KR20080001820A - A composition for skin external application containing antioxidant components for improving skin wrinkle and skin whitening - Google Patents

Abstract

A skin external composition comprising antioxidant components is provided to remove free radicals and increase activity of protection factors associated with antioxidation in the skin, so that it is useful for improving skin wrinkles and whitening the skin. A skin external composition for improving skin wrinkles and whitening the skin comprises 0.001-20 wt.% of at least two antioxidant components selected from lipoic acid, tocopherol, coenzyme Q10, selenium and vitamin C, and is formulated as soft lotion, nutrition lotion, massage cream, nutrition cream, pack, gel, lotion, ointment, cream, patch or spray.

Description

A composition for skin external application containing antioxidant components for improving skin wrinkle and skin whitening}

1 is a graph showing the whitening efficacy of Examples 1-3 and Comparative Examples 1-6.

The present invention relates to an external skin composition containing two or more antioxidant components selected from the group consisting of lipoic acid, tocopherol, coenzyme Q10, selenium, and vitamin C. . More specifically, the composition for external application for skin according to the present invention is at least two antioxidants selected from the group consisting of lipoic acid, tocopherol, tocopherol, coenzyme Q10, selenium, and vitamin C. It contains ingredients to eliminate free radicals or increase the activity of the skin's defense factors related to antioxidants, thereby improving skin wrinkles and skin whitening.

The relationship between aging and oxidation is well known through many studies, and wrinkles and localized blackening caused by skin aging are also known to be closely related to this oxidation. Some people look much younger than their age, while others look much older than they actually are. Aging phenomena, such as skin wrinkles and localized blackening, are caused by endogenous factors such as age increase, the shape of the skeleton and muscles, genetic factors caused by constant relaxation and contraction of muscles, and environmental pollutants and stress. It can be classified as an environmental factor. Wrinkles increase due to the reduction of keratinocytes and fibroblasts, decreased collagen synthesis, increased MMP production, and increased signal transduction of melanin due to the above-mentioned skin aging phenomenon. Blemishes, freckles and blotch are to be increased.

In particular, recent studies have shown that free radicals are eliminated by healthy antioxidant defense agents such as superoxide dismutase and catalase in healthy skin. If not, oxidative action by free radicals (free radicals) may occur, resulting in deterioration of the function of skin cells and tissues. This causes skin wrinkles and localized blackening. This active oxidative reactive oxygen is promoted by external factors (pollution, stress) and internal factors (in vivo energy metabolism), and combines with fat to make harmful substances called lipid peroxides. The lipid peroxide acts on blood vessels and causes various adult diseases including atherosclerosis or thrombosis. In addition, the decrease in the ability to produce collagen, which is closely related to healthy skin, and the abnormal entanglement of these collagen fibers increases, which significantly reduces skin elasticity, and the glycosaminoglycans, a type of hyaluronic acid and glycoproteins, which are responsible for skin moisturizing. It is reported that the production amount is remarkably lowered.

Various methods have been applied to improve the skin aging phenomenon. As a typical method, AHA, retinoic acid, retinol, vitamins, etc. are mainly applied, but these have been much debated about skin irritation and clinical efficacy, limiting the amount of use and the main cause of skin aging There is no fundamental response to the oxidation caused by oxygen. In addition, there are many examples in which the plant extract containing an antioxidant component is used alone, but it is difficult to obtain a satisfactory effect.

Meanwhile, studies on lipoic acid, tocopherol, coenzyme Q10, selenium, and vitamin C are mainly performed in the food field. However, to date, there are few studies on the synergistic effect of the antioxidant power when appropriate combination of the above ingredients, and there is an example of using the extract alone for external application of the skin, but the skin wrinkle through maximizing the antioxidant efficacy by combining these ingredients properly There is no example applied to enhance the whitening effect.

Accordingly, the present inventors studied various antioxidant components to improve skin wrinkles and localized blackening due to oxidation of free radicals such as free radicals, and antioxidant components that restore the activity of antioxidant defense factors in vivo. The study found that two or more selected from the group consisting of lipoic acid, tocopherol, coenzyme Q10, selenium, and vitamin C can be very effective in enhancing skin wrinkles and whitening.

