KR100521768B1 - Cosmetic Compositions for a Skin Whitening - Google Patents

Abstract

The present invention relates to a cosmetic composition for skin whitening,

More specifically, the present invention relates to a whitening composition, which is used in combination with a resveratrol or a water-soluble mixed whitening composition, which not only provides an excellent whitening effect in a small amount, but also during the manufacturing process or storage of a product. It relates to a cosmetic composition for skin whitening that has an effect of not irritating the skin and overcoming problems such as change over time.

Description

Cosmetic composition for skin whitening {Cosmetic Compositions for a Skin Whitening}

The present invention relates to a cosmetic composition for skin whitening. More specifically, the present invention relates to a cosmetic composition for skin whitening containing resveratrol or further containing a water-soluble mixed whitening composition.

Skin is a very important tissue that has direct contact with the external environment, protects the human body and has biochemical and physical functions. This tissue is largely divided into three parts: epidermis, dermis and subcutaneous tissue. Human skin color depends mainly on the number, size, type and distribution of melanocytes containing melanin contained in skin cells. Melanosomes are produced by melanocytes, which are black pigments produced in the epidermis and are produced in cells called melanocytes.

Melanin absorbs the light energy of ultraviolet light in sunlight, protecting cells deeper from damage caused by ultraviolet light. However, abnormally low production of melanin causes skin lesions such as vitiligo, and on the contrary, excessive synthesis of melanin by ultraviolet light not only damages the skin, but also forms spots and freckles, and may cause skin cancer from these lesions. do.

Resveratrol is widely distributed in the herbaceous and dicotyledonous plants and is also present in the free state of plants, but mostly in the form of glycosides associated with sugars (Gorham, J., Prog. Phytochem., 6: 203-). 209, 1980). In addition, resveratrol has a cis type and a trans type, and most of them exist in nature as stable trans isomers (Trela, BC & Waterhouse, A, L., J. Agric. Food Chem., 44 (5): 1253-1257, 1996).

That is, grapes and in particular grape husks, seeds, stems and grape leaves, in particular Vitis vinifera, Vitis rotundifolia and Vitis larusca grapes, and notably these grapes Found in wines and extracts and powders of the above-mentioned natural products, and also a number of Polygonum species (Polygonaceae), for example Polygonum cuspidatum and Polygonum It is present in the roots of multiflorum.

In the present invention, 'resveratrol' refers to trans-3,4,5-trihydroxycistilbene (i.e. suitable resveratrol) and cis isomers, each glycoside, and containing resveratrol obtained from any suitable plant species. Extracts and powders.

Trans-resveratrol is not only anticancer (Jang M., et al., Sci., 275: 218-220, 1997) but also antithrombotic (Chung, ML et al., Planta Med., 58: 274-276, 1992; Frankel , E Net al., Lancet, 341: 1103-1104, 1993; Bertrilli, AA E et al., Int. J. Tissue React., 17: 1-3, 1995; Pae-Asciak, CR et al., Clin. Chim. Acta., 235: 207-219, 1995), anti-inflammatory (Kimura, Y. et al., Biochim. Biophys. Acta., 834: 275-278, 1985) and hyperlipidemia (Arichi, H., et al. , chem. Pharm. Bull., 30 (5): 1766-1770, 1982).

In particular, recently, trans-resveratrol has been spotlighted as a phytoestrogen with a similar effect on female hormone estrogen (Gehm, B.D. et al., Proc. Nasl. Acad. Sci., 94: 14138-14143, 1997). In addition, Japanese Patent Registration No. 06336421, U.S. Patent No. 56,3683, 5439672, and 5151777 disclose a cosmetic composition containing grape extract, and PCT / EP98 / 04223 discloses a cosmetic composition containing grape extract. Cosmetics using resveratrol are disclosed, which relates to cosmetic compositions which inhibit keratinocyte proliferation, inhibit the differentiation of keratinocytes, or regulate skin irritation caused by alpha-hydroxy acids.

