inhibitor of the present invention can be used to inhibit hair loss, promote hair growth, or promote hair growth.
[0040] The term "hair loss" as used in this invention refers to the absence of hair in areas where hair should normally be present, including a reduction in the amount of hair compared to a normal state. The term "hair loss" is a concept that encompasses both non-scarring and scarring hair loss, depending on whether the hair follicles are damaged. Examples include hereditary androgenetic alopecia, alopecia areata, tinea capitis caused by fungal infection, telogen effluvium, trichotillomania, hair growth disorders, as well as hair loss caused by lupus, folliculitis alopecia, lichen planus of the hair, and hair loss due to burns and / or trauma.
[0041] The term "hair loss suppression" as used in this invention refers to preventing existing hair from falling out abnormally or slowing down its rate.
[0042] The term "hair growth" as used in this invention refers to the process by which new hair grows as hair follicles transition from the resting phase to the anagen phase.
[0043] The term "promote hair growth" as used in this invention refers to inducing or activating a new hair growth process.
[0044] The term "promote hair growth" as used in this invention refers to increasing the length and thickness of existing hair, or accelerating its growth rate.
[0045] In this invention, the microtubule inhibitor, as an active ingredient, can provide a pharmaceutical composition for inhibiting hair loss, promoting hair regrowth, or promoting hair growth. Furthermore, it can be used as a pharmaceutical composition for preventing or treating hair loss.
[0046] The term "prevention" in this specification may include suppressing the occurrence of disease.
[0047] The term "treatment" in this instruction manual includes inhibiting, reducing, or eliminating the development of a disease.
[0048] The term "contains...as an active ingredient" in this specification means that the tubulin inhibitor described herein is added to the extent that it can demonstrate the effects mentioned herein. This includes the addition of multiple ingredients as byproducts to formulate the drug in multiple forms for the purpose of drug delivery and stability.
[0049] The pharmaceutical composition is capable of containing the microtubule inhibitor in a pharmaceutically effective amount.
[0050] The term "pharmaceuticalally effective amount" in this instruction manual refers to an amount sufficient to achieve the efficacy or activity of the active ingredient.
[0051] The pharmaceutical composition may also contain a pharmaceutically acceptable diluent or carrier. The diluent may be lactose, corn starch, soybean oil, microcrystalline cellulose, mannitol, or a combination thereof. The carrier may be an excipient, disintegrant, binder, lubricant, or a combination thereof. The excipient may be microcrystalline cellulose, lactose, low-substituted hydroxypropyl cellulose, or a combination thereof. The disintegrant may be calcium carboxymethyl cellulose, sodium starch glycolate, anhydrous calcium hydrogen phosphate, or a combination thereof. The binder may be polyvinylpyrrolidone, low-substituted hydroxypropyl cellulose, hydroxypropyl cellulose, or a combination thereof. The lubricant may be magnesium stearate, silica, talc, or a combination thereof.
[0052] The pharmaceutical composition can be formulated as an oral or parenteral dosage form. Oral dosage forms may be granules, powders, liquids, tablets, capsules, dry syrups, or combinations thereof. Parenteral dosage forms may be injections, ointments, sprays, patches, etc., and the dosage form is not limited.
