KR20120053701A - O/w type cosmetic composition containing liquid crystal complex for enhancing skin permeability - Google Patents

Abstract

PURPOSE: A cosmetic composition containing crystalline structure for enhancing transdermal permeation is provided to enable permeation of water soluble active ingredients into the keratin layer. CONSTITUTION: An oil-in-water cosmetic composition contains water soluble active ingredients, amphiphilic substances, and polymer surfactant as an active ingredient. The water soluble active ingredient includes magnesium, L-ascorbyl-2-phosphate, niacin amide, arbutin, adenosine, ascorbyl glucoside, kojic acid, caffeine, calcium pantetheine sulfonate, trisodium fructose diphosphate, aminopropyl ascorbyl phosphate, or sodium ascorbyl phosphate. The amphiphilic substance includes oleic acid monoglyceride, butane triol, or glycerol ester. The polymer surfactant includes polyethylene glycol/polypropyelen glycol block copolymer, inulin lauryl carbamate, or mixture thereof.

Description

O / W type cosmetic composition containing liquid crystal complex for enhancing skin permeability}

The present invention relates to an oil-in-water cosmetic composition comprising a liquid crystal structure that enhances the percutaneous permeation of the water-soluble useful component, and more particularly, to a polyphase liquid crystal containing a water-soluble useful component, an amphiphilic substance and a polymer surfactant. It relates to a cosmetic composition in which the structure is stably included in an underwater type emulsion.

The outermost stratum corneum of human skin is an organ that maintains the skin barrier function and blocks the incoming material. The stratum corneum of the skin is composed of keratinocytes and intercellular keratinocytes. The keratinocyte lipids fill between the keratinocytes and form a lamellar liquid crystal structure. Such lamellar liquid crystals are known to affect the flexibility and moisturizing of the skin. This unique structure is known as the "Brick and Mortar Model" and gives the skin's very important skin barrier function and keeps moisture in the stratum corneum to give skin elasticity, flexibility and moist feeling. Due to this skin barrier function, there are many difficulties in transferring useful components deep into the skin. Useful ingredients generally applied in the cosmetic field may be classified into components having lipophilic and hydrophilic properties, respectively, according to their molecular structure. Due to the characteristics of the stratum corneum, which is composed of a phospholipid bond structure, it is almost impossible to deliver deeply into the skin through the stratum corneum, especially in the case of the hydrophilic component of the useful components.

The liquid crystal structure constituting the stratum corneum forms various liquid crystals depending on the substance constituting the liquid crystal. Basically, it can be classified into two types according to the principle of liquid crystal formation. The lyotropic liquid crystal and the thermotropic liquid crystal are the lyotropic liquid crystal. Amphiphilic molecules that share both nonpolar and hydrophobic properties.

Liquid crystals mainly used in cosmetics are lyotropic liquid crystals. When two different substances are mixed, the mixture shows different liquid crystal phases when the temperature is changed or the concentration of one component of the mixture is changed. It refers to a liquid crystal that depends on the relative concentration. In other words, it refers to a liquid crystal expressed by the interaction between an amphiphilic molecule and a polar solvent.

When an amphiphilic molecule is dissolved in water, which is a polar solvent, the surfactant is initially present as a monolayer at the interface between water and air, or when the concentration is higher than a certain concentration, micelles are formed. If the hydrophilic group is not strong enough for the hydrophobic group then the molecules form vesicles. This globular blister is a bilayer of surfactant molecules that forms a layer with water inside and outside. If the concentration of the surfactant increases further (usually 50%), micelles or blisters reach a point where they bind to each other to form a larger structure. First, the hexagonally long cylindrical rods are arranged along the long axis of the rods in the hexagonal array. The second is the lamellar phase, which is formed at higher concentrations, forming a flat bilayer in which the surfactants are separated from each other by water. The third is the cubic phase, which exists between the lamellar phase and the hexagonal phase and is connected in such a way that the cubic phases are isolated from each other.