However, the above mentioned inventions do not teach that it helps to skin whitening. Therefore, the present inventors have developed a cosmetic composition containing resveratrol having an excellent skin whitening effect.

Accordingly, the present invention is provided to more efficiently solve the problems of the prior art as described above,

It is an object of the present invention to provide a cosmetic composition for skin whitening comprising a water-soluble mixed whitening composition in combination with resveratrol or a combination thereof, which not only provides an excellent whitening effect in a small amount, but also during the manufacturing process or storage of the product. It is to provide a cosmetic composition for skin whitening that has an effect of not irritating the skin and overcoming problems such as change over time.

The above and other objects can be achieved by the present invention described below.

In order to achieve the above object, the present invention provides a cosmetic composition for skin whitening containing resveratrol.

The resveratrol may be 0.00001 to 2.0 wt%.

The cosmetic composition for skin whitening is a water-soluble mixed whitening composition, a component selected from the group consisting of citrus ounce oil peel extract, aminoethylphosphonic acid, Walderian indica leaf extract, guavaphenone, hydrolyzed yeast aqueous solution and mixtures thereof Can contain more.

The citrus ounce oil peel extract; Aminoethylphosphonic acid; Walderian indica leaf extract or guavaphenone; The mixing ratio of the hydrolyzed yeast solution may be 5: 1: 0.3: 2.

The water-soluble mixed whitening composition may be 0.1 to 50% by weight.

Hereinafter, the present invention will be described in detail.

The present invention is characterized in that it comprises 0.1 to 50% by weight of a water-soluble mixed whitening composition (whitegenic, patent application No. 10-2002-0009503) in parallel with an amount of 0.00001 to 2.0% by weight.

The whitening composition according to the present invention not only provides an excellent whitening effect than the conventionally used arbutin or kojic acid, but also shows an excellent whitening effect even in a small amount, and may be in the manufacturing process or storage of the product when used alone. Overcome problems such as changes over time and there is no irritation effect on the skin.

In the present invention, despite the excellent effects of antioxidants, such as resveratrol, which was difficult to apply as a cosmetic to compensate for.

The water-soluble mixed whitening composition (whitegenic) contains citrus ounce oil peel extract (whitegenic 1), aminoethylphosphonic acid (whitegenic 2), and Walderian indica leaf extract (whitegenic 3) having a compounding ratio of 5: 1: 0.3: 2. ) Or one or more selected from guavaphenone, and a water-soluble mixed composition of a hydrolyzed yeast aqueous solution (whitegenic 4).

The cosmetic composition prepared according to the present invention in combination with resveratrol and the water-soluble mixed whitening composition (whitegenic) provides excellent whitening effect while improving skin safety and product phase stability than when applying resveratrol alone. Mela similar to the actual bio-level than the extracts of ascorbic acid (JP 4-9320), hydroquinone (JP-A 6-192062), kojic acid (JP-A 56-7710), arbutin (JP-A 4-9315), and some extracts. In the melanogenesis experiment of NOMA B16, the effect was superior to the existing whitening agent.

Therefore, by using resveratrol, which was previously difficult to use, in the product, a whitening composition was developed without side effects such as stimulation.

Experiments for confirming the whitening physiological activity of the resveratrol or the water-soluble mixed whitening composition (whitegenic) were carried out as follows. First, the whitening effect was confirmed by measuring the activity inhibitory activity and tyrosinase scavenging ability of tyrosinase enzyme which plays the most important role in melanin formation process, and the actual whitening effect was measured by measuring the inhibitory effect by melanoma cell culture similar to the biological level. It was.

In addition, resveratrol alone when used in combination with a more water-soluble mixed whitening composition (whitegenic) to confirm the safety of the skin through the skin irritation test was carried out in the patch test on the skin of adult adults and the phase stability in the product 40 ℃, 4 It was confirmed by measuring the color change and precipitation over time in ℃ and daylight.

