KR100495454B1 - Cosmetic Compositions for Skin-Whitening Comprising Phytolight as Active Ingredient - Google Patents

Abstract

The present invention apple extract (Pyrus Malus Fruit extract), Golden Root Extract (Scutellaria Baicalensis Root extract), Camellia leaf extract (Camellia sinensis Leaf extract), cucumber extract (Cucumis sativus It provides a whitening cosmetic composition derived from an extract selected from the group consisting of Fruit extract) and mixtures thereof and comprising phyrite as an active ingredient that inhibits tyrosinase activity.

Description

Cosmetic composition comprising phytolight {Cosmetic Compositions for Skin-Whitening Comprising Phytolight as Active Ingredient}

The present invention relates to a whitening cosmetic composition, and more particularly to a cosmetic composition comprising phytolite as an active ingredient.

Pigments that determine human skin color include melanin, hemoglobin, carotenoids, and the like, and various colors of skin, hair, and eyes are determined by these pigments. For skin, the most important pigment that determines color is melanin, which is genetically determined by the amount, nature and distribution of melanin, and melanin production is also influenced by environmental factors such as sun ultraviolet rays and physiological factors such as fatigue and stress. get affected.

Melanin is converted from tyrosine to dopa (DOPA) and dopaquinone (Dopaquinone) by the action of an enzyme called tyrosinase, which is present in pigment cells, and is then produced through a non-enzymatic oxidation reaction. As such, the pathway by which melanin is synthesized is known, but the mechanism of inducing melanin synthesis, which is a step prior to the action of tyrosinase, has not been elucidated in detail.

Melanin is widely distributed in the skin and removes oxygen radicals to protect the skin from damage caused by overproduction of melanin, which is closely related to melanoma, causes skin blackening and produces spots, freckles, etc. It is known that the development of cosmetics and pharmaceuticals for the purpose of preventing overproduction of melanin is being actively performed. Factors that promote the production of melanin include the above-mentioned sunlight (ultraviolet rays) as well as hormones such as estrogen, prostaglandin and bleomycin.

The method of inhibiting skin blackening is to greatly reduce skin pigmentation or prevent excessive pigmentation, and to inhibit melanocyte activity, reduce chemical and biological dopa (L-DOPA), eliminate inflammatory reactions and reduce tyrosinase activity. Is being studied in the direction of.

In the past, many chemicals, such as hydroquinone, have been used to whiten skin by destroying organized melanin structures. However, hydroquinone has not only very low anti-tyrosinase activity but also high cytotoxicity to normal melanocytes. For this reason, arbutine and hydroquinone derivatives with low cytotoxicity have been developed and used, but they lack specificity to the mechanism of pigmentation. Therefore, kojic acid, ascorbic acid and its derivatives, which act at the molecular level within the melanin production regulating mechanism, are used as targets for tyrosinase. However, kojic acid is rapidly oxidized by other raw materials of the cosmetics and exhibits an allergic phenomenon, ascorbic acid is oxidized, decomposed in an aqueous solution, such as poor stability, there is a disadvantage that the use is limited.

In order to solve the problems of the above-described conventional whitening substances, that is, as a result of earnest research efforts to develop a whitening material having excellent whitening effect due to excellent safety of the skin and excellent tyrosinase inhibition ability, Whitening cosmetics containing phytolites derived from plant extracts already secured have been developed.

Accordingly, it is an object of the present invention to provide a whitening cosmetic composition with improved stability and whitening effect.

According to an aspect of the present invention, the present invention is an apple extract ( Pyrus Malus Fruit extract), Scutellaria Baicalensis Root extract, Camellia Sinensis Leaf extract, Cucumber extract It provides a whitening cosmetic composition comprising a phytolight (derived from the extract selected from the group consisting of Cucumis Sativus Fruit extract) and mixtures thereof as an active ingredient.

The present inventors screened various natural plant extracts in order to overcome the problems of conventional cosmetics, that is, lowering of stability, occurrence of side effects and weakening of the whitening effect, and as a result, apple extract, among natural plant extracts, It was found that the golden root extract, camellia leaf extract, and cucumber extract showed a whitening effect but little side effects.

As used herein, the term "phytolight" is a term made by combining the prefix "phyto-", which means plants, with "light", which means whitening, and in this specification, apple extract and golden root extract, which show whitening. Means camellia leaf extract, cucumber extract or a mixture of said extract.

The plant extract included in the cosmetic composition of the present invention can be obtained by various extraction methods, and can be obtained by adding an aqueous or organic solvent. Specifically, it is preferable to use a method of obtaining an extract by adding water, anhydrous or hydrous lower alcohol having 1 to 4 carbon atoms, acetone, ethyl acetate, butyl acetate, chloroform, 1,3-butylene glycol, and the like.