Furthermore, as a result of extensive research by the present inventors, when the antioxidant composition is contained in 0.001 to 20% by weight relative to the total weight of the composition, the skin external composition is found to have excellent skin wrinkle improvement and whitening effect. To complete.

Accordingly, an object of the present invention contains two or more antioxidant components selected from the group consisting of lipoic acid, tocopherol, coenzyme Q10, selenium, and vitamin C to eliminate free radicals or increase the activity of antioxidant defense factors to improve skin wrinkles and It is to provide an external skin composition for excellent skin whitening effect.

In order to achieve the above object, the external composition for skin according to the present invention contains two or more antioxidant components selected from the group consisting of lipoic acid, tocopherol, coenzyme Q10, selenium, and vitamin C to improve skin wrinkles and skin whitening effect Characterized in that represents. In particular, the topical skin composition according to the present invention is characterized by containing the antioxidant component in an amount of 0.001 to 20% by weight based on the total weight of the composition.

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

Lipoic acid used in the present invention is an essential metabolite, and acts as a coenzyme (CoA) that is closely related to thiamine in the complete oxidative decarboxylation system of pyruvic acid or α-ketoglutaric acid. In recent years, it is a material that has a large application area as a physiologically active substance such that its efficacy is proven in diet and diabetes treatment, and cosmetics has excellent effects such as skin wrinkle improvement and whitening. The lipoic acid is contained in an amount of 0.001 to 20% by weight, preferably 0.001 to 5.0% by weight based on the total weight of the composition.

Tocopherol used in the present invention is one of the fat-soluble vitamins in foods, four types of tocopherols (α-, β-, γ-, δ-) and four types of tocotrienols (α-, β-, γ-, δ- ), But the most common and bioactive is α-tocopherol, commonly referred to as vitamin E. The most important function of tocopherol in human body is antioxidant. It prevents cell membrane damage and further tissue damage by inhibiting oxidation of substances that are easily oxidized in cell, especially unsaturated fatty acids that make up cell membrane. In the topical skin composition of the present invention, the tocopherol is contained in an amount of 0.001 to 20% by weight, preferably 0.001 to 5.0% by weight based on the total weight of the composition.

Coenzyme Q10 used in the present invention participates in biochemical reactions that energize nutrients introduced into cells together with other enzymes in the body. The substance is particularly distributed in cells with high energy demands such as cardiomyocytes and muscle cells. It also acts as a powerful antioxidant, preventing cell damage from unstable harmful oxygen. Coenzyme Q10 in the topical skin composition of the present invention is contained in an amount of 0.001 to 20% by weight, preferably 0.001 to 5.0% by weight based on the total weight.

Selenium (Selenium) used in the present invention is a trace element (inorganic substance) essential to our body. The nutrient is an important component of the antioxidant enzyme that protects cells from free radicals generated during normal oxygen metabolism, and can be said to be an essential component for the normal function of the immune system. In the topical skin composition of the present invention, the selenium is contained in an amount of 0.001 to 20% by weight, preferably 0.001 to 5.0% by weight based on the total weight of the composition.

Vitamin C used in the present invention is necessary for tissue growth and repair because it is a basic substance for collagen formation, and is also essential for treating fractures. In addition, it strengthens the gums, improves adrenal function, improves absorption of iron, and has antioxidant activity, which returns oxidized substances in the human body to reduced form. In the external preparation composition for skin of the present invention, the vitamin C is contained in an amount of 0.001 to 20% by weight, preferably 0.001 to 5.0% by weight based on the total weight of the composition.

When the antioxidant components used in the present invention are used in less than 0.001% by weight, respectively, it is difficult to show the effect, and when used in excess of 20.0% by weight may indicate problems such as skin side effects, instability of the formulation.

The external preparation composition for skin of the present invention is not particularly limited in its formulation, and may be, for example, a cosmetic composition having a formulation of a flexible cosmetic water, a nourishing cosmetics, a massage cream, a nourishing cream, a pack, a gel, or a skin adhesive cosmetic. And transdermal dosage forms such as lotions, ointments, gels, creams, patches or sprays.

Hereinafter, although an Example and a comparative example are given and this invention is demonstrated in detail, this invention is not limited only to these examples.

