KR20090075299A - Cosmetic composition using bis-ethylhexyloxyphenol -methoxyphenyltriazine loaded solid lipid capsule - Google Patents

Abstract

An UV protection cosmetic composition containing solid lipid nanoparticle containing an organic UV protector is provided to lower skin irritation by an organic UV protector and have constant capsule. A cosmetic composition of UV protection comprises 0.01-50 weight% of solid lipid capsule. The solid lipid capsule has 100-1000nm of size and contains 0.01-37 weight% of bis-ethylhexyloxyphenolmethoxyphenyltriazine which is an organic UV protector. A method for producing a solid lipid capsule comprises: a step of emulsifying oil phase part containing soli lipid and bis-ethylhexyloxyphenolmethoxyphenyltriazine which is chemical UV protector in water phase part containing emollient; and a step of cooling lipid dispersion material. The cosmetic composition is used in a form of spray type mist, lotion, and cream.

Description

Cosmetic composition using solid lipid capsule containing solid lipid capsule encapsulated with bisethylhexyloxyphenol methoxyphenyl triazine

The present invention relates to a sunscreen cosmetic composition containing a solid lipid capsule encapsulated with bisethylhexyloxyphenol methoxyphenyltriazine, and more particularly, to a vis. A sunscreen cosmetic composition containing a solid lipid capsule prepared by emulsifying an oil phase part composed of 7-hexyloxyphenolmethoxyphenyltriazine (bis-ethylhexyloxyphenolmethoxyphenyltriazine) to form a lipid dispersion composed of lipid / water type and cooling it again. It is about. The present invention can provide a more fine and uniform capsule and less skin irritation and a sunscreen cosmetic composition with improved sunscreen effect.

Ultraviolet rays kill harmful pests in the skin and synthesize vitamin D in the body, which is necessary for calcium metabolism and bone formation. However, when excessive ultraviolet rays are irradiated on the skin, acute skin reactions and chronic skin reactions occur. In the case of ultraviolet rays that are harmful to the human body, UVB is absorbed mostly by the epidermis, causing sunburn and skin cancer, and UVA penetrates deep into the dermal layer of the skin, although it is weak energy, and penetrates deep into the dermis of the skin, depositing melanin of keratinocytes and blackening the skin. It reduces the elasticity by modifying collagen and elastin, causing skin aging after prolonged exposure. Recently, the amount and intensity of ultraviolet rays reaching the earth's surface are increasing every year due to the destruction of the ozone layer due to air pollution caused by industrial development. A 1% decrease in ozone increases UV radiation in the atmosphere by about 2%, leading to a 3% increase in skin cancer patients. This can significantly increase the incidence of sunburn, cataracts, skin aging, and skin cancer, adversely affecting health. Therefore, in order to protect the skin from ultraviolet light, appropriate measures are required, and among them, the use of sunscreen is one of the easy methods.

The skin is histologically composed of epidermis, dermis and subcutaneous fat. The thickness varies according to the site, age and sex. The skin plays a role in external barrier function and other physiological functions. The stratum corneum is a high-density structure of keratin, a relatively insoluble protein with high hydrophobicity, sandwiched between intercellular lipid bilayers, a thin layer of lipids, and a unique hierarchical structure of a matrix rich in lipids and insoluble proteins. Create an impervious nature for However, in the case of cosmetics, components such as solvents and emulsifiers promote skin penetration of drugs, and recently, cosmetics are designed to reduce the side effects of drugs and maximize the efficacy and efficacy to deliver the required amount of drugs locally to the skin. The introduction of drug delivery systems (DDS) using nanotechnology, such as formulations, so-called liposomes, microsponges, polymer microcapsules and nanocapsules, is increasing.

Generally, various physical and chemical methods (liposomes, nanocapsules, amphiphilic molecular structure of drugs, etc.) are used to promote the percutaneous absorption of drugs to enhance the effects of bioactive substances. Skin penetration and exposure to sunlight can lead to poor UV protection, photoallergy, phototoxicity, and skin irritation. The maximum UV absorption wavelength (λmax) of a chemical sunscreen is changed by the effect of pH value between the sunscreen and the formulation, the shift effect according to the use of polar or nonpolar solvents, and the unique extinction coefficient of the sunscreen. Affects. Therefore, it is desirable to introduce an appropriate drug delivery system for the sunscreen to remedy these shortcomings.

Therefore, the inventors of the present invention are developing capsules by applying solid lipids while developing a new delivery system that can improve the disadvantages of the existing organic sunscreen, bisethylhexyloxyphenolmethoxyphenyltriazine. In this case, it was found that not only a fine and uniform capsule can be obtained while lowering the skin irritation, but also the sunscreen effect can be increased.