As a result of this experiment, the resveratrol or the skin whitening composition containing a water-soluble mixed whitening composition (whitegenic) in combination with the present invention has an excellent whitening effect as compared to the arbutin, kojic acid, etc. which have been previously used commercially. It can improve the phase stability and skin safety in the product and can be effectively used as a whitening cosmetic.

Hereinafter, the present invention will be described in detail by the following examples and comparative examples. However, the following examples are merely to illustrate the present invention, the content of the present invention is not limited to the following examples.

Experimental Example 1 Tyrosinase Inhibitory Effect Test

Inhibition of tyrosinase enzymes involved in the main stage of melanin synthesis was measured to evaluate the whitening ability and the results are shown in Table 1 below.

In the main stage of melanin synthesis, tyrosine used as a substrate and mushroom tyrosinase or tyrosinase fractions isolated from melanocytes were added and reacted for a certain time to measure the absorbance at the absorption wavelength of dopachrome, the reaction product. Evaluated.

Tyrosinase Inhibition Activity (%) = 100-((ODexp.-ODcon.) / ODstd. X 100)

ODexp .: Sample test value, measured value with tyrosinase

ODcon .: sample test value, measured value without tyrosinase,

ODstd .: measured value with tyrosinase, in the absence of a sample

Tyrosinase Inhibitory Activity Sample name IC50 (ug / ml) Resveratrol 2 Kojic acid 5 Soluble Licorice Extract > 50 Morus Pea Powder > 50 Vitamin C > 100 Arbutin > 100 Water-soluble mixed whitening material (whitegenic) > 100 Lettuce extract > 1000 Grape seed extract > 1000 # IC50: A concentration that inhibits tyrosinase activity by about 50% (the smaller the IC50 value, the greater the inhibitory effect of tyrosinase) White Zen 1 (Sederma, France): White Zen 2 (Exymol, Monaco): White Zen 3 (Sero, France) or Guavaphenone: 10% aqueous solution: White Zen 4 (Sapporo, Japan) = 5: 1: 0.3: 2

As can be seen from Table 1, it was confirmed that resveratrol and kojic acid are excellent components in tyrosinase inhibitory activity.

Experimental Example 2 Free radical scavenging force test test

In order to determine the antioxidant effect was carried out a free radical scavenging test as follows, the results are shown in Table 2 below.

The dissipation of relatively stable blue-green DPPH (1,1-diphenyl-2-hydrzyl) radicals produced by dissolving in methanol changed to a clear solution and the absorbance was measured at a wavelength of 516 nm.

Free radical scavenging power (%) = 100-((ODexp.-ODcon.) / ODstd. X 100

ODexp .: Sample test value, measured value with DPPH

ODcon .: sample test value, measured value without DPPH,

ODstd .: measured value with DPPH if no sample

Free radical scavenging force test result Sample name IC50 (ug / ml) Vitamin C 3 Resveratrol 10 Arbutin > 50 Morus Pea Powder > 100 Kojic acid > 200 Soluble Licorice Extract > 250 Grape seed extract > 250 Water Soluble Blending Whitening Agent (Whitegenic) > 250 Lettuce extract > 1000 # IC50: The concentration at which free radicals are eliminated by about 50% (the smaller the IC50 value, the greater the free radical scavenging power) White Zen 1 (Sederma, France): White Zen 2 (Exymol, Monaco): White Zen 3 (Sero, France) or Guavaphenone: 10% Water Soln's: White Zen 4 (Sapporo, Japan) = 5; 1; 0.3 ;2

As can be seen in Table 2, it was confirmed that vitamin C and resveratrol are excellent components in free radical scavenging ability.

Experimental Example 3 Whitening Effect Test Using Skin Melanin Cell Culture

Resveratrol was tested for the inhibition of melanin production using normal human melanin forming cells and the results are shown in Table 3 below.

The whitening effect test using the skin melanin cell culture was performed by the following method.

