KR20030037106A - Nanoemulsion containing nicotinamide and Cosmetic comprising the same - Google Patents

Abstract

PURPOSE: Nanoemulsion containing nicotine amide, useful for improving dry skin and inhibiting skin aging is provided. The nanoemulsion has excellent percutaneous absorption, stability, moisture retaining effect on the skin. CONSTITUTION: The nanoemulsion contains 1.0 to 10.0% by weight of nicotine amide comprising lecithin, ceramide, cholesterol, fatty acid and oil in a ratio of 1.0 to 5.0:1.0 to 2.0:2.0 to 4.0:1.0 to 2.0:10.0 to 20.0, based on the total weight of the nanoemulsion. The lecithin has a phosphatidylcholine content of 30%. The ceramide is selected from the group consisting of cerebroside, ceramide I, ceramide II, ceramide III, ceramide IV, ceramide V, ceramide VI derivatives and a mixture thereof. The cosmetic contains 0.1 to 20% by weight of the nanoemulsion, based on the total weight of the composition.

Description

Nanoemulsion containing nicotinamide and Cosmetic comprising the same

The present invention relates to nicotinamide-containing nanoemulsions useful for improving dry skin and inhibiting skin aging and to cosmetics comprising the same. More specifically, nano-containing nicotinamide in nanoemulsions composed of lecithin, ceramide, cholesterol, fatty acids and oils. It relates to an emulsion and a cosmetic comprising the same.

In general, the moisture content of the normal stratum corneum is about 10 to 30%. The proper moisture contained in the stratum corneum will not only smooth and soften the skin's surface, but also allow the body to function properly. When the moisture content of the stratum corneum is less than 10%, the skin becomes rough and the body loses its protective function, causing aging. For example, in the dry skin, the scaling of keratinocytes is weakened and scales are peeled off from the surface of the skin, resulting in scaling. In this way, the skin is dried. This is because the barrier function is not properly performed. In addition, even in healthy skin, the lack of moisture caused by changes in the external environment may cause a poor skin condition.

Therefore, it is very important to properly maintain the moisture content of the stratum corneum. To this end, conventionally, sebum-like components, NMF components, or moisturizers such as polyols have been used in cosmetics, but only temporary effects have been obtained.

Recent studies have shown that ceramide, the main component of intercellular lipids in the stratum corneum, maintains the water retention ability of the stratum corneum, strengthens the barrier function of the skin, and plays an important role in maintaining the cohesion and adhesion of keratinocytes. . Therefore, attempts have been made to maintain the water retention ability of the stratum corneum and enhance the barrier function by adding the ceramide component to the cosmetic. For example, US Pat. Nos. 5294444, 5368857 and Japanese Patent Laid-Open No. 81-123210 disclose cosmetics in which ceramide is incorporated into a formulation. However, ceramide is not compatible with other raw materials, so it is difficult to formulate the ceramide to a concentration sufficient to exhibit efficacy in the product when the ceramide is simply formulated in the cosmetics as described above. Therefore, since the amount of use is limited, there is a disadvantage in that the water retention ability and barrier function improvement effect of the stratum corneum is insignificant.

On the other hand, nicotinamide is a substance useful for preventing pellagra, a skin disease, and is a kind of vitamin B called vitamin P (Pellagra Preventive). Nicotinamide is a component of two important hydrogen transfer coenzymes, Nicotinamide Adenine Dinucleotide (NAD) and Nicotinamide Adenine Dinucleotide Phosphate (NADP), which are known to be involved in the physiology of various enzymes. In addition, nicotinamide has been reported to have a wound healing effect, a soothing effect, a water retention effect, and a ceramide synthesis promoting effect (Palmarcol. Biochem. Behav.) 1996-4; 53 (7); 783-90, Ann N. Y. Acad. Scio., 1996-6; 15; 786; 135-51. In addition, PCT Patent Application No. 9625943A, EP396422A and Japanese Patent Application Laid-Open No. 92-2777540 describe that nicotinamide exhibits hair and nail growth, whitening and moisturizing effects. However, in the above-mentioned documents, nicotinamide was simply formulated into a formulation and applied to cosmetics, and thus it is difficult to achieve the desired effect. This is due to the low transdermal absorption of nicotinami et al.

