KR100917673B1 - Composition for preventing alopecia or growing hair containing the cation/anion mixed surfactant comprising a caffein - Google Patents

Abstract

The present invention relates to a hair composition for preventing hair loss and hair growth, and more particularly, a bilayer including caffeine that inhibits the growth of hair follicle cells (hair papilla cells) and inhibits the action of an active male hormone, dihydrotestosterone (DHT). By containing a cationic / anionic surfactant mixed vesicle having a cationic structure, it promotes adsorption to the hair and the scalp, and prevents hair loss produced to enhance the effect of caffeine without relatively irritating the scalp with a small amount of caffeine. It relates to a composition for hair for hair growth.

Caffeine, cationic / anionic surfactant mixed vesicles, enhance effects, prevent hair loss, hair growth

Description

Composition for preventing alopecia or growing hair containing the cation / anion mixed surfactant comprising a caffein}

The present invention relates to a hair composition for preventing hair loss and hair growth, and more particularly, a bilayer including caffeine that inhibits the growth of hair follicle cells (hair papilla cells) and inhibits the action of an active male hormone, dihydrotestosterone (DHT). By containing a cationic / anionic surfactant mixed vesicle having a cationic structure, it promotes adsorption to the hair and the scalp, and prevents hair loss produced to enhance the effect of caffeine without relatively irritating the scalp with a small amount of caffeine. It relates to a composition for hair for hair growth.

In the modern society that emphasizes beauty, various studies are being actively conducted around the world to treat and promote hair growth of men or women suffering from severe mental pain due to genetic or environmental hair loss.

Human hair is about 100,000 to 150,000, each hair will grow and degenerate through different cycles. Hair is a growing period (Anagen), a degenerative period (Catagen) where metabolic processes slow down while maintaining the shape of the hair, and hair papilla atrophy, hair follicles atrophy gradually, hair roots are pushed upwards, and the hair follicles become smaller (Telogen) The three-step cycle of) is repeated, and the hair cycle and lifespan may vary according to various conditions such as nutrition, medical history, heredity, constitution, hormone secretion or aging. In alopecia patients, the growth phase of the hair transitions to the degenerative and resting phases, and the growth phase ratio is lowered, leading to more hair falling out abnormally and atrophy of hair follicles.

The most common causes of hair loss include genetic causes and male hormones. In other words, hair loss must have a genetic predisposition and its expression depends on male hormones. The major male hormones involved in hair loss are the most active male hormones, dihydrotestosterone (DHT), activated by 5 alpha-reductase enzymes, as well as stress, illness, childbirth, changes in diet, irregular life, and blood circulation. Circulation disorders, infectious inflammation and peroxides are widely known to be involved in hair loss. However, the decisive cause for hair loss has not yet been identified, and with the advent of the industrial informatization era, the overall hair loss population has increased, and among the recently increased hair loss patients, the lower age group and the women have been prominent.

Among the existing anti-hair loss treatments, external minoxidil, approved by the US FDA, leads to the growth phase in the resting hair cycle and maintains the induced growth phase hair cycle in addition to its vasodilatation function as its unique potassium channel opener. Activity has been reported (British Journal of Dermatology. 2004; 150: 186-194).

In addition, an oral administration drug, Finasteride (Propecia; MSD), which inhibits the action of 5 alpha-reductase and inhibits the production of the active male hormone dihydrotestosterone, is marketed as a hair regrowth with the approval of the US FDA. However, there is a limit to use as the occurrence of expensive and side effects are reported. Thus, there has been a continuing need for drugs that are free of hair growth and side effects compared to the two major drugs previously developed.

As such, research on hair loss preventing agents and hair loss agents has been intensified, and various products have been developed. However, excellent efficacy and safe hair loss preventing agents are insufficient. Related products currently developed include minoxidil in the West, Propecia hair regrowth and hair growth agents containing herbal extracts in Japan, but it is still too early to address hair loss and hair growth in terms of efficacy.