[Test Example 1] Free radical scavenging action of lipoic acid, tocopherol, coenzyme Q10, selenium, vitamin C and mixtures thereof

In order to confirm the free radical scavenging action of the antioxidant components used in the present invention, the measurement method is a 1,1-Diphenyl-2-pycryl-Hydrazyl (DPPH) method, and the reagents used are all US Sigma (St. Louis). , MO, USA) was used. These reagents are relatively stable free radicals and are an in vitro method used primarily to confirm free radical scavenging action.

The concentration of the material used for the DPPH measurement was 5.0 vol%, 1.0 vol%, 0.1 vol%, and 0.01 vol%, first into a 96 well plate, and the total volume of DPPH prepared with 5 mM ethanol solution was added to 200 μl. After leaving for 30 minutes at 37 ℃ absorbance was observed by 520nm ELISA reader. Free radical scavenging action (%) was calculated by the following equation 1, the results are shown in Table 1 below.

Free radical scavenging effect (%) = 100-B / A X 100

A: absorbance of control wells without sample

B: absorbance of the experimental group wells treated with the sample

ingredient 5.0% by volume 1.0 volume% 0.1 volume% 0.01 volume% Lipoic Acid (A) 78.4 45.8 18.4 10.8 Tocopherol (B) 85.6 54.2 32.8 22.1 Coenzyme Q10 (C) 83.7 48.7 27.0 16.7 Selenium (D) 80.5 49.3 28.6 15.3 Vitamin C (E) 75.2 50.2 20.0 15.3 A + B, 1: 1 92.8 80.4 45.1 25.1 A + C, 1: 1 91.5 75.3 40.5 20.6 A + D, 1: 1 92.3 85.9 50.6 28.3 A + E, 1: 1 92.9 88.7 54.3 30.4 B + C, 1: 1 93.5 89.7 52.6 29.4 B + D, 1: 1 95.5 85.4 55.3 31.1 B + E, 1: 1 93.9 87.2 55.4 32.6 C + D, 1: 1 94.2 88.5 56.6 32.5 C + E, 1: 1 93.1 88.4 54.7 33.5 D + E, 1: 1 92.1 89.7 52.6 29.4 A + B + D, 1: 1: 1 95.5 85.4 55.3 31.1 A + B + D, 1: 1: 1 98.2 87.2 55.4 32.6 A + B + C + D, 1: 1: 1: 1 98.1 88.5 56.6 32.5 A + B + C + E, 1: 1: 1: 1 98.9 88.7 56.8 33.5 A + B + C + D + E, 1: 1: 1: 1: 1 97.9 89.7 53.8 35.5

As shown in the results of Table 1, lipoic acid, tocopherol, coenzyme Q10, selenium, and vitamin C each had a free radical scavenging effect, and this free radical scavenging effect has a concentration dependent effect, in particular, these components are mixed. When used, it could be confirmed that it shows a high synergistic effect.

Test Example 2 Measurement of Tropoelastin and Fibrillin Production in Human Skin Fibroblasts

It was determined by the following method whether the antioxidant component used in the present invention increases the production of tropoelastin and fibrilin, which plays an important role in elasticity in human skin.

Fibroblasts isolated from human skin were placed in ⁴ wells of each 24 well cell culture plate and attached for 24 hours. Subsequently, the test cells were treated to the concentrations of the following Table 2, and then 2 days later, the medium was harvested. Enzyme immunoassay (ELISA) was used to quantify tropoelastin and fibrin in the harvested medium. The results were reported as a control group as a relative ratio to 100, and the results are shown in Table 2 below.

Test substance Concentration (ppm) Tropoelastin Production (%) Fibrillin production (%) Lipoic Acid (A) 100 127 124 10 116 116 Tocopherol (B) 100 138 135 10 121 123 Coenzyme Q10 (C) 100 132 130 10 122 117 Selenium (D) 100 127 121 10 114 112 Vitamin C (E) 100 123 125 10 110 111 A + B, 1: 1 100 155 158 10 140 134 A + B + C, 1: 1: 1 100 165 158 10 143 136 A + B + C + D, 1: 1: 1: 1 100 170 153 10 142 137 Control - 100 100

As can be seen in Table 2, it was found that a lot of tropoelastin and fibrin are synthesized depending on the concentration of each test substance. In particular, when using the test materials together, it can be seen that the synergistic effect is greater than when using the raw materials alone.