In order to solve this problem, attempts have been made to improve the transdermal absorption of nicotinamide using amphoteric surfactants, but the percutaneous absorption has been improved to some extent, but skin irritation occurs (G Ridout, RS Hinz, JJ Hostynek). , AK Reddy and RH Guy, Fund.Appl.Toxicol., 1991 16:41).

Therefore, the technical problem to be achieved by the present invention is to solve the above problems, there is no skin irritation, excellent transdermal absorption and impart excellent moisture retention ability to the skin, it is excellent in the improvement effect of dry skin and inhibiting skin aging However, the present invention provides a nicotineamide-containing nanoemulsion having good stability over time.

Another technical problem of the present invention is to provide a cosmetic containing the nicotinamide-containing nanoemulsion.

In order to achieve the above technical problem, the present invention provides nicotine to a nanoemulsion in which lecithin, ceramide, cholesterol, fatty acids and oils are each formulated in a weight ratio of 1.0 to 5.0: 1.0 to 2.0: 2.0 to 4.0: 1.0 to 2.0: 10.0 to 20.0. Provided is a nicotinamide-containing nanoemulsion comprising an amide. The nicotinamide-containing nanoemulsion formed at such a compounding ratio not only enhances the skin's water retention ability, promotes the synthesis of ceramides, but also enhances the compatibility between ceramides and other components to improve transdermal absorption.

The content of nicotinamide contained in the nanoemulsion is preferably 1.0 to 10.0% by weight based on the total weight of the nanoemulsion.

As the lecithin constituting the nanoemulsion according to the present invention, it is preferable to use a phosphaticholine content of 30% by weight or more, and ceramides include ceramides of copper and plant origin, and ceramides of yeast origin, namely, ceramide I , Ceramide II, ceramide III, ceramide IV, ceramide V, derivatives of ceramide VI, and the like.

In order to achieve the above another technical problem, the present invention provides a cosmetic, characterized in that containing 0.1 to 20% by weight of the nicotinamide-containing nanoemulsion based on the total weight of the cosmetic.

Hereinafter, the nicotinamide-containing nanoemulsion of the present invention and the cosmetic comprising the same will be described in detail.

The nicotinamide-containing nanoemulsion of the present invention is a nicotine in a nanoemulsion in which lecithin, ceramide, cholesterol, fatty acids and oils are blended in a weight ratio of 1.0 to 5.0: 1.0 to 2.0: 2.0 to 4.0: 1.0 to 2.0: 10.0 to 20.0, respectively. It is formed by containing amide. By the blending ratio, it is possible to prepare a nanoemulsion having no skin irritation and excellent stability over time, and the nanoemulsion improves the moisture retention and transdermal absorption of the skin and shows an excellent dry skin improvement effect and skin aging inhibitory effect.

Lecithin used in the preparation of the nanoemulsion of the present invention is a kind of copper and plant cell membrane components, it is preferable to use a phosphaticholine content of 30% or more represented by the following formula (1).

In addition, ceramides may be used alone or in combination of ceramides of cerebromide and yeast origin, namely, ceramide I, ceramide II, ceramide III, ceramide IV, ceramide V, ceramide VI, and the like. It can be mixed and used. As cholesterol, cholesterol, cholesteryl nonanoate, cholesteryl cinnamate, cholesteryl benzoate, cholesteryl adipate, cholesteryl linate, cholesteryl stearate, cholesteryl isostearate Cholesterol such as cholesterol derivatives such as cholesteryl propionate, cholesteryl oleyl carbonate, cholesteryl isostearyl carbonate, and the like.

In addition, examples of the fatty acid constituting the nanoemulsion according to the present invention include palmitic acid, stearic acid, arabic acid, and the like. As the oil, one or more of oils such as octyldodecanol, squalane, octyltodecyl myristate, octyl palmitate, caprylic capric triglyceride, cyclomethicone and dimethicone can be used.

