KR101429818B1 - Skin Whitening Composition Comprising Arbutin and Pectinase - Google Patents

Abstract

The present invention relates to a skin whitening composition comprising arbutin and pectinase, and more particularly, to a composition for skin whitening which has excellent skin whitening effect by converting arbutin into pectinase and converting it into hydroquinone.

Description

BACKGROUND ART Skin Whitening Composition Comprising Arbutin and Pectinase Containing Arbutin and Pectinase [

The present invention relates to a skin whitening composition comprising arbutin and pectinase, and more particularly, to a composition for skin whitening which has excellent skin whitening effect by converting arbutin into pectinase and converting it into hydroquinone.

In general, when the skin is exposed to ultraviolet rays, the epidermis becomes black because melanin, a melanocyte, is synthesized and released from the melanocyte. Tyrosinase in melanocytes synthesizes dopaquinone from tyrosine, and dopaquinone undergoes spontaneous oxidation to form melanin. Melanin acts to absorb excessive amounts of light in vivo, but it is also intensively deposited in certain areas to produce spots, black spots, and abnormal discoloration of the skin due to pregnancy blockage or skin pathology. In addition, there is a strong desire to whiten the skin in terms of cosmetics, and many commercially available cosmetic compositions contain a whitening agent.

In order to prevent the skin from becoming black, a method of inhibiting melanin production by inhibiting some reactions during the melanin production process is mainly used. As such whitening agents, hydroquinone and its derivatives, arbutin and its derivatives, kojic acid and its Derivatives, ascorbic acid, and the like. In addition, Japanese cedar (Korean Patent Application No. 2000-035398), tabernum or apple (Registration No. 1998-147412) extracts containing these components have been used in whitening cosmetics.

However, the use of ascorbic acid, kojic acid, glutathione, and herbal extracts is problematic in terms of skin irritation and formulation stability, and its use is limited. Moreover, kojic acid and its derivatives are very expensive and difficult to use in mass-market products. Arbutin is defatted by sunlight and heat, thereby inhibiting the inhibitory effect of tyrosinase, and significantly less whitening effect than hydroquinone It is known.

Hydroquinone is the most effective whitening agent known to date and is widely used for prescription of over-the-counter medicines and dermatologists, and there have been a number of clinical reports showing the effectiveness of hyperpigmentation such as spots (Arndt et al., JAMA, 194 : 965-967, 1965). Hydroquinone acts as an inhibitor of tyrosinase, an enzyme that regulates the conversion of tyrosine into dopaquinone, which is an intermediate step in skin pigmentation in vivo.

However, hydroquinone has a disadvantage in that it is very unstable in the formulation such that the reactivity is so strong that it is easily discolored on an aqueous solution or an emulsifier and its efficacy is lost. (Choudat et al., J. Ind. Med. 45 (6): 376-80, 1988), even at low concentrations, resulting in chronic or acute irritation of the skin or contact skin allergy. In order to avoid side effects of these hydroquinone formulations, dermatological hospitals have prescribed hydroquinone concentrations by adjusting the patient's skin sensitivity (Pearl E. et al., Archi. Dermatol. 131: 1453-1457, 1995).

Arbutine is a hydroquinone glycoside having a structure in which beta-D-glucose is bound to hydroquinone. Arbutin is currently used in some whitening cosmetics, but not only does it absorb skin well, but also has a whitening effect that is significantly lower than that of hydroquinone. In experiments inhibiting the activity of tyrosinase, which is mainly involved in the production of melanin, It is known that it exhibits only a small efficacy (Kazuhisa Maeda and Minoru Fukuda, Arbutin: Mechanism of its depigmenting action in human melanocyte culture. J. Pharm. Exp. Therap.1996; 276 (2): 765-769). In order to promote skin absorption of arbutin, there has been known a method using a surfactant to which nitrogen atom is added (U.S. Patent No. 5,759,528). In addition, many studies have been conducted to develop new derivatives having high whitening effect, There is no report. Thus, arbutin is more stable than hydroquinone and less irritating to the skin, but has not been widely used as a whitening agent due to its low skin absorption and low whitening effect.