[Examples 1-3 and Comparative Examples 1-6]

The external preparations for skin compositions of Examples 1 to 3 and Comparative Examples 1 to 6 were prepared in a cream formulation according to the composition of Table 3 below.

Compounding ingredients (content; wt%) Example 1 Example 2 Example 3 Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Comparative Example 6 Purified water To 100 To 100 To 100 To 100 To 100 To 100 To 100 To 100 To 100 Lipoic Acid (A) - - - - 1.00 - - - - Tocopherol (B) - - - - - 1.00 - - - Coenzyme Q10 (C) - - - - - - 1.00 - - Selenium (D) - - - - - - - 1.00 - Vitamin C (E) - - - - - - - - 1.00 A + B, 1: 1 1.00 A + B + C, 1: 1: 1 1.00 A + B + C + D, 1: 1: 1: 1 1.00 Vegetable Cured Oil 1.50 1.50 1.50 1.50 1.50 1.50 1.50 1.50 1.50 Stearic acid 0.60 0.60 0.60 0.60 0.60 0.60 0.60 0.60 0.60 Glycerol Stearate 1.00 1.00 1.00 1.00 1.00 1.00 1.00 1.00 1.00 Ceteanyl Alcohol 2.00 2.00 2.00 2.00 2.00 2.00 2.00 2.00 2.00 Arakidil Behenyl Alcohol & Arakidil Glucoside 1.00 1.00 1.00 1.00 1.00 1.00 1.00 1.00 1.00 Cetylaryl Alcohol & Cetearyl Glucoside 2.00 2.00 2.00 2.00 2.00 2.00 2.00 2.00 2.00 PEG-100 Stearate & Glycerolate & Propylene Glycol 1.50 1.50 1.50 1.50 1.50 1.50 1.50 1.50 1.50 Caprylic / Capric Triglycerides 11.00 11.00 11.00 11.00 11.00 11.00 11.00 11.00 11.00 Cyclomedicon 6.00 6.00 6.00 6.00 6.00 6.00 6.00 6.00 6.00 Preservative, incense Quantity Quantity Quantity Quantity Quantity Quantity Quantity Quantity Quantity Triethanol amine 0.10 0.10 0.10 0.10 0.10 0.10 0.10 0.10 0.10

Test Example 3 Measurement of Wrinkle Formation Improvement Effect in Humans

Examples 1 to 3 and Comparative Examples 1 to 2 were carried out the following experiment to confirm the wrinkle improvement effect.

Dividing 100 women in their 30s into 5 sets of 20 people each, applying one of Examples 1 to 3 and Comparative Examples 1 to 2 once daily for 8 weeks, and then scooping up a replica using silicone The state of was measured with a aging degree gauge (visiometer; SV600, Courage + Khazaka electronic GmbH, Germany) for image analysis. The results are shown in Table 4 below, and each value represents the average of each parameter value after subtraction of the parameter value before application after 8 weeks of application. In Table 4, R1 is the difference between the highest and lowest values of the wrinkled contours, R2 is an arbitrary division of the wrinkled contours by 5 spaces, and then the average of R1 values, R3 is the highest value of the R1 values divided by 5, and R4 is the baseline of the wrinkled contours ( R5 is the difference between the baseline of the wrinkle contour and the contour of each wrinkle minus the baseline of the wrinkle contour.

division R1 R2 R3 R4 R5 Example 1 -0.18 -0.13 -0.06 -0.05 -0.04 Example 2 -0.19 -0.16 -0.07 -0.06 -0.05 Example 3 -0.25 -0.19 -0.1 -0.09 -0.07 Comparative Example 1 0.06 0.05 0.02 -0.01 0.00 Comparative Example 2 -0.10 -0.07 -0.4 -0.03 -0.03

As can be seen in Table 4, it was confirmed that Examples 1 to 3 exhibited a better skin wrinkle improvement effect than Comparative Examples 1 to 2.

