阅读说明：本技术 卡拉胶寡糖的用途及含有卡拉胶寡糖的组合物 (Application of carrageenan oligosaccharide and composition containing carrageenan oligosaccharide ) 是由 张春毅 王斐 曾翰庭 易志伟 产竹华 曾润颖 何雄飞 于 2019-09-06 设计创作，主要内容包括：本发明涉及卡拉胶寡糖作为生发剂或护发剂的用途及包含卡拉胶寡糖的组合物,具体涉及卡拉胶寡糖在制备用于改善和/或促进毛发生长,或者消除和/或缓解与毛发生长状态不良有关的病症或状态的产品中的用途。本发明提供的包含卡拉胶寡糖的组合物具有显著的防脱生发功效,无刺激性、无副作用、安全性高。(The invention relates to application of carrageenan oligosaccharide as a hair growing agent or a hair care agent and a composition containing the carrageenan oligosaccharide, in particular to application of the carrageenan oligosaccharide in preparing a product for improving and/or promoting hair growth or eliminating and/or relieving symptoms or conditions related to poor hair growth conditions. The composition containing carrageenan oligosaccharide provided by the invention has remarkable alopecia preventing and hair growing effects, and has no irritation, no side effect and high safety.)

1. Use of carrageenan oligosaccharides as an active ingredient for the manufacture of a product for improving and/or promoting hair growth, or eliminating and/or alleviating a disorder or condition associated with a poor hair growth condition.

2. Use according to claim 1, wherein said condition or state associated with poor hair growth status is hair loss or slow hair growth.

3. Use according to claim 1 or 2, wherein the carrageenan oligosaccharides are selected from the group consisting of: at least one of kappa-carrageenan oligosaccharide, iota-carrageenan oligosaccharide and lambda-carrageenan oligosaccharide;

Preferably, the carrageenan oligosaccharides comprise at least kappa-carrageenan oligosaccharides.

4. The use according to claim 1 or 2, wherein the carrageenan oligosaccharides comprise 0.01-1 wt% of the total weight of the product.

5. Use according to claim 1 or 2, characterized in that the product comprises physiologically acceptable adjuvants; preferably, the physiologically acceptable excipients include small molecule polyols and non-ionic surfactants.

6. a composition, characterized in that the composition comprises: (1) carrageenan oligosaccharide, and (2) pharmaceutically or cosmetically acceptable adjuvants, wherein the carrageenan oligosaccharide is present in the composition at a concentration that promotes hair growth and improves hair condition, and the composition is a pharmaceutical or cosmetic.

7. The composition according to claim 6, wherein the carrageenan oligosaccharides comprise 0.01-1 wt% of the total weight of the composition.

8. The composition according to claim 6 or 7, wherein the pharmaceutically or cosmetically acceptable adjuvant comprises a small molecule polyol and a non-ionic surfactant; the mass ratio of the small-molecule polyol to the nonionic surfactant is preferably 2-12: 1-10.

9. The composition of claim 8, wherein the small molecule polyol is selected from the group consisting of: at least one of glycerol, propylene glycol, butylene glycol, and pentylene glycol; the nonionic surfactant is selected from the group consisting of: at least one of PEG, Tween and SPAN.

10. A hair restorer or hair conditioner comprises carrageenan oligosaccharide as effective component for improving hair papilla cell activity, especially for improving androgen induced hair papilla cell injury activity.

Technical Field

The invention relates to the use of carrageenan oligosaccharides, in particular to the effect of carrageenan oligosaccharides as an active ingredient for improving hair growth, more particularly to the use in preventing hair loss and promoting hair growth.

Background

Alopecia and baldness caused by the same are common phenomena, and mental stress caused by the same brings about a lot of troubles and obstacles to human relationships and social life. With the acceleration of pace of life, the increase of living pressure and environmental pressure, people suffering from alopecia are younger and younger at present, and the alopecia of women is gradually increased not only for men, so that a plurality of treatment medicines, hair care external products and hair growth external products for preventing alopecia are provided.

The reasons for alopecia are complex and are the combined action of various factors. The most common type of hair loss is "androgenic alopecia", otherwise known as "seborrheic alopecia", the main cause of which is that sebum secretion is regulated by androgens, and when sebum is abnormally secreted or abnormally produced, hair health is affected, thus causing hair loss. At present, the problems of scalp grease are generally solved by methods such as androgen control or cleaning in the medicines and hair care products. For example, taking a bautamide tablet (i.e., N- (1, 1-dimethylethyl) -3-oxo-4-aza-5 α -st-1-en-17 β -amide) inhibits androgen levels, promotes hair growth, and treats androgenic alopecia and baldness. Topical minoxidil (6- (1-piperidinyl) -2, 4-pyrimidinediamine, 3-oxide) is used to treat androgenic alopecia. The two medicines have obvious treatment effect, but simultaneously, the level of androgen is reduced, so that corresponding side effects such as erectile dysfunction, hyposexuality, rash, inflammation, pruritus and the like on external application are also generated.