In the nicotinamide-containing nanoemulsion according to the present invention, the content of nicotinamide is preferably 1.0 to 10.0% by weight based on the total weight of the nanoemulsion in consideration of the stability according to the activity and solubility of nicotinamide.

The nanoemulsion according to the present invention may be prepared by heating, dissolving and mixing lecithin, ceramide, cholesterol, fatty acids and oil in the above-mentioned ratios, and then adding nicotinamide to high-pressure emulsifying.

The nicotinamide-containing nanoemulsion prepared as described above may be applied to cosmetics made of various formulations such as lotions, creams, essences, etc., preferably added in the range of 0.1 to 20.0 wt% based on the total weight of the cosmetics. If the content of the nicotinamide-containing nanoemulsion is less than 0.1% by weight may be a slight effect, if it exceeds 20.0% by weight it may be difficult to prepare a formulation such as lotions, creams, essences.

Hereinafter, the present invention will be described in detail with reference to experimental examples and examples. However, embodiments according to the present invention can be modified in many different forms, the scope of the present invention should not be construed as limited to the embodiments described below. Embodiments of the present invention are provided to more completely explain the present invention to those skilled in the art.

Examples 1 to 3

The raw materials of 1-6 were mixed and stirred at 70-75 degreeC, and melted according to the composition of the following Table 1. After adding ethanol to it, a 50 degreeC distilled water solution in which nicotinamide was dissolved was added while maintaining the temperature at 50 to 55 ° C. Nicotinamide-containing nanoemulsions were prepared by passing three times at 1000 bar in a high pressure emulsifier while maintaining the temperature of the entire solution at a temperature of 50 to 55 ° C.

Raw material name (wt%) Example 1 Example 2 Example 3 1. Lecithin 2.0 2.0 2.0 2. Ceramide 1.5 1.5 1.5 3. Cholesterol 1.5 3.0 5.0 4. Fatty acid 1.5 1.5 1.5 5. Propylene Glycol 5.0 5.0 5.0 6. Caprylic Capric Triglycerides 15.0 20.0 25.0 7. Ethanol 10.0 10.0 10.0 8. Distilled Water Remaining amount Remaining amount Remaining amount 9. Nicotinamide 0.1 1.0 10.0

In Table 1, lecithin was used S 75-3 product of Lipoid, Germany, ceramide was used ceramide LS 3773 of Serobiologiques, France, and the product of Roche, Switzerland.

Examples 4-6

To prepare an oil-in-water cosmetic emulsion containing a nicotinamide-containing nanoemulsion according to the composition of Table 2.

First, the water phase and the oil phase were heated and dissolved at 75-80 degreeC, respectively, and the oil phase was added to the water phase. The mixture thus obtained was emulsified with a homomixer at a rate of 4,000 to 6,000 rpm with stirring for 4 to 6 minutes, and then nicotinamide-containing nanoemulsion was added at 45 to 50 ° C. to obtain an oil-in-water cosmetic emulsion.

division Raw material name (wt%) Example 4 Example 5 Example 6 Awards Purified water Remaining amount Remaining amount Remaining amount Triethanolamine 0.15 0.15 0.15 Carboxy vinyl polymer (1 wt% aqueous solution) 10.0 10.0 10.0 Dark glycerin 2.0 2.0 2.0 Propylene glycol 3.0 3.0 3.0 Paraoxybenzoic Acid Ester 0.2 0.2 0.2 Paid Cetostearyl alcohol 0.8 0.8 0.8 Glyceryl Monostearate 1.5 1.5 1.5 Sorbitol Monostearate 0.3 0.3 0.3 POE (20) sorbitan monostearate 1.5 1.5 1.5 Paraoxybenzoic acid propyl 0.1 0.1 0.1 Isocetil Myristate 7.0 7.0 7.0 Isocetyl octinoate 5.0 5.0 5.0 additive Nanoemulsion of Example 3 1.0 10.0 20.0