1. Human dermal melanocytes were cultured and maintained in MGM (Melanocyte Growth Media, Clonetics) medium at 37 ℃, 5% CO2 incubator.

2. For experiments, a certain number of cells (2 × 10 6 cells) were cultured in a 75T culture flask to confirm cell adhesion, and then cultured for 2 to 3 days by adding a constant concentration of test substance to the cell culture solution.

3. After the culture was removed, the cells were washed with phosphate buffer (PBS) and trypsin solution was added to harvest the cells.

4. The pellet was obtained by centrifugation, and then the color was observed. The color was dissolved in 1N NaOH and absorbance was measured at 475 nm.

5. Calculate the amount of melanin using the absorbance obtained from the melanin standard and correct the value with the total protein amount of melanocytes and express it as the amount of melanin per protein.

Melanoma production inhibition rate (%) = [(A-B) / A] X 100

A: melanin amount / protein amount of the control group

(Control: Melano cells grown normally in culture medium without processing raw materials)

B: amount of melanin / protein amount processed for each sample

Melanin inhibition test results of individual whitening substances (sample concentration: 0.02%) Sample name  Melanin inhibition rate (%) Resveratrol 53.17 Water Soluble Blending Whitening Agent (Whitegenic) 35.00 Kojic acid 22.62 Vitamin C 19.72 Soluble Licorice Extract 13.20 Morus Pea Powder 5.1 Arbutin 2.00 Lettuce extract 1.80 Grape seed extract 1.52 White Zen 1 (Sederma, France): White Zen 2 (Exymol, Monaco): White Zen 3 (Sero, France) or Guavaphenone: 10% aqueous solution: White Zen 4 (Sapporo, Japan) = 5; 2

As can be seen from Table 3, resveratrol and water-soluble mixed whitening agent (whitegenic) was confirmed to be an excellent component in the melanin inhibition rate.

On the basis of the results obtained in the above experiments to prepare a cosmetic composition that can safely maintain and increase the whitening effect of resveratrol whether it is possible to maintain the skin whitening effect while making skin safety more smooth, superior product stability Whitening efficacy experiment using the same skin melanocyte culture was tested.

[Examples 1 to 3 and Comparative Examples 1 to 3] Preparation of the lotion

To the composition ratio shown in Table 4 1 to 4 After the aqueous part and the alcohol parts of 5 to 9 were each dissolved at room temperature with an azimuth mixer, the alcohol parts were solubilized while gradually added to the aqueous part. After solubilization, the additive parts of 10 to 12 were slowly added, mixed for about 10 to 20 minutes, and then the preparation of the lotion was completed.

division Raw material name Example (% by weight) Comparative Example (wt%) One 2 3 One 2 3 Water Part 1. Purified water To 100 To 100 To 100 To 100 To 100 To 100 2. Water soluble mixed whitening composition 5.0 20.0 50.0 - - 20.0 3. Arbutin - - - - 2.0 2.0 4. pH adjuster 0.10 0.10 0.10 0.10 0.10 0.10 Alcohol Part 5. Ethanol 6.0 10.0 12.0 10.0 10.0 10.0 6. Hydroxy caster oil POE (60) 0.5 0.8 1.5 0.8 0.8 0.8 7. Incense 0.08 0.08 0.08 0.08 0.08 0.08 8. Preservative 0.10 0.10 0.10 0.10 0.10 0.10 9. Dimethicone Oil 0.2 0.3 0.2 0.3 0.2 0.2 Addition Part 10. Ethanol 2.0 5.0 20.0 5.0 - - 11.1,3-BG 1.0 5.0 10.0 5.0 - - 12. Resveratrol 0.02 0.50 2.0 0.50 - -

[Examples 4 to 5 and Comparative Examples 4 to 5] Preparation of Emulsion

By the composition ratio shown in Table 5 below 1 to 5 After the water phase parts and the oil phase parts of 6 to 10 were completely dissolved by heating to 75 to 80 ° C., the oil phase parts were gradually added to the water phase parts and emulsified at 75 to 80 ° C. at 3000 rpm for 5 minutes.