Some cosmetics achieve hair loss prevention or hair growth promotion effects by adding plant extracts. For example, chinese patent document CN105640803A discloses an anti-dandruff, anti-alopecia and hair care product and a preparation method thereof, which utilizes plant essential oil to disinfect and resist bacteria and balance the oil secretion on the surface layer of skin; chinese patent document CN101810553A discloses a hair loss preventing and hair growth promoting composition, which comprises various plant extracts such as angelica sinensis, polygonum multiflorum, radix sileris, radix sophorae flavescentis, rhizoma zingiberis, notopterygium root and the like. According to the theory of traditional Chinese medicine, the extracts generally have the efficacies of dispelling wind, removing dampness, promoting blood circulation, reducing pathogenic fire and the like, but the functional components of the extracts are unclear, so the action principle is unclear, and the extracts are easy to cause adverse reactions such as allergy, irritation, dermatitis and the like due to the complex components. Therefore, the development of a new product having the effects of protecting hair, preventing hair loss, and promoting hair growth is still expected by those skilled in the art.

Carrageenan is a sulfated galactan extracted from marine red algae (Gelidium amansii, Carrageenan, Pelvetia siliquosa, Eucheuma Gelatinosum, etc.), and has a skeleton structure formed by alternately connecting 1, 3-beta-D galactose and 1, 4-alpha-D galactose. The carrageenan oligosaccharide can be prepared by degrading the carrageenan through a chemical method or a biological method, is oligosaccharide, has small molecular weight and good solubility, and has various physiological activities. The gelling effect of the carrageenan oligosaccharide has immunoregulation and anti-tumor activity; the protective effect on radiation damage is obvious; has antibacterial and antiviral activity; has obvious antioxidant activity; has anticoagulant activity. Various red algae extracts are listed in cosmetic catalogues, such as gelidium amansii extract, chenopodium album extract, carrageenan sodium and the like, but the application of carrageenan oligosaccharide in cosmetics is not reported.

Common carrageenan oligosaccharides mainly comprise Kappa (Kappa-) type, Iota (Iota-) type and Lambda (Lambda-) type according to the connection mode of monosaccharides and the positions of groups, but no single-component or mixed-component carrageenan oligosaccharide is reported to have the functions of protecting hair, preventing hair loss and growing hair.

Disclosure of Invention

The invention aims to provide the function of carrageenan oligosaccharide as an active ingredient for improving hair growth, in particular to the application of carrageenan oligosaccharide in preventing alopecia and promoting hair growth. The present invention has surprisingly found that the use of carrageenan oligosaccharides and compositions thereof is effective in improving hair growth status, and in particular in preventing hair loss and promoting hair growth.

To this end, in a first aspect, the present invention provides the use of carrageenan oligosaccharides as an active ingredient in the manufacture of a product for improving and/or promoting hair growth, or eliminating and/or alleviating a condition or condition associated with a poor hair growth condition.

Further, the carrageenan oligosaccharides are selected from the group consisting of: at least one of kappa-carrageenan oligosaccharide, iota-carrageenan oligosaccharide and lambda-carrageenan oligosaccharide.

specifically, the kappa-carrageenan oligosaccharides are selected from the following group: at least one of kappa-carrageenan trisaccharide, kappa-carrageenan pentasaccharide, kappa-carrageenan heptasaccharide, kappa-carrageenan nonasaccharide, kappa-carrageenan undecanose, kappa-carrageenan decatrisaccharide, kappa-carrageenan pentadecasaccharide, kappa-carrageenan heptasaccharide, and kappa-carrageenan nonasaccharide; preferably kappa-carrageenan pentasaccharide.

further, the condition or state associated with poor hair growth state refers to alopecia or slow hair growth rate.

Further, the alopecia refers to androgenetic alopecia.

further, the product is a topical application product.

Further, the product is a topical application product for external application to the skin.

Further, the product is a pharmaceutical or cosmetic.

Further, the product is in the form of a solution, a cream, a paste, a cream, or a gel.

Further, the carrageenan oligosaccharide accounts for 0.01-1 wt%, preferably 0.01-0.5 wt%, more preferably 0.1-0.5 wt% of the total weight of the product.

Further, the product comprises: (1) the carrageenan oligosaccharide and (2) physiologically acceptable auxiliary materials.

Further, the physiologically acceptable auxiliary material is selected from the group consisting of: at least one of emulsifier, colorant, humectant, solubilizer, and antiseptic.

Further, the physiologically acceptable auxiliary materials comprise small molecule polyol and nonionic surfactant.

Further, the small molecule polyol is selected from the group consisting of: at least one of glycerol, propylene glycol, butylene glycol and pentylene glycol, preferably glycerol.