[0053] For example, for mammals, a daily dose of one pharmaceutical composition may be approximately 0.0001 mg / kg to 10000 mg / kg, 0.0001 mg / kg to 5000 mg / kg, 0.0001 mg / kg to 1000 mg / kg, 0.0001 mg / kg to 900 mg / kg, 0.0001 mg / kg to 800 mg / kg, 0.0001 mg / kg to 700 mg / kg, 0.0001 mg / kg to 600 mg / kg, 0.0001 mg / kg to 500 mg / kg, 0.0001 mg / kg to 400 mg / kg, 0.0001 mg / kg to 300 mg / kg, 0.0001mg / kg to 200mg / kg, 1mg / kg to 1000mg / kg, 1mg / kg to 900mg / kg, 1mg / kg to 800mg / kg, 1mg / kg to 700mg / kg, 1mg / kg to 600mg / kg, 1mg / kg to 500mg / kg, 1mg / kg to 450mg / kg, 1mg / kg to 400mg / kg, 1mg / kg to 350mg / kg, 1mg / kg to 300mg / kg, 1mg / kg to 250mg / kg, 1 0 mg / kg to 1000 mg / kg, 10 mg / kg to 900 mg / kg, 10 mg / kg to 800 mg / kg, 10 mg / kg to 700 mg / kg, 10 mg / kg to 600 mg / kg, 10 mg / kg to 500 mg / kg, 10 mg / kg to 450 mg / kg, 10 mg / kg to 400 mg / kg, 10 mg / kg to 350 mg / kg, 10 mg / kg to 300 mg / kg, 10 mg / kg to 250 mg / kg, 100 mg / kg to 1 000mg / kg, 100mg / kg to 900mg / kg, 100mg / kg to 800mg / kg, 100mg / kg to 700mg / kg, 100mg / kg to 600mg / kg, 100mg / kg to 500mg / kg, 100mg / kg to 450mg / kg, 100mg / kg to 400mg / kg, 100mg / kg to 350mg / kg, 100mg / kg to 300mg / kg, 100mg / kg to 250mg / kg, 200mg / kg The dosage can be up to 1000 mg / kg, 200 mg / kg to 900 mg / kg, 200 mg / kg to 800 mg / kg, 200 mg / kg to 700 mg / kg, 200 mg / kg to 600 mg / kg, 200 mg / kg to 500 mg / kg, 200 mg / kg to 450 mg / kg, 200 mg / kg to 400 mg / kg, 200 mg / kg to 350 mg / kg, 200 mg / kg to 300 mg / kg, or 200 mg / kg to 250 mg / kg, but is not limited thereto. The pharmaceutical composition of this application can be administered once daily or divided into several doses. In any case, the dosage does not limit the scope of this application.
[0054] The pharmaceutical compositions provided in this specification can be administered to mammals including humans, dogs, cats, horses, cattle, pigs, goats, rabbits, mice, rats, etc., or cells, tissues or cultures thereof isolated from them. In one example, the subject can be an individual who needs to prevent, improve and / or treat the skin disease described above, or an individual (human mammals) suffering from a skin disease or cells, tissues or cultures thereof isolated from them.
[0055] A pharmaceutical composition may comprise 1 to 80% by weight, 5% to 80% by weight, 5% to 75% by weight, 5% to 70% by weight, 5% to 65% by weight, 50% to 70% by weight, 55% to 65% by weight, 60% to 65% by weight, 10% to 60% by weight, 15% to 60% by weight, 20% to 60% by weight, 1% to 50% by weight, 5% to 50% by weight, 10% to 50% by weight, 15% to 50% by weight, and 20% to 50% by weight. The microtubule inhibitors are 1 to 40% by weight, 5% to 40% by weight, 10% to 40% by weight, 15% to 40% by weight, 20% to 40% by weight, 1% to 30% by weight, 5% to 30% by weight, 10% to 30% by weight, 15% to 30% by weight, 20% to 30% by weight, 1% to 25% by weight, 5% to 25% by weight, 10% to 25% by weight, 15% to 25% by weight, 20% to 25% by weight, or 23% to 25% by weight.
[0056] Alternatively, the composition can be a topical skin composition.
[0057] The aforementioned topical skin agents may be creams, gels, skin emulsifiers, skin suspensions, transdermal patches, medicated bandages, lotions, sprays, or combinations thereof, but are not limited thereto.
[0058] In this invention, the skin topical agent can be appropriately combined with ingredients commonly used in skin topical agents such as cosmetics or pharmaceuticals, for example, with aqueous ingredients, oily ingredients, powder ingredients, alcohols, moisturizers, thickeners, ultraviolet absorbers, whitening agents, preservatives, antioxidants, surfactants, fragrances, colorants, various skin nutrients, metal ion chelating agents, sugars, or combinations thereof, as needed.