Neutralization agent of claim 11 was added during the emulsification to neutralize. After the completion of the first emulsification, the mixture was added to the flavors and additives 1 and 2 of claim 12 to 16 at 50 to 55 ° C., and then emulsified for 2 minutes at 3000 rpm at a homomixer, and then cooled and finished at 27 to 30 ° C. An emulsion was prepared.

division Raw material name Example Comparative example 4 5 4 5 Awards part 1. The number of tablets To 100 To 100 To 100 To 100 2. Arbutin - - - 2.0 3. Preservative 0.20 0.20 0.20 0.20 4. Carbomer 0.40 0.40 0.40 0.40 5. Xanthan Gum 0.10 0.10 0.10 0.10 Paid Part 6. Cetostearyl Alcohol 1.2 2.0 2.0 2.0 7. Self-emulsifying glycerin monostearate 1.0 2.0 2.0 2.0 8. Hydroxy caster oil POE (60) 1.0 1.5 1.5 1.5 9. Cetyl Octanoate 5.0 5.0 5.0 5.0 10. Cyclomethicone 3.0 3.0 3.0 3.0 corrector 11.Triethanolamine 0.4 0.4 0.4 0.4 Additives1 12. Incense 0.12 0.12 0.12 0.12 13. Water soluble mixed whitening composition 2.0 10.0 - - Additive2 14. Ethanol 1.0 5.0 5.0 5.0 15. 1,3 BG 1.0 5.0 5.0 5.0 16. Resveratrol 0.001 1.0 1.0 -

The following tests were carried out to determine the efficacy and effect of the compositions of the Examples and Comparative Examples.

Experimental Example 4 Skin Irritation Experiment

In order to confirm skin irritation of the water-soluble mixed whitening composition according to the present invention, a patch test using a skin of a normal person was performed.

Skin irritation test results (Closed Patch Test (24 Hours, 20 people)) sample Stimulus index Stimulus Example 1 1.3 Minimal stimulation Example 2 1.0 Minimal stimulation Example 3 1.8 Minimal stimulation Example 4 0.5 Minimal stimulation Example 5 1.2 Minimal stimulation Comparative Example 1 3.5 Moderate irritation Comparative Example 2 3.0 Moderate irritation Comparative Example 3 2.1 Mild stimulation Comparative Example 4 2.7 Mild stimulation Comparative Example 5 3.2 Moderate irritation

(Stimulus index = Σ (Evaluation standard value * Number of evaluation value) X 100)

                Total Subject * Maximum Criteria Value

Stimulation plate 1.9 or less: minimum stimulation, 2.0 to 2.9: mild stimulation,

3.0 to 3.9: moderate stimulation, 4.0 or higher: severe stimulation

As can be seen from the results of Table 6, when the resveratrol according to the present invention is used in parallel with the water-soluble mixed whitening composition (whitegenic) as an adjuvant, it can be seen that the intradermal irritation is alleviated.

Experimental Example 5 Phase Stability Experiment

In order to experiment the phase stability of the resveratrol or the water-soluble mixed whitening composition (whitegenic) according to the present invention, changes in room temperature, 40 ° C., 4 ° C. and daylight were observed in Table 7 below.