Further, the nonionic surfactant is selected from the group consisting of: at least one of polyethylene glycol (PEG), tween and SPAN, preferably PEG, and more preferably PEG-400.

In a second aspect, the present invention provides a composition, characterized in that it comprises: (1) carrageenan oligosaccharide, and (2) pharmaceutically or cosmetically acceptable adjuvants, wherein the carrageenan oligosaccharide is present in the composition at a concentration that promotes hair growth and improves hair condition, and the composition is a pharmaceutical or cosmetic.

Further, the carrageenan oligosaccharides are selected from the group consisting of: at least one of kappa-carrageenan oligosaccharide, iota-carrageenan oligosaccharide and lambda-carrageenan oligosaccharide.

Specifically, the kappa-carrageenan oligosaccharides are selected from the following group: at least one of kappa-carrageenan trisaccharide, kappa-carrageenan pentasaccharide, kappa-carrageenan heptasaccharide, kappa-carrageenan nonasaccharide, kappa-carrageenan undecanose, kappa-carrageenan decatrisaccharide, kappa-carrageenan pentadecasaccharide, kappa-carrageenan heptasaccharide, and kappa-carrageenan nonasaccharide; preferably kappa-carrageenan pentasaccharide.

Further, the carrageenan oligosaccharide accounts for 0.01-1 wt%, preferably 0.01-0.5 wt%, and more preferably 0.1-0.5 wt% of the total weight of the composition.

Further, the acceptable auxiliary materials in the medicine or the cosmetics are selected from the following groups: at least one of emulsifier, colorant, humectant, solubilizer, and antiseptic.

Further, the pharmaceutically or cosmetically acceptable auxiliary materials include small molecule polyols and nonionic surfactants.

Further, the small molecule polyol is selected from the group consisting of: at least one of glycerol, propylene glycol, butylene glycol and pentylene glycol, preferably glycerol.

further, the nonionic surfactant is selected from the group consisting of: at least one of PEG, Tween and SPAN, preferably PEG, and more preferably PEG-400.

Further, the mass ratio of the small-molecule polyol to the nonionic surfactant is 2-12: 1-10.

In a preferred embodiment, the glycerol represents from 1 to 6% by weight, preferably from 1 to 4% by weight, of the total weight of the composition; the PEG-400 is present in an amount of 0.5 to 5 wt%, preferably 0.5 to 2 wt%, based on the total weight of the composition.

in a specific embodiment, the composition consists of carrageenan oligosaccharides, glycerin, PEG-400, and water.

Further, the composition is in the form of a solution, a cream, a paste, a cream, or a gel.

In a third aspect, the invention provides a hair restorer or hair conditioner, which takes carrageenan oligosaccharide as a pharmacodynamic active ingredient and is used for improving the vitality of hair papilla cells.

Further, carrageenan oligosaccharide is used as an active ingredient for protecting hair, preventing hair loss, and/or promoting hair growth.

Further, carrageenan oligosaccharide is used as an active ingredient for improving the activity of hair papilla cells; in particular, carrageenan oligosaccharides are used to increase the viability of damaged hair papilla cells caused by androgens (such as dihydrotestosterone).

Further, carrageenan oligosaccharides are used to promote the ability of dermal papilla cells to secrete cytokines.

Further, carrageenan oligosaccharides are used to promote hair length growth and hair weight increase.

further, the carrageenan oligosaccharides are selected from the group consisting of: at least one of kappa-carrageenan oligosaccharide, iota-carrageenan oligosaccharide and lambda-carrageenan oligosaccharide.

Specifically, the kappa-carrageenan oligosaccharides are selected from the following group: at least one of kappa-carrageenan trisaccharide, kappa-carrageenan pentasaccharide, kappa-carrageenan heptasaccharide, kappa-carrageenan nonasaccharide, kappa-carrageenan undecanose, kappa-carrageenan decatrisaccharide, kappa-carrageenan pentadecasaccharide, kappa-carrageenan heptasaccharide, and kappa-carrageenan nonasaccharide; preferably kappa-carrageenan pentasaccharide.

The carrageenan oligosaccharide is oligosaccharide with low polymerization degree obtained by hydrolyzing carrageenan or red algae with carrageenin enzyme, and can be obtained commercially. Carrageenan oligosaccharide has various biological activities, but the functions of protecting hair, preventing hair loss and growing hair in the cosmetic field are not reported before the application date of the invention. The invention performs experiments on carrageenan oligosaccharide, and verifies that the carrageenan oligosaccharide has the functions of preventing hair loss and growing hair by using a cell model.