Recently, caffeine stimulates the metabolism of dermal papilla cells to promote hair follicle growth (Zygote, 2004; 12; 31-38, Arch Dermatol Res, 2005; 296; 450) and dihydrotestosterone, an active male hormone that atrophies hair follicles Research has shown that it inhibits the action of (International Journal of Dermatology, 2007; 46; 27-35). However, some studies show that too much caffeine may affect the dermal papilla cells and cause cell death (Cancer Res, 2004; 64; 3344-3349). In other words, if caffeine reaches hair follicles in an amount sufficient to prevent hair loss and hair growth, 60 cups of caffeine-containing coffee or tea should be consumed per day or caffeine solution that can be applied to the scalp will cause hair loss. Due to the high efficacy and safe hair loss prevention agent development is insufficient.

Therefore, there is an urgent need for a method capable of improving the hair growth prevention and hair growth effects of caffeine without the scalp irritation caused by caffeine in a relatively small amount.

Accordingly, the present inventors have tried to find a delivery method capable of adsorbing caffeine to the hair and the scalp more, so as to promote hair growth prevention and hair growth effects with a relatively small amount of caffeine without stimulation, and caffeine is a bilayer-type cation. By capturing into a cationic / anionic surfactant mixed vesicle having sex, it was found that the composition for hair containing the same enhances hair loss prevention and hair growth effects without scalp irritation.

It is therefore an object of the present invention to provide a composition for hair for hair loss prevention and hair growth.

In order to achieve the above object, the present invention provides a composition for preventing hair loss and hair growth containing a cation / anionic surfactant mixed vesicle having a bilayer structure containing caffeine.

The composition for hair according to the present invention contains a cation / anionic surfactant mixture having a double layered cationic composition containing caffeine as an active ingredient, a cationic surfactant having a mole fraction of 0.45 to 0.90, and an anionic surfactant having a mole fraction of 0.55 to 0.10. By containing cicle, caffeine is better adsorbed to hair and scalp to deliver it to the dermal papilla and promote the effect of caffeine, which promotes the growth of hair follicle cells and inhibits the action of the active male hormone dihydrotestosterone (DHT). It has been shown to induce hair growth and alleviate alopecia.

Hereinafter, the present invention will be described in more detail.

Hair generally has an isoionic point and isoelelctric point. In particular, the isoelectric point refers to the pH when it does not move in the electric field in relation to the acid-base characteristics of the hair surface. Therefore, this isoelectric point has an important effect when adsorbing active ingredients to hair. Human hair is generally known to have an isoelectric point between pH 3.5 and pH 4.0. And since most of the cosmetic composition for hair and scalp is at least pH 5.0 or more when applied to the hair and scalp the hair becomes an environment above the isoelectric point to show the anion. Therefore, more negatively adsorbed compositions are adsorbed on such anionic hair. In addition, membranes of biological tissues such as hair and scalp have a double layer structure. Therefore, to apply the active ingredient through the membranes of biological tissues such as hair and scalp, the active ingredient is better delivered by affinity and is more likely to penetrate hair and scalp when it is stabilized by a bilayer structure similar to the membrane of biological tissues.

Based on this theory, in the present invention, relatively small amount of caffeine is well adsorbed on the surface of the anion-containing hair so that it can prevent hair loss and promote hair growth effect without irritation, while maintaining the membrane of biological tissues such as hair and scalp. It has been developed a hair composition that can be easily delivered to the penetration easily.

Unless stated otherwise, all percentages and ratios set forth herein are based on weight.