Currently, encapsulation method using solid lipids has improved solid solubility and encapsulation efficiency in addition to classical solid lipid capsules made of lipids such as wax, mono-, di-, triglycerides, fatty acid alcohols, and glycerin trifatty acid esters. and the liquid phase and the like nanostructured lipid carriers is presented consisting of a mixture of lipids. (International Journal of Pharmaceutics . 2000: 199 : 167-177, SOFW Journal . 2007: 133: 14-20) in the case of solid lipid capsules until now applying physiologically active ingredients such as Ascorbyl palmitate and Coenzyme Q10, Fellulic acid is much (International Journal of Pharmaceutics . 2005: 295 : 261-268, International Journal of Pharmaceutics . 2007: doi:. 10.1016 / j.ijpharm.2007.03.022 ) However, in the case of solid lipid apply sunscreen capsule, case applying the benzophenone-3 and oxybenzone are some reported (International Journal of Pharmaceutics . 2002: 242 : 373-375, International Journal of Pharmaceutics . 2003: 254 : 65-68), but there is no use of bisethylhexyloxyphenol methoxyphenyl triazine applied in the present invention. Similarly, there is a report on a sunscreen cosmetic composition (Korean Patent 10-0684367) in which bisethylhexyloxyphenolmethoxyphenyltriazine is supported on a polysilsesquioxane spherical capsule having a sunscreen, but the present invention has been applied. Different from solid lipid capsules.

In addition, in the cosmetic composition of the present invention, if the purpose of the development of a spray type mist (MIST) or lotion, cream-type sunscreen products, it is possible to make a sunscreen product with ease of use and excellent UV blocking ability.

Accordingly, an object of the present invention is to provide a solid lipid capsule having a size of 100 to 1000 nm using bisethylhexyloxyphenol methoxy phenyl triazine as an organic sunscreen.

In addition, an object of the present invention is to provide a sunscreen cosmetic composition with less skin irritation, fine and uniformly applied to the skin to improve the sunscreen effect.

And it is to provide a sunscreen cosmetic composition of the spray type mist (MIST) easy to use by using the characteristics of the fine solid lipid capsule.

In order to achieve the above object, the present invention relates to a sunscreen cosmetic composition containing a solid lipid capsule of 100 to 1000nm size prepared using bisethylhexyloxyphenol methoxyphenyl triazine as an organic sunscreen.

Bisethylhexyloxyphenol methoxyphenyl triazine-encapsulated method of producing a solid lipid capsule of the present invention has been reported (Korean Patent Laid-Open Patent No. 1994-7002365) has been utilized by those skilled in the art. As follows.

A suitable amount of bisethylhexyloxyphenol methoxyphenyltriazine and solid lipid is mixed and then dissolved at 80 ° C. The molten lipid phase is added to an aqueous phase of 80 ° C. in which an appropriate amount of emulsifier and polyol are dissolved, and then treated by a mechanical method using a sonicator or a high pressure emulsifier to homogenize and finely quenched to 10 ° C. or lower. After standing for 24 hours at ℃ ℃ through the physical stability period is obtained a solid lipid capsule of 100 ~ 1000nm size is encapsulated bisethylhexyloxyphenol methoxyphenyl triazine.

In another aspect, the present invention provides a cosmetic composition containing 0.01 to 37% by weight of bisethylhexyloxyphenolmethoxyphenyltriazine and 0.01 to 50% by weight of solid lipid capsules based on the total weight of the cosmetic composition.

If the content of the bis-hexyloxy phenol methoxy phenyl triazine is less than 0.01% by weight is almost no UV protection effect, when more than 37% by weight is not economical and the sealing efficiency is lowered. When the content of the solid lipid capsule is less than 0.01% by weight, the sunscreen effect is also insignificant, and when it is more than 50.0% by weight, the feeling of use is inferior and economical.

In addition, the sunscreen cosmetic composition obtained by the present invention can be formulated as a spray mist (MIST), lotions, creams and the like.

Traditionally, emulsions that form emulsified particles depending on emulsifiers are not able to produce spray-type mist (MIST) formulations due to the significant change of oil droplets due to external stress, but solid lipid capsules are formed into uniform microspheres of 100-1000 nm. Since there is no change in particle size due to external physical change, it is possible to easily provide a sunscreen cosmetic composition in the form of a spray mist.

Furthermore, the sunscreen cosmetic composition of the present invention may be mixed with disodium phenyldibenzimidazole tetrasulfonate, phenylbenzimidazole sulfonic acid, etc., to further improve the sunscreen effect.

Hereinafter, the present invention will be described in more detail with reference to Examples. However, these Examples are only illustrative description of the present invention and the scope of the present invention is not limited to these Examples.