According to an embodiment of the present invention, the phytolite may include one of the above extracts, and more preferably includes a combination of two or more of the above extracts.

Apple extract included in the phytolite of the present invention may be prepared from various organs (flowers, fruits, stems, roots, leaves, etc.) of the apple tree, but is preferably extracted from apple fruit. The content of the apple extract is preferably 0.001-10% by weight based on the total phyrite.

The golden extract included in the phytolite of the present invention may be prepared from various organs of gold (flowers, fruits, stems, roots, leaves, etc.), but is preferably extracted from the golden roots. The content of the golden root extract is preferably 0.001-10% by weight based on the total phytolite.

Camellia extract included in the phytolite of the present invention may be prepared from various organs (flowers, fruits, stems, roots, leaves, etc.) of the camellia, but is preferably extracted from the leaves of the camellia. The content of camellia leaves is preferably 0.001-10% by weight based on the total phyrite.

Cucumber extract included in the phytolite of the present invention may be prepared from various organs (flowers, fruits, stems, roots, leaves, etc.) of the cucumber, but is preferably extracted from the fruit of the cucumber. The content of cucumber fruit is preferably 0.001-10% by weight based on the total phyrite.

According to a preferred embodiment of the present invention, the phyrite of the present invention may additionally include EDTA. EDTA functions to inhibit tyrosinase by binding to copper ions, which is a metallic cofactor required to oxidize tyrosine during melanogenesis in phyrite. More preferably EDTA is in the form of a stable salt, such as disodium EDTA.

In the whitening cosmetic composition of the present invention, the amount of phytolite is preferably 0.001-10% by weight based on the total cosmetic composition, and when the amount is less than 0.001% by weight, the whitening effect that can be achieved is too weak and exceeds 10% by weight. There is a problem that the increase in the effect of increasing the content is too small and there is a problem that the cytotoxicity is increased.

The components included in the cosmetic composition of the present invention include components conventionally used in cosmetic compositions in addition to phyrite as active ingredients, and include, for example, conventional auxiliaries such as antioxidants, stabilizers, solubilizers, vitamins, pigments and perfumes, and Carrier.

The whitening composition of the present invention may be prepared in any formulation conventionally prepared in the art, for example, solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, soaps, surfactant-containing It may be formulated as cleansing, oil, powder foundation, emulsion foundation, wax foundation, spray, and the like, but is not limited thereto. More specifically, it may be prepared in the form of a flexible lotion, nutrition lotion, nutrition cream, massage cream, essence, eye cream, cleansing cream, cleansing foam, cleansing water, pack, spray or powder.

When the formulation of the present invention is a paste, cream or gel, animal oils, vegetable oils, waxes, paraffins, starches, trachants, cellulose derivatives, polyethylene glycols, silicones, bentonites, silicas, talc or zinc oxide may be used as carrier components. Can be.

When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used, in particular in the case of a spray, additionally chlorofluorohydrocarbon, propane Propellant such as butane or dimethyl ether.

When the formulation of the present invention is a solution or emulsion, a solvent, solubilizer or emulsifier is used as the carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 Fatty acid esters of, 3-butylglycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan.

When the formulation of the present invention is a suspension, liquid carrier diluents such as water, ethanol or propylene glycol, suspending agents such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, microcrystals Soluble cellulose, aluminum metahydroxy, bentonite, agar or tracant and the like can be used.

When the formulation of the present invention is a surfactant-containing cleansing, the carrier component is an aliphatic alcohol sulfate, an aliphatic alcohol ether sulfate, a sulfosuccinic acid monoester, isethionate, an imidazolinium derivative, a methyltaurate, a sarcosinate, a fatty acid amide. Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, lanolin derivatives or ethoxylated glycerol fatty acid esters and the like can be used.

In the whitening cosmetic composition of the present invention, phytolite shows a whitening effect by inhibiting tyrosinase activity in melanocytes, and does not show cytotoxicity, so there are almost no side effects.

Hereinafter, the present invention will be described in more detail with reference to Examples. These examples are only for illustrating the present invention in more detail, it is to those skilled in the art that the scope of the present invention is not limited by these examples in accordance with the gist of the present invention. Will be self-evident.

Example 1 Preparation of Phytolite Composition

The phytolite component used as an active ingredient in the cosmetic composition of the present invention was prepared as follows.

First, the apple extract is chopped 100 g of apples, added 100 ml of 95% hydrous ethanol to the dry weight, and extracted by heating to 50-100 ° C. for 10 hours while the cooling condenser is installed to prevent the active ingredient from evaporating After filtration, it was concentrated under reduced pressure completely and dried to obtain 5 g of powdered extract.