Caffeine is a xantine structure with three methyl groups, 1-1.5% in Brazilian coffee beans, 1-5% in oriental tea leaves, 3% in Cola fruit in tropical Africa, 1-2% in Mate tea in Paraguay, and Brazil. It is an excitable component present in 3 ~ 5% of guarana seeds. It is white light crystal. Caffeine is known as a central nervous stimulant, respiratory stimulant, cardiac and diuretic, and is known to be effective in reducing fatigue and in migraine or heart disease. However, much is not known about the effects of hair growth. However, studies related to hair growth have shown that caffeine is a phosphodiestearase inhibitor that promotes hair follicle growth by stimulating the metabolism of dermal papilla cells by increasing cell cAMP levels. It also inhibits the action of testosterone, a male hormone that causes hair loss by contracting hair follicles, and dihydrotestosterone, an active male hormone produced therefrom. However, too much caffeine content can affect the dermal papilla cells and cause necrosis, which may cause hair loss. Therefore, it is important to obtain hair growth prevention and hair growth effects with a content of caffeine that does not stimulate the dermal papilla cells.

The hair composition according to the present invention contains caffeine in an amount of 0.001% to 0.01%, preferably 0.001% to 0.005%, based on the total weight of the composition. When the content of caffeine is 0.001% or less, hair loss prevention and hair growth effects are less. If the caffeine content is 0.01% or more, it may cause hair loss because it may affect the dermal papilla cells and cause necrosis of the cells due to scalp stimulation. .

Cationic / anionic surfactant mixed vesicles with cationicity of double layer structure are cationic so that adsorption on the anionic hair surface and scalp is better, and after adsorption, membranes of biological tissues such as hair surface and scalp and It has a similar bilayer structure, and its affinity allows for better penetration of caffeine, an active ingredient, into hair and scalp. This infiltrated caffeine diffuses from the hair and scalp and is better delivered to the dermal papilla cells to promote hair loss prevention and hair growth effects.

This cationic / anionic surfactant mixed vesicle having a bilayer structure is a mixed system consisting of a cationic surfactant of a single alkyl group having 16 to 18 carbon atoms and an anionic surfactant of a single alkyl group having 12 carbon atoms. And form a stable bilayer vesicle. In addition, for the cationic / anionic surfactant mixed vesicle to be cationic, the mole fraction of the cationic surfactant of a single alkyl group of 16 to 18 carbon atoms must be between 0.45 and 0.90.

As for the cationic / anionic surfactant mixed vesicle having a bilayer structure of cationic used in the present invention, cationic surfactants have a mole fraction of 0.45 to 0.90, and anionic surfactants have a mole fraction of 0.55 to 0.10.

The cationic surfactant used in the present invention is appropriately cetyltrimethylammonium chloride or octadecyltrimethylammonium chloride, and the anionic surfactant is preferably, but not limited to, ammonium lauryl sulphate or sodicurlauryl sulfate. .

The hair composition according to the present invention contains the above cationic / anionic surfactant mixed vesicles at 0.1% to 0.2% based on the total weight of the composition. If the content of the vesicle is 0.1% or less, it is difficult to capture the caffeine as an active ingredient, and when 0.2% or more, it is difficult to use because it has a very low solubility in water and a strong hydrophobic complex due to strong attraction between the counter ions.

Hair composition for hair loss prevention and hair growth of the present invention is not particularly limited in formulating, but may be a cosmetic composition having a formulation such as hair tonic, scalp treatment, hair shampoo, hair conditioner and hair cream.

Hereinafter, the structure and the effect of the present invention will be described in more detail with reference to Examples and Test Examples. However, these examples are for illustrating the present invention, and the present invention is not limited only to these examples.

[Examples 1-4 and Comparative Examples 1-3]

Each of the components shown in Table 1 were mixed to prepare Examples 1 to 4 and Comparative Examples 1 to 3 (unit: wt%).

ingredient Comparative Example 1 Comparative Example 2 Comparative Example 3 Example 1 Example 2 Example 3 Example 4 Caffeine 0.002 0.003 0.004 0.002 0.002 0.002 0.002 Octadecyltrimethylammonium chloride - - 0.06 0.09 0.12 0.18 Ammonium Lauryl Sulfate - - 0.04 0.01 0.08 0.02 Purified water balance balance balance balance balance balance balance