[0059] Furthermore, the present invention provides a quasi-pharmaceutical composition comprising a microtubule inhibitor as an active ingredient for inhibiting hair loss, promoting hair regrowth, or promoting hair growth. It can also be used as a quasi-pharmaceutical composition for preventing or treating hair loss.
[0060] In this invention, a quasi-medicine refers to all products that are not related to the treatment or prevention of a disease.
[0061] In this invention, "quasi-medicine" refers to all products that are not related to the treatment or prevention of diseases. The term "quasi-medicine" refers to articles used for the purpose of diagnosing, treating, improving, alleviating, managing, or preventing diseases in humans and animals, but with a milder effect than pharmaceuticals. For example, according to the Korean Pharmaceutical Affairs Act, quasi-medicine excludes articles used for pharmaceutical purposes, including but not limited to fiber and rubber products used in the treatment or prevention of diseases in humans / animals, products with mild or indirect effects on the human body, those that are not instruments or machinery or similar, and bactericides and insecticides used to prevent infectious diseases.
[0062] The quasi-pharmaceutical composition or dosage form of the present invention is not particularly limited, but preferably can be a disinfectant, bath liquid, mouthwash, wet wipes, laundry soap, hand sanitizer, humidifier filler, mask, ointment or filter filler, etc.
[0063] When the quasi-pharmaceutical contains the composition of the present invention, it can be used directly or together with other quasi-pharmaceutical ingredients, and can be used appropriately according to conventional methods. The amount of active ingredient mixed can be appropriately determined according to the purpose of use, and the quasi-pharmaceutical composition of the present invention may contain 0.01 to 20 weight percent of the microtubule inhibitor relative to the total weight of the composition.
[0064] Furthermore, the present invention provides a cosmetic composition for skin diseases containing a microtubule inhibitor as an active ingredient, for inhibiting hair loss, promoting hair growth, or alleviating hair loss symptoms. It can also be used as a cosmetic composition for the prevention or treatment of hair loss.
[0065] The term “improvement” in this instruction manual can refer to any behavior that at least reduces parameters related to the state to be relieved or treated, such as the severity of symptoms.
[0066] Relative to the total weight of the cosmetic composition, it may contain 0.0001 to 80% by weight, 0.01 to 70% by weight, 0.01 to 60% by weight, 0.01 to 50% by weight, 0.01 to 40% by weight, 0.01 to 30% by weight, 0.1 to 70% by weight, 0.1 to 60% by weight, 0.1 to 50% by weight, 0.1 to 40% by weight, and 0.1% to [missing information - likely a percentage]. The tubulin inhibitor may be present in amounts of 30% by weight, 0.5% to 70% by weight, 0.5% to 60% by weight, 0.5% to 50% by weight, 0.5% to 40% by weight, 0.5% to 30% by weight, 1% to 70% by weight, 1% to 60% by weight, 1% to 50% by weight, 1% to 40% by weight, or 1% to 30% by weight. For example, it may contain 30% by weight of the tubulin inhibitor, but is not limited thereto.
[0067] The cosmetic composition is not particularly limited to a specific dosage form and can be appropriately selected according to the target content. For example, the cosmetic composition may have a soluble dosage form, an emulsifying dosage form, or a dispersing dosage form. The cosmetic composition may have a cosmetic dosage form of softening lotion, nourishing lotion, massage cream, nourishing cream, serum, mask, gel, ampoule, or skin patch type, but is not limited to these.
[0068] In addition to the active ingredients disclosed in this specification, the cosmetic composition may also contain ingredients commonly used in cosmetic compositions, such as antioxidants, stabilizers, solubilizers, surfactants, dispersants, emulsifiers, preservatives, vitamins, pigments and fragrances, as well as other common auxiliary agents and carriers.