As described above, hydroquinone is known to be the most effective whitening agent in terms of activity. However, due to the toxicity and stability of the skin, various side effects have been exposed. In addition, hydroquinone has a high whitening effect like hydroquinone, It has been urgently required to produce a whitening agent.

Accordingly, the present inventors have conducted studies to develop a whitening agent having high whitening effect and low skin irritation and stable formulation by taking only the formulation stability of arbutin and the efficacy merit of hydroquinone, and as a result, arbutin and pectinase The present inventors discovered that whitening agents as active ingredients are not only less irritating to the skin and are stable and exhibit a high whitening effect by producing hydroquinone due to the action of pectinase when applied to skin, Thereby completing the present invention.

It is an object of the present invention to provide a new skin whitening composition which has a high whitening effect and a small skin irritation and is formulated stable.

In order to accomplish the above object, the present invention provides a composition for skin whitening comprising arbutin and pectinase.

In the present invention, the arbutin may be natural arbutin or synthetic arbutin, and the natural arbutin may be added in the form of an extract of a bilberry leaf.

In the present invention, the pectinase may be Cytolase PCL5, and the pectinase may be derived from Aspergillus niger .

In order to achieve the above object, the present invention also provides a skin lightening agent comprising a first composition comprising arbutin and a dermatologically acceptable carrier, and a second composition comprising a pectinase and a dermatologically acceptable carrier do.

In the present invention, the pectinase may be contained in an amount of 5 to 95% by weight based on the second composition. The first composition and the second composition may comprise 2: 1 to 1: 2 by volume. It is preferable that the conversion of arbutin to hydroquinone is 40% or more by mixing the first composition and the second composition.

The skin whitening composition of the present invention contains a pectinase which produces hydroquinone by mixing with arbutin and arbutin, thereby exhibiting a whitening effect similar to that of hydroquinone alone but having little skin irritation, stable formulation and no side effects, Can be used as a whitening agent.

Figure 1 shows albutine and hydroquinone peaks by HPLC analysis.
2 shows the conversion of arbutin to hydroquinone according to the use of the composition for skin whitening according to an embodiment of the present invention.
FIG. 3 shows the conversion of arbutin to hydroquinone according to the use of the skin whitening composition according to another embodiment of the present invention.

The present invention provides a composition for skin whitening comprising arbutin and pectinase.

The arbutin may be natural arbutin, synthetic arbutin or arbutin produced by a biotechnological method, and more preferably natural arbutin is obtained from an extract of a plant known to have a high arbutin content, such as a bilberry leaf, May be included in the composition of the present invention as the extract itself. The pectinase is an enzyme that hydrolyzes α-1,4-galacturonic acid linkages such as pectic acid, pectin, and pectic acid, and is widely distributed in bacteria, fungi, yeast, plants, insects and the like. In the present invention, Cytolase PCL5 derived from Aspergillus niger can be used as a pectinase. Cytolase PCL5 is an acidic pectinase and is mainly used as a cleavage enzyme in the processing of various fruit juices. Of course, the pectinase that can convert arbutin to hydroquinone can be used in the skin whitening composition of the present invention for the purpose of the present invention, regardless of its origin, as long as it has the usual knowledge in the art It will be obvious to the person.

In the composition for skin whitening of the present invention, arbutin and pectinase are provided as separate formulations, respectively, and the two components may be mixed immediately before application to the skin. When arbutin and pectinase are used simultaneously, arbutin is converted to hydroquinone by the effect of pectinase. The whitening effect is exhibited by the hydroquinone produced by the reaction, and it is possible to obtain superior effects in terms of stability and skin irritation as compared with the conventional product comprising hydroquinone.