Test Example 1 Stability Test

UV spectroscopy was used to determine the stability of cation-containing cationic / anionic surfactant mixed vesicles having a bilayer structure. Examples 1 and 3 show that the mole fraction of octadecyltrimethylammonium chloride, which is a cationic surfactant of a single alkyl group, is 0.55, but both caffeine / anionic surfactant mixed vesicles with different concentrations of use are 0.1% and 0.2%, respectively. In Examples 2 and 4, the mole fractions of octadecyltrimethylammonium chloride, which are cationic surfactants of a single alkyl group, were all 0.88, but caffeine was added to cation / anionic surfactant mixed vesicles having different concentrations of use, respectively, at 0.1% and 0.2%, respectively. It is contained. Examples 1 to 4 all showed the same excellent stability, especially the higher the content of the mixed vesicles, the stronger the attraction between the counter ions to form a very low solubility in water and a strong hydrophobic complex to affect the stability Absorbance measurement results of Examples 3 and 4 having a high content in the mole fraction are shown in FIGS. 1 and 2. FIG. 1 shows the absorbance measured immediately after preparation, 30 days and 65 days after Example 3 for a molar fraction of octadecyltrimethylammonium chloride, which is a cationic surfactant of a single alkyl group, of 0.55 and a mixed vesicle content of 0.2%. 2 is immediately after preparation, 4 days after, 7 days after, and 10 days after the preparation for Example 4 in which the mole fraction of octadecyltrimethylammonium chloride, which is a cationic surfactant of a single alkyl group, is 0.88 and the content of mixed vesicles is 0.2%. Absorbance after 30 days and after 65 days was measured.

As shown in the results of FIGS. 1 and 2, there was no significant change in absorbance tendency immediately after preparation and after 65 days. The fact that the absorbance is almost unchanged indicates that the cationic / anionic surfactant mixed vesicle having the initially formed double layered cationic property has remained stable for at least two months.

Test Example 2 Surface Charge Test

To determine the surface charge of cation-containing cationic / anionic surfactant mixed vesicles containing caffeine, 0.1% and 0.2% daily depending on the mole fraction of octadecyltrimethylammonium chloride, a cationic surfactant of a single alkyl group. When the zeta potential was measured, the results are shown in FIG. As shown in the results of FIG. 3, it was found that the surface charge of the cationic / anionic surfactant mixed vesicle exhibited cationicity when the mole fraction of octadecyltrimethylammonium chloride, which is a cationic surfactant of a single alkyl group, was 0.45 or more. In particular, the molar fractions of octadecyltrimethylammonium chloride, which is a cationic surfactant of a single alkyl group, were all 0.55, but Examples 1 and 3, each having different concentrations of use, showed surface charges of about 40-50 mV. The molar fractions of octadecyltrimethylammonium chloride, the cationic surfactants, were 0.88, but Examples 2 and 4 at 0.1% and 0.2%, respectively, showed surface charges of about 65 to 75 mV, indicating a very strong cation. Could know.

Test Example 3 Hair Loss Prevention Effect Test

Thirty subjects with initial hair loss were tested for anti-hair loss for 12 weeks. After using the compositions of Comparative Examples 1 to 3 and Examples 1 to 4 once a day for 12 weeks, after 12 weeks have elapsed after collecting the hair fall hair collected again to count the number and the results are shown in Figure 4 It was.

As can be seen from the results of Figure 4, it was confirmed that the treatment of the composition of Examples 1 to 4 according to the present invention significantly reduced the number of hair loss compared to Comparative Examples 1 to 3.

Test Example 4 Hair Growth Effect Test Through Mouse

7 weeks old mouse (C57BL / 6) was removed, and the back skin was selected to be clean, and 8 mice were selected for each substance group, and each mouse was treated with the composition of Comparative Examples 1-3 and Examples 1-4 daily. 150 μl per group was applied for 21 days.

After 23 days, a photograph of the degree of growth of the mouse hair was taken, and the weight of the newly grown hair was measured, and the results are shown in Table 2 and FIG. 5.