Comparative Examples 1 to 3

An oil-in-water cosmetic emulsion was prepared in the same manner as in Examples 4 to 6, except that nicotinamide was simply added according to the conventional method instead of the nicotinamide-containing nanoemulsion according to the composition of Table 3 below.

division Raw material name (wt%) Comparative Example 1 Comparative Example 2 Comparative Example 3 Awards Purified water Remaining amount Remaining amount Remaining amount Triethanolamine 0.15 0.15 0.15 Carboxy vinyl polymer (1 wt% aqueous solution) 10.0 10.0 10.0 Dark glycerin 2.0 2.0 2.0 Propylene glycol 3.0 3.0 3.0 Paraoxybenzoic Acid Ester 0.2 0.2 0.2 Paid Cetostearyl alcohol 0.8 0.8 0.8 Glyceryl Monostearate 1.5 1.5 1.5 Sorbitol Monostearate 0.3 0.3 0.3 POE (20) sorbitan monostearate 1.5 1.5 1.5 Paraoxybenzoic acid propyl 0.1 0.1 0.1 Isocetil Myristate 7.0 7.0 7.0 Isocetyl octinoate 5.0 5.0 5.0 additive Nicotinamide 0.1 1.0 2.0

In Tables 2 and 3, the carboxyvinyl polymers are prepared in US B. Chem. F. Carbopol 941 (BF Goodrich) in a 1% by weight aqueous solution, sorbitol monostearate is Arlacel 60, a product of ICI (USA), Pio (20) sorbitan monostea The late used Tween 60 of Isaiah, USA, and the isocetyloctanoate of ICEH from Nihon Kokyo Alcohol of Japan.

The oil-in-water cosmetic emulsion prepared by the above-described method was measured as follows for the effect of percutaneous absorption, skin irritation, moisture retention and dry skin.

Percutaneous absorption measurement test

In order to evaluate the transdermal absorption promoting effect of nicotinamide contained in the samples prepared according to Examples 4 to 6 and Comparative Examples 1 to 3, three skin permeation tests were performed using the skin of hairless mice. 48 μl of each sample was injected into the skin surface of 7.5 mm in diameter, and the amount of nicotinamide permeated after 24 hours using a transdermal absorption device (Microette, Hanson Co.) was analyzed by high performance liquid chromatography. Quantification The results are shown in Table 4 as transmittance (%).

sample Example 4 Example 5 Example 6 Comparative Example 1 Comparative Example 2 Comparative Example 3 Transmittance (%) 12.9 14.9 17.6 3.81 3.86 3.90

As shown in Table 4, the cosmetics of Examples 4 to 6 containing nicotinamide-containing nanoemulsions were significantly promoted percutaneous absorption compared to the cosmetic compositions of Comparative Examples 1 to 3 containing nicotinamide simply, and further contained nicotinamide. As the nanoemulsion content increases (Example 4 → 6), it can be seen that the transdermal absorption of nicotinamide also increases proportionally.

Skin primary irritation test

25 healthy adults men and women were placed on the back of each of the samples prepared according to Examples 4 to 6 and Comparative Examples 1 to 3 (approximately 0.2 g), followed by 4 hours of removal of the pin chamber. Then, the skin condition change was visually read and the results are shown in Table 5. The criteria for evaluation are as follows.

-: No erythema or unusual phenomenon

+-: Slightly reddish

+: Significantly redder than the surroundings

++: Severe reddening and swelling around

In addition, the skin irritation index was determined according to the following formula.

Stimulus = [(+-) number * 1 + (+) number * 2 + (++) number * 3] / [(+-) number * 1 + (+) number * 2 + (++) number * 3 + (-) numbers]

sample Judgment result (the number of people) Stimulus ++ + +- - Example 4 0 0 One 24 0.04 Example 5 0 0 2 23 0.08 Example 6 0 0 One 24 0.04 Comparative Example 1 0 0 One 24 0.04 Comparative Example 2 0 0 2 23 0.08 Comparative Example 3 0 0 2 23 0.08

As shown in Table 5, the cosmetics of Examples 4 to 6 showed a stable irritation degree without significant difference compared to the cosmetics of the conventional Comparative Examples 1 to 3.