Production Example  1: Preparation of Solid Lipid Capsule

In the present production example, the aqueous phase (A) was heated and dissolved in the composition ratio of Table 1 and physically dispersed in the aqueous phase (B), followed by quenching and aging for 1 day to solidify bisethylhexyloxyphenolmethoxyphenyltriazine. The preparation of lipid capsules was completed.

ingredient Content (in 100 g) Preparation Example 1 (A) Bisethylhexyloxyphenol methoxyphenyl triazine 10 Cetyl palmitate 10 (B) Soybean hydrogenated lecithin 2.0 Polysorbate 60 0.5 Butylene Glycol 10 glycerin 10 Purified water Remaining amount

Production Example  2 to 4: UV protection with solid lipid capsule Cosmetics  Preparation of the composition

Preparation Examples 2 to 4 were prepared by heating and mixing the composition of the sunscreen cosmetic composition to which the solid lipid capsules were added, as shown in Table 2, and added the solid lipid capsules of Preparation Example 1. The solid lipid capsule of Preparation Example 4 was prepared by the same method as Preparation Example 1, in which bisethylhexyloxyphenol methoxyphenyl triazine was not encapsulated.

ingredient Content (in 100 g) Preparation Example 2 Preparation Example 3 Preparation Example 4 Acrylate / C10-30 Alkyl Acrylate Crosspolymer Quantity Quantity Quantity Butylene glycol 10.0 5.0 5.0 C12-15 Alkyl Benzoate 10.0 - - Polysorbate 60 1.0 - - Sorbitanate 3.0 - - Bisethylhexyloxyphenol methoxyphenyl triazine 1.0 - - Preparation Example 1 - 10.0 - Solid lipid capsule (placebo) - - 10.0 Triethanolamine Quantity Quantity Quantity Preservative Quantity Quantity Quantity Purified water  Remaining amount

The composition of the present invention was shown in Preparation Examples 5, 6, and 7 in several formulations.

ingredient Content (in 100 g) Preparation Example 5 Mist Preparation Example 6 Cream Preparation Example 7 Lotion Ethylenediaminetetradiacetic acid sodium Quantity Quantity Quantity Cetearyl Alcohol / Cetearyl Glucoside - 1.0 - Sodium hyaluronate - 1.0 1.0 Glyceryl Stearate SE - 2.0 2.0 Soybean hydrogenated lecithin - 0.5 0.5 Cetanol - 1.5 0.5 Phenylbenzimidazolesulfonic acid 3.0 3.0 3.0 Preparation Example 1 20.0 20.0 20.0 Squalane - 5.0 0.5 ethanol 10.0 - - Butylene glycol 5.0 5.0 5.0 Propylene glycol 2.0 - - Triethanolamine Quantity Quantity Quantity Tocopherol Acetate - 1.0 0.50 Preservative Quantity Quantity Quantity Spices Quantity Quantity Quantity Purified water Quantity Remaining amount Quantity

Production Example  8 to 9: Light stability  Preparation of the composition for the experiment

Preparation Examples 8 to 9 were prepared by mixing bisethylhexyloxyphenol methoxyphenyltriazine in a composition ratio as shown in Table 4 and adding the solid lipid capsule of Preparation Example 1.

ingredient Content (in 100 g) Preparation Example 8 Preparation Example 9 Tetrahydrofuran 25 - Carbomer - 0.1 Triethanolamine - 0.1 Bisethylhexyloxyphenol methoxyphenyl triazine 0.1 - Preparation Example 1 - 1.0 Purified water Remaining amount Remaining amount

Test Example  1: for ultraviolet in in vitro  Cell viability experiment

Table 5 below is an experiment for evaluating the sunscreen effect of the cosmetic composition of Preparation Example 2 and Preparation Example 3, and evaluates the UV blocking ability of the solid lipid capsule. Human dermal fibroblasts used in this test example were used from the American Type Culture Collection (ATCC) Accession No .: CRL 1635.

Evaluation of the sunscreen effect of the solid lipid capsule containing the sunscreen on human dermal fibroblasts was performed as follows.

Cell viability test for UV irradiation using human dermal fibroblasts (HDFs) is carried out in a 35Φ plate at a concentration of 1.5 × 10 ⁵ cells / mL and incubated until reaching 80% confluency. Remove the culture medium before UVB irradiation and wash with PBS to remove serum in medium. 0.4 mL of Preparation Example 2 and Preparation Example 3 were taken on the plate, and the plate was covered with a quartz plate (100 mm × 100 mm × 30 mm) uniformly coated to a thickness of 0.04 mm using an applicator and irradiated with ultraviolet rays. The UVB light source was G6T5E (Sankyo denky Co., Japan), and the UV irradiation intensity was 50 mJ / cm ² , after 24 hours of irradiation. It was then incubated in a 37 ℃ CO ² incubator for 2 hours. Lysing the cells with DMSO and transferring 100 μl each into a 96-well plate. The cell viability was compared by measuring the absorbance at 565 nm with an ELISA reader.