Camellia leaf extract is chopped 100 g of camellia leaf, and added 100 ml of 95% hydrous ethanol to the dry weight and heated to 50-100 ℃ for 10 hours while the cooling condenser is installed to prevent the active ingredient from evaporating. Extraction and filtration, and then concentrated under reduced pressure completely, dried to obtain 3.1 g of a powdery extract.

The golden root extract is extracted by heating 100 g of golden root and adding 100 ml of 95% hydrous ethanol to the dry weight, and heating at 50-100 ° C. for 10 hours while the cooling condenser is installed to prevent the active ingredient from evaporating. After filtration, it was concentrated under reduced pressure completely and dried to obtain 3.7 g of a powdery extract.

Cucumber extract is chopped 100 g of cucumber and added 100 ml of 95% hydrous ethanol to the dry weight, and the extract is filtered by heating to 50-100 ℃ for 10 hours while the cooling condenser is installed to prevent the active ingredient from evaporating. The mixture was concentrated under reduced pressure completely and dried to obtain 2.8 g of a powdery extract.

Subsequently, 1-5% by weight of disodium EDTA, 2% by weight of sodium sulfite and sodium metabisulfite, respectively, and the remaining amount of purified water were added to 1-5% by weight of the extract to prepare a phyrite composition. It was.

Experimental Example 1: Tyrosinase Inhibition Activity Test

The reaction solution was prepared by adding 500 μl of tyrosine (tyrosine, Sigma Co., Ltd.) at 0.1 mg / ml, phytolite, kojic acid, ascorbic acid, and hydroquinone at various concentrations. Sodium phosphate buffer (pH 6.8) was used as the buffer solution. 500 µl of tyrosinase (250 U / ml, Sigma) was added to the reaction solution, reacted at 37 ° C for 10 minutes, and the absorbance was measured at 475 nm. No inhibitor was added as a control.

Inhibition was calculated according to the following equation (1).

Inhibition (%) = (1 - control group absorbance (OD ₄₇₅₎ / control absorbance (OD ₄₇₅₎₎ × 100

The experimental results are shown in Table 1.

Sample (wt%) Inhibition (%) Control 0 Phytolite (0.01) 0 Phytolite (0.1) 82.7 ± 3.1 Phytolite (1.0) 93.8 ± 2.8 Phytolite (10) 95 ± 2.9 Kojic acid (0.1) 71 ± 1.4 Kojic acid (1.0) 80 ± 0.8 Ascorbic acid (0.1) 66 ± 2.2 Hydroquinone (0.4) 0 Hydroquinone (0.8) 0 Hydroquinone (1.6) 0

As can be seen in Table 1, it can be seen that the phytolite of the present invention greatly inhibits the activity of tyrosinase, and furthermore, it has an increased inhibitory effect compared to cosine and ascorbic acid, which are known as tyrosinase inhibitors. Indicates.

Experimental Example 2: Cytotoxicity Test

Incubate for 45 min by adding 1% of kojic acid, ascorbic acid and phytolite to NHFB cells (Korea Cell Line Bank) incubated in a 96-well plate for 24 hours, removing supernatant and injecting 200 μl of medium again. Time incubation. After incubating for 4 hours by adding 50 µl of 5 mg / ml MTT reagent to the culture, the absorbance was measured at 540 nm by an ELISA reader. Cytotoxicity is expressed in% by the following equation. Cells cultured without any material were used as controls.

Cytotoxicity (%) = (1- Comparative Absorbance (OD ₅₄₀ ) / Control Absorbance (OD ₅₄₀ )) × 100

The experimental results are shown in Table 2.

Sample (wt%) Cell survival rate (%) Control 100 Kojic acid (1%) 44 ± 2.2 Ascorbic acid (1%) 15 ± 1.8 Phytolite (1%) 93.8 ± 1.5

As can be seen in Table 2, it can be seen that the phytolite of the present invention has almost no adverse effect on the survival of the cells, while the conventional whitening cosmetics, kojic acid and ascorbic acid, greatly reduced the survival rate of the cells.

Experimental Example 3: Effect on melanin production in melanocytes

Melanosite was used by purchasing a mouse-derived B-16 melanoma (ATCC CRL 6323) cell line. Melanoma cell lines were inoculated in DMEM medium containing 4.5 g of glucose, 10% serum and 1% antibiotics and incubated at 37 ° C. in a 50 ml T-flask. After incubation for 24 hours under 5% CO ₂ conditions, cells were isolated by treatment with 0.05% trypsin containing 0.02% EDTA, and then incubated in 50 ml T-flask for 48 hours. At this time the cell number was 4.57 × 10 ⁶ cells / flask. Samples of appropriate concentration were diluted in DMEM medium, treated with cultured melanoma cells, and incubated at 37 ° C. for 5 days. After incubation, all of the medium was removed, cells were separated by treatment with 1 ml of phosphate buffered saline (PBS) containing 0.02% EDTA and 0.05% trypsin, followed by centrifugation for 5 minutes to collect only cells. Then, 5% trichloroacetate (TCA) was treated, stirred, and centrifuged to wash the precipitated melanin with PBS. 1N NaOH was dissolved and dissolved in the precipitated melanin, and the absorbance was measured at 475 nm. Melanin concentrations were determined from standard concentration curves of synthetic melanin (Sigma).