Moisture retention test

In order to determine the water retention capacity of the samples prepared according to Examples 4 to 6 and Comparative Examples 1 to 3, the following tests were performed twice a day for 24 months on 24 adult men and women with dry hand regions.

First, before using the samples of Examples 4 to 6 and Comparative Examples 1 to 3, the skin moisture content measuring device (Skin Surface Hygrometer) ), Model name: SKICON-200, manufactured by IBM Corporation, Japan. Then, the skin moisture content after using the samples for 3 months on the back of the hand was measured and the results are shown in Table 6 (unit of the value used here is μs).

Example 4 Example 5 Example 6 Comparative Example 1 Comparative Example 2 Comparative Example 3 Before use 2.3 2.3 2.4 2.5 2.3 2.5 after use 45 56 62 23 29 41

As shown in Table 6, the cosmetics of Examples 4 to 6 containing nicotinamide-containing nanoemulsions were superior in the moisture retention effect compared to the cosmetics of Comparative Examples 1 to 3 in which nicotinamide was simply blended. In addition, it can be seen that the water retention ability increases significantly in proportion to the content of nicotinamide.

Dry skin improvement effect measurement test

In order to examine the dry skin improvement effects of the samples prepared according to Examples 4 to 6 and Comparative Examples 1 to 3, the following tests were conducted twice a day for 24 months on 24 adult men and women with dry hand regions. Was performed.

First, before using the samples according to Examples 4 to 6 and Comparative Examples 1 to 3, the scale generated on the skin with respect to the area of the 4 cm x 4 cm area of the back of the subject's hand was selected as a dry evaluation parameter and used as a handy scope. After measuring the back of the hand, the scale area was measured using image analysis. Then, the scale area after using the samples on the back of the hand for 3 months was measured and the results are shown in Table 7. The figures used are% of scale area.

Example 4 Example 5 Example 6 Comparative Example 1 Comparative Example 2 Comparative Example 3 Before use 15.3 15.0 14.8 15.1 14.8 14.7 after use 4.6 3.1 1.4 6.2 5.0 4.3

As shown in Table 7, the cosmetics of Examples 4 to 6 containing nicotinamide-containing nanoemulsions were significantly reduced in scale compared to the cosmetics of Comparative Examples 1 to 3 containing nicotinamide simply. Therefore, it can be seen that the cosmetic composition containing the nicotinamide-containing nanoemulsion according to the present invention is more excellent in terms of improving dry skin.

As described above, the cosmetic containing the nicotinamide-containing nanoemulsion according to the present invention is not only skin irritation and excellent transdermal absorption, and can impart excellent moisture retention ability to the skin, thereby improving dry skin and skin Excellent anti-aging effect, good stability over time according to temperature changes.

Claims (5)

Nicotinamide, characterized in that nicotinamide is contained in a nanoemulsion comprising lecithin, ceramide, cholesterol, fatty acids and oils in a weight ratio of 1.0 to 5.0: 1.0 to 2.0: 2.0 to 4.0: 1.0 to 2.0: 10.0 to 20.0, respectively. Containing nanoemulsions. The nicotinamide-containing nanoemulsion of claim 1, wherein the nicotinamide content is 1.0 to 10.0 wt% based on the total weight of the nanoemulsion. The nicotinamide-containing nanoemulsion of claim 1, wherein the lecithin has a phosphaticholine content of 30% by weight or more. The nicotinamide of claim 1, wherein the ceramide is any one selected from the group consisting of cerebromide, ceramide I, ceramide II, ceramide III, ceramide IV, ceramide V, derivatives of ceramide VI, and mixtures thereof. Containing nanoemulsions. A cosmetic comprising the nicotinamide-containing nanoemulsion of claim 1 in an amount of 0.1 to 20% by weight based on the total weight of the cosmetic.