Phase stability experiment division 1 day later 1 week later after 2 weeks 3 weeks later Example 2 Room temperature ◎ ◎ ◎ ◎ 40 ℃ ◎ ◎ ◎ ○ 4 ℃ ◎ ◎ ◎ ◎ daylight ◎ ◎ ○ ○ Example 5 Room temperature ◎ ◎ ◎ ◎ 40 ℃ ◎ ◎ ○ ○ 4 ℃ ◎ ◎ ◎ ◎ daylight ◎ ◎ ○ ○ Comparative Example 1 Room temperature ◎ ○ ▲ ▲ 40 ℃ ◎ ○ ▲ ★ 4 ℃ ○ ○ ▲ ★ daylight ○ ▲ ★ ★ Comparative Example 2 Room temperature ◎ ○ ○ ▲ 40 ℃ ◎ ○ ▲ ★ 4 ℃ ◎ ◎ ◎ ◎ daylight ◎ ○ ▲ ★ Comparative Example 4 Room temperature ◎ ○ ○ ▲ 40 ℃ ◎ ○ ▲ ★ 4 ℃ ◎ ○ ▲ ★ daylight ○ ▲ ★ ★ Comparative Example 5 Room temperature ◎ ○ ○ ▲ 40 ℃ ◎ ○ ▲ ★ 4 ℃ ◎ ◎ ◎ ◎ daylight ◎ ○ ▲ ★

(◎: No change, ○: Light discoloration, ▲: Many color change, Separation sign or suspension ★: Complete color change, Separation or precipitation)

As shown in Table 7, in the case of the comparative example, discoloration or precipitation occurs rapidly in each condition, whereas in the case of the example containing the water-soluble mixed whitening composition (whitegenic), the product phase stability was maintained.

Table 8 shows the results of testing the rate of melanin production using normal human melanin forming cells to test the whitening effect.

Experimental Example 6 Whitening Effect Test Using Skin Melanin Cell Culture

To test the whitening efficacy, the inhibition rate of melanin production using normal human melanin forming cells was tested for Example 2 and Comparative Examples 1 to 3 and the results are shown in Table 8 below.

Melanin inhibition rate according to the mixing ratio of water-soluble whitening substance Sample name Melanin inhibition rate (%), sample concentration 0.5% Example 2 75.05 Comparative Example 1 45.26 Comparative Example 2 11.20 Comparative Example 3 26.58

Experimental Example 7 Clinical Result of Whitening Effect on Human Body

Experimental Methods: Fifteen healthy women over the age of 18 were applied twice a day to the facial face, and the effect of black and white on the skin was measured using a colorimeter (Minolta CR2002). L *, a *, b * colorimeters are used to indicate color. In this experiment, L * value (brightness) was used as an index. The L * values range from black (L * = 0) to white (L * = 100) and ΔL * was obtained from the difference of L * 28 one month after L * 0 when the sample was applied, and is shown in Table 9 below.

division △ L * Example 5 15.53 Comparative Example 5 3.35

As shown in Table 9, the case of Example 5 according to the present invention was found to have a relatively much better whitening effect than Comparative Example 5.

The cosmetic composition for skin whitening of the present invention not only provides an excellent whitening effect even in a small amount, but also overcomes problems such as changes over time, which may occur during the manufacturing process or storage of the product, which may occur when the product is applied by resveratrol alone. It has no skin irritation effect.

While the invention has been described in detail above with reference to the described embodiments, it will be apparent to those skilled in the art that various modifications and variations are possible within the scope and spirit of the invention, and such modifications and variations fall within the scope of the appended claims. It is also natural.

Claims (6)

delete delete In the cosmetic composition for skin whitening, Resveratrol; And A water-soluble mixed whitening composition selected from the group consisting of citrus-unus oil peel extract, aminoethylphosphonic acid, Walderian indica leaf extract, guavaphenone, hydrolyzed yeast aqueous solution, and mixtures thereof; Cosmetic composition for skin whitening, characterized in that comprises a. The method of claim 3, The resveratrol cosmetic composition for skin whitening, characterized in that 0.00001 to 2.0% by weight. The method of claim 3, The citrus ounce oil peel extract; Aminoethylphosphonic acid; Walderian indica leaf extract or guavaphenone; A cosmetic composition for skin whitening, wherein the mixing ratio of the hydrolyzed yeast aqueous solution is 5: 1: 0.3: 2. The method of claim 3, Cosmetic composition for skin whitening, characterized in that the water-soluble mixed whitening composition is 0.1 to 50% by weight.