When the carrageenan oligosaccharide is further applied to an animal model, aiming at the skin environment (skin contains grease), two components of small molecular polyol and surfactant are selected and compounded with the carrageenan oligosaccharide, and the penetration and dispersion of the carrageenan oligosaccharide on natural skin are promoted by utilizing the compatibility of alcohol to water and oil and the dispersion characteristic of the surfactant, so that the carrageenan oligosaccharide can effectively play a role when being applied to the natural skin.

The small molecular polyol used in the invention is a polyol with a carbon chain length of 10 or less. The small molecular polyol used for compounding can be selected from small molecular polyols which have the compatible characteristics of water and oil and the moisturizing property and are commonly used in medicines or cosmetics, and the small molecular polyols comprise glycerol, propylene glycol, butanediol, pentanediol and the like; surfactants may include polyethylene glycol, tween, SPAN, and the like. Glycerol and polyethylene glycol are preferred in the present invention due to a combination of safety, non-irritation, and approved use. The glycerol has the compatible characteristics of water and oil, is beneficial to the permeation of carrageenan oligosaccharide, and meanwhile, the glycerol has the moisturizing effect and is beneficial to increasing the water required by the normal metabolism of hair; third, glycerin is a well-recognized raw material for pharmaceuticals and cosmetics with high safety. The polyethylene glycol is a safe nonionic surfactant, is helpful for reducing surface tension, enhancing the contact of carrageenan oligosaccharide and glycerol on skin, and promoting penetration to fully play a role in promoting hair growth.

The auxiliary materials which can be used for compounding the carrageenan oligosaccharide are various, in order to provide a composition which is convenient to further compound with other auxiliary materials to form various products, the composition which is composed of kappa-carrageenan pentasaccharide, glycerol, PEG-400 and water and has the hair loss preventing and hair growing effects is preferably selected, and the composition can be applied to raw materials of hair care products and can also be directly used as the hair care products.

In summary, compared with the prior art, the invention has the following advantages:

(1) The invention provides a new application of carrageenan oligosaccharide. The carrageenan oligosaccharide has high safety, no side effect and no irritation when used for preventing alopecia and nourishing hair. The existing products for preventing hair loss and nourishing hair mainly comprise finasteride, minoxidil and plant extracts, and the finasteride and minoxidil have strong side effects; plant extracts are prone to produce irritation due to their complex composition.

(2) The carrageenan oligosaccharide has clear mechanism and definite effect on the anti-hair loss and hair growth effects, and the inhibition effect of dihydrotestosterone on hair papilla cells is proved to be relieved by the carrageenan oligosaccharide for the first time, so that the activity of the hair papilla cells is improved. The plant extract widely used in the prior art has complex components, some components even have bad or negative effects on hair loss prevention and hair care, the hair loss prevention and hair growth promotion effects are reduced, the extract effects in different batches are unstable, the cost is increased, and waste is caused.

(3) The composition has the effects of protecting hair, preventing alopecia and promoting hair growth, and has the advantages of remarkable anti-alopecia and hair growth-promoting effect, no irritation, no side effect and high safety.

Drawings

Various other advantages and benefits will become apparent to those of ordinary skill in the art upon reading the following detailed description of the preferred embodiments. The drawings are only for purposes of illustrating the preferred embodiments and are not to be construed as limiting the invention. In the drawings:

FIG. 1 is a graph of the effect of different concentrations of DHT on dermal papilla cell viability;

FIG. 2 is a graph of the effect of different concentrations of carrageenan oligosaccharides on dermal papilla cell viability;

FIG. 3 shows the effect of carrageenan oligosaccharides on VEGF expression when acting on an androgen alopecia in vitro cell model;

FIG. 4 shows the effect of DHT on the expression levels of DKK-1, TGF- β 2, β -catenin, and AR when applied to hair papilla cells;

FIG. 5 shows the effect of carrageenan oligosaccharides (DP3-19) on the expression levels of DKK-1, TGF- β 2, β -catenin and AR when they act on an in vitro cell model of androgenetic alopecia;

FIG. 6 shows the effect of kappa-carrageenan pentasaccharide (DP5) on the expression levels of DKK-1, TGF-beta 2, beta-catenin and AR when applied to an in vitro cell model of androgenetic alopecia;

Figure 7 shows the results of transdermal permeation of kappa-carrageenan pentasaccharide and compositions thereof.

Detailed Description

Exemplary embodiments of the present disclosure will be described in more detail below with reference to the accompanying drawings. While exemplary embodiments of the present disclosure are shown in the drawings, it should be understood that the present disclosure may be embodied in various forms and should not be limited to the embodiments set forth herein. Rather, these embodiments are provided so that this disclosure will be thorough and complete, and will fully convey the scope of the disclosure to those skilled in the art.

The invention is described generally and/or specifically for the materials used in the tests and the test methods, in the following examples,% means wt%, i.e. percent by weight, unless otherwise specified. The reagents or instruments used are not indicated by manufacturers, and are all conventional reagent products which can be obtained commercially.