The skin whitening agent of the present invention may comprise a first composition comprising arbutin and a dermatologically acceptable carrier, and a second composition comprising a pectinase and a dermatologically acceptable carrier. The content of arbutin is preferably 2 to 25% by weight with respect to the first composition. The content of the pectinase is preferably 5 to 95% by weight with respect to the second composition. When the content of arbutin or pectinase is too low, the whitening effect intended in the present invention is not sufficiently exerted, and skin irritation may occur in too many cases.

The skin whitening agent of the present invention preferably contains the first composition and the second composition in a volume ratio of 2: 1 to 1: 2, more preferably 1: 1 to 1: 2. If the second composition is contained in an amount less than the above range, the conversion of arbutin to hydroquinone may be inferior and the whitening effect may not be exhibited. If the second composition is contained in an amount exceeding the above range, side effects due to skin irritation still occur. In the skin whitening agent of the present invention, the conversion of arbutin to hydroquinone is preferably 40% or more. When the conversion of hydroquinone is less than 40%, the whitening effect can not be exhibited properly.

The dermatologically acceptable carrier may be volatile or non-volatile. Suitable carriers are those which dissolve or uniformly disperse the active ingredient of the whitening agent of the present invention. Specifically, the carrier is selected from the group consisting of water, lower alcohols such as ethanol and isopropanol, bivalent alcohols such as propylene and butylene glycol, polyols such as glycerin and hydroalcohol mixtures, hydrocarbons such as isobutane, (Such as acetone, isododecane, and straight or branched chain hydrocarbons having from about 8 to about 20 carbon atoms), halogenated hydrocarbons (e.g., Freon), linalool, hydrocarbon esters (e.g., ethyl acetate, dibutyl phthalate) , Phenethylpentamethyldisiloxane, methoxypropylheptamethylcyclotetrasiloxane, chloropropylpentamethyldisiloxane, hydroxypropylpentamethyldisiloxane, octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane), volatile dimethicone, and But are not limited to, mixtures thereof.

The composition for skin whitening of the present invention may be added to, but not limited to, soft skin lotion (skin), nutritional lotion (milk lotion), nutritional cream, massage cream, essence, pack. Other suitable whitening agents, moisturizing agents, antioxidants, ultraviolet absorbers, surfactants, thickeners, alcohols, preservatives, gelling agents, fragrances, fillers and dyes used in ordinary cosmetics and the like may be blended as required. The amount of the adjuvant is suitably used in the cosmetics field, for example, about 0.01 to 20% of the total weight of the composition. Specific examples of the thickening agent include hyaluronic acid, xanthan gum, hydroxyethyl cellulose (HEC), ULTRES 21 and the like.

The skin whitening composition of the present invention may be in any form of dermatological form commonly used for topical application, for example in the form of a dispersion, emulsion, microcapsule, microparticle or vesicle dispersion in the form of a solution, gel, lotion or emulsion Lt; / RTI > In particular, when arbutin and pectinase are contained in the same formulation, one of arbutin or pectinase is prepared in the form of a microcapsule, a microparticle or a lipid vesicle dispersion according to a technique commonly used in cosmetics, The stability can be maximized.

In a preferred embodiment of the present invention, high performance liquid chromatography (HPLC) was used to confirm that arbutin was converted to hydroquinone by pectinase.

In addition, healthy adults and girls are irradiated with UV light to deposit a pigment on the skin, and a first composition containing arbutin and a whitening agent prepared by separately preparing a second composition containing pectinase are simultaneously used to form arbutin and pept As a result of examination of the whitening effect by tinase, the skin whitening composition of the present invention showed superior whitening effect than that of arbutin alone, and showed no adverse effects due to skin irritation when hydroquinone was treated.

Hereinafter, the present invention will be described in more detail with reference to examples. However, the following embodiments are only examples of the present invention, and the present invention is not intended to be limited thereto.

Example 1: Preparation of a whitening agent according to the present invention

A first composition comprising arbutin and a second composition comprising pectinase were prepared as shown in Table 1 below. And a composition containing hydroquinone as a comparative example was prepared. In Table 1, the contents are based on% by weight.