The experimental results are shown in Table 3.

Sample (wt%) Melanin production inhibition rate Control 0 Kojic acid (1%) 78 ± 0.8 Ascorbic acid (1%) 65 ± 2.0 Phytolite (1%) 94 ± 3.1

As can be seen in Table 3, it can be seen that the phytolite of the present invention significantly inhibits the production of melanin in melanocytes.

Hereinafter, although an example of the flexible lotion, lotion, cream and pack as an example of the formulation of the present invention, the formulation including the cosmetic composition of the present invention is not limited thereto.

Formulation Example 1 Flexible Lotion (Skin)

ingredient Content (% by weight) Phytolite 2.0 1,3-butylene glycol 5.2 Oleyl alcohol 1.5 ethanol 3.2 Polysorbate 20 3.2 Benzophenone-9 2.0 Carboxyl Vinyl Polymer 1.0 glycerin 3.5 incense a very small amount antiseptic a very small amount Purified water Remaining amount system 100

Formulation Example 2: Emulsion (Lotion)

ingredient Content (% by weight) Phytolite 2.0 glycerin 5.1 Propyl glycol 4.2 Tocopheryl Acetate 3.0 Floating paraffin 4.6 Triethanolamine 1.0 Squalane 3.1 Macadamia Nut Oil 2.5 Polysorbate 60 1.6 Sorbitan sesquirrolate 1.6 Propylparaben 0.6 Carboxyl Vinyl Polymer 1.5 incense a very small amount antiseptic a very small amount Purified water Remaining amount system 100

Formulation Example 3: Cream

ingredient Content (% by weight) Phytolite 2.0 glycerin 4.0 vaseline 3.5 Triethanolamine 0.5 Liquid paraffin 24.0 Squalane 3.0 Beeswax 2.1 Tocopheryl Acetate 0.1 Polysorbate 60 2.4 Carboxyl Vinyl Polymer 1.0 Sorbitan sesquioleate 2.3 incense a very small amount antiseptic a very small amount Purified water Remaining amount system 100

Formulation Example 4: Pack

ingredient Content (% by weight) Phytolite 2.0 Ethyl alcohol 3.0 EDTA-2Na 0.02 Propylene glycol 5.1 glycerin 4.5 Cabopol 1.0 Polyoxide 0.1 antiseptic a very small amount incense a very small amount Purified water Remaining amount system 100

Experimental Example 4: Measurement of the whitening effect

Thirty Korean female volunteers aged 19-40 years old were selected, especially those with dark skin. Minolta CR 300 was used as a measuring instrument and measured at two week intervals over a two month period. The measurement site was marked 5 cm by 1 cm on the arm, and four different prescriptions (Formulations 1 and 2, Comparative Examples 1 and 2) were applied and one was placed as a control value for comparison. The difference from the control is shown in Table 5. The comparative example is the formulation which did not add phyrite in Formulation Examples 1 and 2.

Formulation Example 1 Formulation Example 2 Comparative Example 1 Comparative Example 2 Control ΔL value 1.95 2.15 0.80 0.65 0

As can be seen from Table 5, the ΔL value after 8 weeks is higher in the formulation example of the present invention to which phytolite was added than in the comparative example without phytolite, it can be seen that the phytolite shows a whitening effect.

As described in detail above, the present invention provides a whitening cosmetic composition comprising phytolite as an active ingredient. The whitening cosmetic composition of the present invention is excellent in whitening effect because it has a large effect of inhibiting the activity of tyrosinase in melanocytes, and has little side effects because it does not exhibit cytotoxicity.

Claims (6)

0.001-10 wt% Apple Extract ( Pyrus Malus Fruit extract), 0.001-10 wt% Golden Root Extract ( Scutellaria Baicalensis Root extract), 0.001-10 wt% Camellia Sinensis Leaf extract and 0.001-10 wt% Cucumber extract ( Cocumis Sativus Fruit Extract) A whitening cosmetic composition comprising a phytolite that inhibits tyrosinase activity composed of a mixture of Cucumis Sativus Fruit extract. delete delete delete delete The whitening cosmetic composition according to claim 1, wherein the amount of phytolite is 0.001 to 10% by weight based on the total cosmetic composition.