Treatment group Hair weight (mg) Comparative Example 1 59 ± 12 Comparative Example 2 62 ± 10 Comparative Example 3 65 ± 7 Example 1 72 ± 8 Example 2 73 ± 12 Example 3 75 ± 11 Example 4 93 ± 14

In the results of Table 2 and FIG. 5, caffeine alone was used when caffeine was used as an active ingredient in the present invention and octadecyltrimethylammonium chloride / ammonium lauryl sulphate mixed vesicle having a bilayer structure of cationic property was used. Higher hair growth could be observed.

Hereinafter, based on the results of the above test example, various formulation examples are shown and presented. However, these formulation examples are intended to illustrate the present invention, and it will be apparent to those skilled in the art that the scope of the present invention is not limited to these examples.

Formulation Example 1 Hair Tonic Formulation

ingredient Content (% by weight) ethanol 55 Castor Oil 5 Octadecyltrimethylammonium chloride 0.18 Ammonium Lauryl Sulfate 0.02 Caffeine 0.001 Spices and Colors A reasonable amount Purified water balance

Formulation Example 2 Hair Lotion Formulation

ingredient Content (% by weight) Cetostearyl alcohol 2.0 Stearyl Triethyl Ammonium Chloride 2.0 Hydroxyethyl cellulose 0.5 Pyrotonolamine 0.1 Octadecyltrimethylammonium chloride 0.18 Ammonium Lauryl Sulfate 0.02 Caffeine 0.001 Spices and Colors A reasonable amount Purified water balance

<Formulation Example 3> hair nutrient lotion formulation

ingredient Content (% by weight) Beeswax 4.0 Polysorbate 60 1.5 Sorbitan sesquioleate 0.7 Liquid paraffin 5.0 Squalane 5.0 Caprylic / Capric Triglycerides 5.0 glycerin 3.0 Butylene glycol 3.0 Propylene glycol 3.0 Carboxy Vinyl Polymer 0.1 Triethanolamine 0.2 Octadecyltrimethylammonium chloride 0.18 Ammonium Lauryl Sulfate 0.02 Caffeine 0.001 antiseptic A reasonable amount Spices and Colors A reasonable amount Purified water balance

<Formulation Example 4> Shampoo Formulation

ingredient Content (% by weight) Sodium lauryl sulphate 10.0 Polyoxyethylene lauryl ammonium sulfate 5.0 Cocoamidopropylbetaine 5.0 Ethylene Glycol Distearate 1.0 Octadecyltrimethylammonium chloride 0.18 Ammonium Lauryl Sulfate 0.02 Caffeine 0.001 Preservatives, Colors and Flavors Quantity Purified water balance

1 is a graph showing the stability of Example 3 in the composition according to the present invention.

2 is a graph showing the stability of Example 4 in the composition according to the present invention.

3 is a graph showing the surface charge of a composition according to the invention.

Figure 4 is a graph showing the hair loss prevention effect of the composition according to the present invention.

5 is a graph and photograph showing the hair growth effect of the composition according to the present invention.

Claims (6)

A composition for preventing hair loss or hair growth, containing 0.1 to 0.2% by weight based on the total weight of the composition of a cation / anionic surfactant mixed vesicle having caffeine therein, The cationic surfactant is octadecyltrimethylammonium chloride, The anionic surfactant is ammonium lauryl sulphate anti-hair loss prevention or hair growth composition. The composition of claim 1, wherein the caffeine is contained in an amount of 0.001 to 0.01% by weight based on the total weight of the composition. The composition of claim 1, wherein the cationic / anionic surfactant mixed vesicle having a bilayer structure has a mole fraction of 0.45 to 0.90 and a mole fraction of anionic surfactant of 0.55 to 0.10. delete delete The composition of claim 1, wherein the composition is formulated as a hair tonic, a scalp treatment, a hair shampoo, a hair conditioner or a hair cream.

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