 As a result, looking at the following Table 5, when smearing the sunscreen cosmetic composition of Preparation Example 3, the cell survival rate was 88% or more, so that the solid lipid capsules encapsulated with bisethylhexyloxyphenol methoxyphenyl triazine were exposed to the skin against ultraviolet rays. It was found to be more effective in protection.

sample Cell survival rate (%) No UVB Probe 100 UVB 50mJ / cm ² Probe 54 Preparation Example 2 67 Preparation Example 3 88

Test Example  2: In in vitro  UV protection effect experiment

This test example is an experiment for evaluating the sunscreen effect of the cosmetic composition of Preparation Example 2, Preparation Example 3 and Preparation Example 4, and evaluates the ultraviolet blocking ability of the solid lipid capsule. Evaluation of the sunscreen effect of the solid lipid capsule encapsulated with a sunscreen was performed by the following method. In In vitro SPF (ultraviolet ray block index) and PFA (erythema index) were measured by Optometrics SPF 290 Analyzer (USA). Xenone arc lamp is used as the light source and the wavelength range is 290 ~ 400nm. In the measurement method, after attaching a quartz plate (100 mm × 100 mm × 30 mm) to the sample holder, take 0.2 mL of Preparation Example 2, Preparation Example 3, and Preparation Example 4, respectively, and apply uniformly to a thickness of 0.04 mm using an applicator. The total position was scanned six times by changing the position every two measurements on one plate. In the results of Table 6, the cosmetic composition of Preparation Example 3, the UV protection index and erythema index of 12.71 and 11.46 was about 2.5 times higher than in Preparation Example 2 it was found that the skin protection effect against ultraviolet rays is more excellent. In the case of Preparation Example 4, the ultraviolet ray blocking effect was weak.

sample UV Protection Index (SPF) Erythema Index (PFA) Preparation Example 2 4.63 ± 0.21 4.84 ± 0.19 Preparation Example 3 12.71 ± 0.58 11.46 ± 0.44 Preparation Example 4 1.18 ± 0.01 1.32 ± 0.01

SPF = minimum amount of erythema at the product application site / minimum amount of erythema at the product-free area

PFA = minimum continuous instantaneous blackening of the product application site / minimum continuous instantaneous blackening of the product coating site

Test Example  3: solid lipid capsule Light stability  Improvement effect experiment

This test example measured the photodegradation improvement effect of bisethylhexyloxyphenol methoxyphenyl triazine after ultraviolet irradiation with respect to the composition of manufacture example 8 and manufacture example 9. In the experiment, Preparation Example 7 in which bisethylhexyloxyphenol methoxyphenyltriazine was dispersed in the form of oil droplets and Preparation Example 8 in the form of solid lipid capsules were used as test samples. In a quartz tube (10 mm × 10 mm × 40 mm), using a solar simulator (200W Xenon-Mercury lamp, UVA + UVB filter, 601-300 Multiport®, Solar light Co., USA) 4 times of 3 hours were investigated. After irradiation, the degree of photolysis of bisethylhexyloxyphenolmethoxyphenyltriazine in the product was measured using HPLC. The results of Table 7 show that the degree of decomposition of bisethylhexyloxyphenol methoxyphenyltriazine was 12 hours after ultraviolet irradiation, and the bisethylhexyloxyphenol methoxyphenyltriazine of Preparation Example 9 was 91% or more of the drug. Although the content was maintained, the bis-hexyl oxy phenol methoxyphenyl triazine of Preparation Example 8 was reduced by about 20%. The solid lipid capsule form lipid construct of the present invention thus exhibits excellent photostability with respect to bisethylhexyloxyphenolmethoxyphenyltriazine.

sample % Recovery 0 hours 3 hours 6 hours 9 hours 12 hours Preparation Example 8 100 91 91 85 80 Preparation Example 9 100 97 96 92 91

1 is a photograph of the appearance and size of a solid lipid capsule containing bisethylhexyloxyphenol methoxyphenyl triazine applied to the present invention by cryo-SEM.

Claims (4)

Bisethylhexyloxyphenolmethoxyphenyltriazine, an organic sunscreen, is encapsulated in an amount of 0.01 to 37% by weight of solid lipid capsules of 100 to 1000 nm in size. A sunscreen cosmetic composition comprising the solid lipid capsule of claim 1 in an amount of 0.01 to 50% by weight based on the total weight of the composition. The sunscreen cosmetic composition of claim 2, wherein the sunscreen cosmetic composition is formulated as a spray mist, lotion, cream, or the like. The sunscreen according to claim 3, wherein the sunscreen is selected from water-soluble auxiliary sunscreens such as disodium phenyl dibenzimidazole tetrasulfonate and phenylbenzimidazole sulfonic acid. A sunscreen cosmetic composition, characterized in that the substance is contained in an amount of 0.01 to 4% by weight, respectively.

Images