[0069] Furthermore, the present invention provides hair or scalp products containing microtubule inhibitors as active ingredients.
[0070] The product may be one or more of the following: hair growth agent, scalp cleanser, scalp exfoliant, scalp massage agent, scalp care agent, detergent, shampoo, tonic, conditioner, hair lotion, hair gel, hair mask, hair cream, serum, powder, spray, hair oil, soap, ointment, hair styling agent, hair dye, and perming agent.
[0071] Another embodiment of the present invention provides a method for inhibiting hair loss, promoting hair growth or preventing, improving or treating hair loss, comprising the step of administering a therapeutically effective amount of a microtubule inhibitor to an individual in need.
[0072] The term "effective quantity" refers to the quantity that can produce the effect mentioned.
[0073] The individuals may be mammals, such as humans, cattle, horses, pigs, dogs, sheep, goats, or cats. The individuals may be those who require preventative, ameliorative, or therapeutic effects for skin diseases.
[0074] The terms “administered”, “introduced”, and “transplanted” used in this specification are used interchangeably and may refer to a composition that is delivered into an individual by a method or route that causes at least partial localization at a desired site.
[0075] Administration can be performed using methods known in the technical field to which this invention pertains. The route of administration, frequency of administration, and other methods of administration can be appropriately selected by a person skilled in the art. For example, administration can be performed directly to an individual by any means via intravenous, intramuscular, oral, transdermal, mucosal, intranasal, oral, intratracheal, or subcutaneous routes. The administration can be systemic or local. The administration can be included in skin application.
[0076] In this invention, a specific example of the composition can be administered to each individual daily at doses of 0.1 mg to 1,000 mg, for example, a specific example of the composition can be administered at doses of 0.1 mg to 500 mg, 0.1 mg to 100 mg, 0.1 mg to 50 mg, 0.1 mg to 25 mg, 1 mg to 1,000 mg, 1 mg to 500 mg, 1 mg to 100 mg, 1 mg to 50 mg, 1 mg to 25 mg, 5 mg to 1,000 mg, 5 mg to 500 mg, 5 mg to 100 mg, 5 mg to 50 mg, 5 mg to 25 mg, 10 mg to 1,000 mg, 10 mg to 500 mg, 10 mg to 100 mg, 10 mg to 50 mg, or 10 mg to 25 mg. However, dosage can be prescribed in a variety of ways, taking into account factors such as preparation method, route of administration, patient's age, weight, sex, disease state, diet, administration time, route of administration, metabolic rate, and response sensitivity. Practitioners can adjust the dosage appropriately by considering these factors. Dosage can be administered once daily, or more than twice daily within clinically tolerable side effects. For administration sites, one or more sites can be used. Dosage can be administered daily or at intervals of 2 to 5 days, with a total treatment duration ranging from 1 to 30 days. If necessary, the same treatment can be repeated after the prescribed period. For animals other than humans, the same dosage per kg as for humans can be administered, or, for example, the dosage calculated based on the volume ratio (e.g., average value) of the target animal's organs (heart, etc.) to those of humans.
[0077] Another embodiment of the present invention provides the use of the microtubule inhibitor in preparing compositions for inhibiting hair loss, promoting hair growth, or promoting hair growth.
[0078] Another embodiment of the present invention provides the use of the microtubule inhibitor in the preparation of a medicament for inhibiting hair loss, promoting hair growth, or promoting hair growth.
[0079] Another embodiment of the present invention provides a food composition for inhibiting hair loss, promoting hair growth, or promoting hair growth, comprising the microtubule inhibitor of the present invention as an active ingredient.
[0080] The food composition of one embodiment of the present invention can be in liquid or solid dosage form, and can be tablets, capsules, soft capsules, pills, granules, beverages (drinks), slimming bars, chocolate, caramel dosage form, or biscuit dosage form, and its dosage form is not particularly limited. In addition to the active ingredient, the food composition of the present invention may also contain small amounts of excipients, sugars, flavorings, colorings, oils, proteins, etc., as needed.