[Test Example 4] melanin production inhibitory effect measurement

HM3KO cells (Y. Funasaka, Department of dermatology, Kobe university school of medicine, 5-1 Kusunoki-cho 7-chrome, Chuo-ku, Kobe 650, Japan), which are human melanoma cells, contain a minimum of 10% fetal bovine serum Incubated in essential essential medium (Minimum Essential Medium; MEM) at 37 ℃, 5% CO ₂ conditions. The cultured cells were spread over 75 flasks so that the number of cells was 3 × 10 ⁵ per flask, waited overnight for the cells to adhere to the wall, and after confirming that the cells adhered well, the medium contained 10 ppm of the test substance of Table 5 below. I changed to a new badge. As a control, a medium containing DMSO was used. In this way, every two to three days, the cells were transferred to a new medium containing samples, and the cells were incubated until the flask was filled. Thereafter, the culture medium was removed, washed with PBS, dissolved with 1N sodium hydroxide, and measured for absorbance at 500 nm. Then, the melanin production inhibition rate was calculated according to the following Equation 2, and the results are shown in Table 5 below.

Melanin inhibition rate (%) = 100-(absorbance of each test substance / absorbance of control X 100)

Test substance Melanin production inhibition rate (%) Lipoic Acid (A) 15.2 Tocopherol (B) 12.3 Coenzyme Q10 (C) 14.7 Selenium (D) 3.45 Vitamin C (E) 14.8 A + B, 1: 1 25.8 A + C, 1: 1 22.8 A + D, 1: 1 23.5 A + E, 1: 1 26.1 B + C, 1: 1 23.5 B + D, 1: 1 26.4 B + E, 1: 1 21.9 C + D, 1: 1 26.5 C + E, 1: 1 25.9 D + E, 1: 1 21.7 A + B + D, 1: 1: 1 30.5 A + B + D, 1: 1: 1 29.3 A + B + C + D, 1: 1: 1: 1 35.1 A + B + C + E, 1: 1: 1: 1 33.5 A + B + C + D + E, 1: 1: 1: 1: 1 36.5

Test Example 5 Whitening Effect Test on Human Skin

Twelve healthy men were placed with opaque tape with six 1.5cm diameter holes in the upper forearm area of the subject, followed by 1.5-2 times the UVB of the Minimal Erythema Dose. The blackening of the skin was induced by irradiating and the test materials were applied and two months later, the contrast of the skin was measured using a color difference meter. Each test substance was applied to the skin external preparations of Examples 1-3 and Comparative Examples 1-6 twice daily in the morning and evening. The determination of the effect was determined by obtaining a "L" value representing the darkness of the skin (unburned Korean skin color generally indicates a value of 50-70). When the test material is effective, the L value is gradually increased, and the comparison between the test materials is calculated according to the following equation (3) of the difference in skin color (ΔL) at the time of application start and completion time, This is shown in Table 6 and FIG.

△ L * = L * value two months after application-L * value at the start of application

Whitening effect test on human skin Test substance Whitening Effect (△ L) Example 1 2.82 Example 2 3.04 Example 3 3.55 Comparative Example 1 1.27 Comparative Example 2 1.67 Comparative Example 3 1.82 Comparative Example 4 1.79 Comparative Example 5 1.20 Comparative Example 6 2.01

As can be seen in Table 6 and FIG. 1 below, it was found that Examples 1 to 3 had excellent whitening effects as compared to Comparative Examples 1 to 6 in human clinical experiments.

As described above, the external preparation composition for skin according to the present invention contains two or more antioxidant components selected from the group consisting of lipoic acid, tocopherol, coenzyme Q10, selenium, and vitamin C to eliminate free radicals or to prevent skin related to antioxidant. By increasing the activity of the defense factor, it provides an excellent skin wrinkle improvement and whitening effect.

Claims (3)

A skin external composition for improving wrinkles of skin, comprising two or more antioxidant components selected from the group consisting of lipoic acid, tocopherol, coenzyme Q10, selenium, and vitamin C. A skin external preparation composition for skin whitening, comprising two or more antioxidant components selected from the group consisting of lipoic acid, tocopherol, coenzyme Q10, selenium, and vitamin C. The composition for external application for skin according to claim 1 or 2, wherein the antioxidant component is contained in an amount of 0.001 to 20% by weight based on the total weight of the composition.

Images