Ingredients The first composition The second composition Comparative Example 1 Purified water 77.250 49.250 84.250 Hyaluronic acid 0.500 0.500 0.500 Citric acid 0.200 0.200 0.200 Cytolase PCL5 - 40,000 - KATHON-CG 0.050 0.050 0.050 glycerin 10,000 10,000 10,000 Arbutin 12,000 - - Hydroquinone   - - 5.000 Sum   100.00   100.00 100.00

The first composition and the second composition were mixed at a volume ratio of 1: 1 to prepare a skin lightening agent. (Example 1) A skin whitening agent was prepared by mixing the first composition and the second composition at a volume ratio of 2: 1. (Example 2)

Experimental Example 1: Conversion of arbutin to hydroquinone

Figure 1 shows albutine and hydroquinone peaks by HPLC analysis. Specifically, FIG. 1A shows an arbutin peak (RT: about 5.45 min), and FIG. 1B shows a hydroquinone peak (RT: about 6.68 min).

The first composition and the second composition of Preparation Example 1 were mixed at a volume ratio of 1: 1, and hydroquinone conversion from arbutin was calculated by HPLC analysis. FIG. 2A shows the result of mixing the first composition and the second composition for 5 minutes and FIG. 2B shows the results after mixing the first composition and the second composition for 15 minutes. It can be seen from FIG. 2A that about 40% of arbutin is converted to hydroquinone, and from FIG. 2b, about 80% of arbutin is converted to hydroquinone. When the first composition and the second composition were mixed at a volume ratio of 1: 1, the hydroquinone conversion rate was initially about 40%, but it was assumed that the application to the skin would be more than considering skin temperature and frictional heat do.

The first composition and the second composition of Preparation Example 1 were mixed at a volume ratio of 2: 1, and hydroquinone conversion from arbutin was calculated by HPLC analysis. FIG. 3A shows the result of mixing the first composition and the second composition for 5 minutes, and FIG. 3B shows the results after mixing the first composition and the second composition for 15 minutes. 3A shows that about 20% of arbutin is converted to hydroquinone, and from FIG. 3B about 50% of arbutin is converted to hydroquinone. When the first composition and the second composition were mixed at a volume ratio of 2: 1, the hydroquinone conversion rate was initially about 20%, but it was supposed to be more than the skin temperature and frictional heat when applied to the skin do.

Experimental Example 2: Skin whitening effect

Ten healthy men and women were divided into two round holes with a diameter of 1.5 cm and a patch of 4 holes was attached to each of the lower limbs. Ultrasonic waves (Phillies TL20W / 12UV lamps and TM02 / 09UV lamps) And the skin pigment was deposited. After the test materials shown in Table 2 were applied twice a day for 6 weeks, the skin deposition improvement effect was visually observed and the results were recorded.

Test substance Skin pigmentation improvement effect Effective effect Slight effect No change Skin side effects Comparative Example 1
(Hydroquinone) 5 2 - 3 The first composition (arbutin) - 3 7 - Example 1 5 3 One - Example 2 3 2 2 -

As shown in Table 2, when albutin alone was included, it showed almost no effective whitening effect. However, when hydroquinone alone was included, it was effective, but it was not suitable for use due to high rate of deterioration due to skin adverse effects . In contrast, when albutin and pectinase were mixed together, they exhibited a high whitening effect and had no skin side effects at all.

Claims (7)

A first composition comprising arbutin and a dermatologically acceptable carrier, and a second composition comprising a pectinase and a dermatologically acceptable carrier,
Wherein the pectinase is 5 to 95% by weight based on the second composition and the arbutin is 2 to 25% by weight based on the first composition,
The volume ratio of the first and second compositions is 1: 1 to 2: 1,
Wherein the arbutin has a hydroquinone conversion rate of 20% or more by mixing the first composition with the second composition for 5 minutes or more. delete delete delete delete delete delete

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