[0081] Given the complexity of this specification, repeated content will be omitted. Unless otherwise stated, the terminology in this specification shall have the meanings commonly used by one of ordinary skill in the art to which this invention pertains.
[0082] The present invention will now be described in detail through embodiments. However, the following embodiments are merely illustrative of the invention, and the scope of the invention is not limited to these embodiments. Detailed Implementation
[0083] Example 1. Confirmation of the hair growth efficacy of microtubule inhibitors in animal models. To confirm the hair regrowth efficacy of tubulin inhibitors, hos:HR-1 (hairless) mice were used as experimental animals. Because these animal models lack hair, they offer the advantage of allowing direct application of drugs to the skin or inducing skin diseases using chemical or biological allergens for related research. Furthermore, being 8-10 weeks old, their skin thickness is approximately 0.4 mm, similar to human skin, making them useful for studying the pathological matrix of skin diseases and confirming biochemical changes within skin tissue.
[0084] The same amount of 2% ABT-751 or 2% TN-16 was applied to the dorsal skin of hos:HR-1 (hairless) mice (hereinafter referred to as HR-1 mice) once a day for 2 weeks.
[0085] After each application, measure the degree of hair regrowth. Figure 1 The results were obtained from photos taken 14 days later.
[0086] like Figure 1 As shown, it can be confirmed that compared with the control group without the compound, mice treated with ABT-751, TN-16, punabulin or compressin-A4, which are microtubule inhibitors, showed a significant increase in hair growth.
[0087] Example 2. Hair regrowth efficacy of topical application in animal models To quantitatively confirm the hair regrowth efficacy of the microtubule inhibitor, hair density was measured. Hair density was calculated based on the number of hairs per unit area. For measuring hair density, specimens were imaged using a microscope at its original magnification x400. Data was collected by directly counting the number of hairs in the relevant areas through analysis of the captured images. Based on these hair counts, charts were created to visualize the results, such as… Figure 2 As shown.
[0088] like Figure 2As shown, it can be confirmed that, compared with the control group that does not contain the compound, mice treated with ABT-751, TN-16, punabulin or compressin-A4, which are microtubule inhibitors, showed significant hair growth.
Claims
1. A composition for inhibiting hair loss, promoting hair growth, or promoting hair growth, characterized by, It contains microtubule inhibitors as an active ingredient.
2. The composition for inhibiting hair loss, promoting hair growth, or promoting hair growth according to claim 2, characterized by, The microtubule inhibitor is selected from one or more of the group consisting of ABT-751, TN16, Compressorin-A4, and Punabulin.
3. A pharmaceutical composition for inhibiting hair loss, promoting hair regrowth, or promoting hair growth, characterized in that, It contains microtubule inhibitors as an active ingredient.
4. A quasi-pharmaceutical composition for inhibiting hair loss, promoting hair regrowth, or promoting hair growth, characterized in that, It contains microtubule inhibitors as an active ingredient.
5. A cosmetic composition for inhibiting hair loss, promoting hair regrowth, or alleviating hair loss symptoms, characterized in that, It contains microtubule inhibitors as an active ingredient.
6. A product for use on hair or scalp, characterized in that, It contains microtubule inhibitors as an active ingredient.
7. The product for hair or scalp according to claim 6, characterized in that, The product is selected from one or more of the following groups: hair growth agent, scalp cleanser, scalp exfoliant, scalp massage agent, scalp care agent, detergent, shampoo, tonic, conditioner, hair cream, hair gel, hair mask, hair cream, serum, powder, spray, hair oil, soap, ointment, hair styling agent, hair dye, and perming agent.
8. A method for inhibiting hair loss, promoting hair regrowth, or alleviating hair loss symptoms, characterized in that, This includes the step of administering microtubule inhibitors to individuals in need.