Amphiphilic substances in polar solvents are dissolved or hydrated and form spherical micelles as the concentration increases. As the concentration increases, the spherical micelles are cylindrical micelles and cylindrical micelles. Hexagonal phase, cubic phase, and lamellar phase, which are formed by stacking, form higher concentrations and the hydrophilicity and lipophilic part change, resulting in more dense cubic and reverse hexagonal phases. phase). The inverted hexagonal liquid crystals having lipophilic properties on the outside and hydrophilic properties on the inside have liquid crystal structures such as the stratum corneum and the lipophilic exterior, and thus have high affinity with the stratum corneum and interact with the stratum corneum.

In the present invention, a method of collecting and delivering a hydrophilic useful material therein by using a liquid crystal forming an inverted hexagonal structure having lipophilic properties among various methods proposed to solve the skin permeation problem of the hydrophilic useful material mentioned above. Try to use The liquid crystal structure similar to that of the stratum corneum layer is used to disturb the phospholipid liquid crystal structure, which forms the stratum corneum layer, and transfer useful substances between the stratum corneum layers.

Although this technique has been used in a limited range of pharmaceutical drug delivery applications, it has been very difficult to apply to cosmetics due to various problems. In the case of the inverted hexagonal structure, the continuous phase is dispersed in the O / W emulsion, which is not well distributed, and is not evenly distributed, and there is a problem in that the structure cannot be maintained intact due to the influence of a surfactant used in cosmetics.

Accordingly, the present inventors made an emulsion containing a polymer surfactant to stably include a liquid crystal having a polymorphic structure in an underwater type emulsion (O / W Emulision) that improves the skin permeability of hydrophilic useful components. The invention was found to be able to make a uniform and stable O / W emulsion to complete the present invention.

Accordingly, it is an object of the present invention to provide a stable oil-in-water cosmetic composition comprising a polyhedral liquid crystal structure that promotes skin permeation of a hydrophilic useful component.

In order to achieve the above object, the present invention provides an oil-in-water cosmetic composition stabilized polyhedral liquid crystal structure by including a water-soluble useful material, an amphiphilic material and a polymer surfactant as an active ingredient.

The water-based cosmetic composition according to the present invention forms a multi-phase liquid crystal using an amphiphilic material, so that the lipophilic exterior has a high degree of interaction with a highly useful stratum corneum, which can easily perturb the stratum corneum structure and penetrate deeper. The water-soluble useful ingredient may be absorbed through the stratum corneum together. In addition, by stabilizing the liquid crystal structure evenly dispersed with a polymer surfactant it is excellent in stability and can maintain the liquid crystal structure for a long time.

1 is a transmission electron micrograph of a dispersed liquid crystal structure according to the present invention.

The present invention provides an oil-in-water cosmetic composition stabilized polyhedral liquid crystal structure by including a water-soluble useful material, an amphiphilic material and a polymer surfactant as an active ingredient.

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

Amphiphilic material used to form a polyphase liquid crystal in the present invention may be used oleic acid monoglyceride (oleic acid monoglyceride), butanetriol (butantriol), glycerol ester (glycerol ester) and the like. These materials are known to have spontaneous curvature (SC) values spontaneously forming liquid crystals when HLB values and dense structures are formed. When mixed with water using the above components, the lipophilic liquid crystal structure is spontaneously increased to increase the penetration of the useful components into the skin.

Amphiphilic material forming the liquid crystal structure used in the present invention is contained in 5 to 20% by weight based on the total weight of the composition. If the content is less than 5% by weight, the formation of the liquid crystal structure is not good, if it exceeds 20% by weight it is difficult to add to the emulsion is not suitable.

Such a lipophilic liquid crystal structure is difficult to stably exist in an oil-in-water emulsion. Polyphase liquid crystals, which have a very low affinity with the aqueous phase, which is a continuous phase of oil-in-water emulsions, are not evenly dispersed and have a non-uniform particle size as a commonly used dispersing method. In this case, unification by Ostwalt Ripening This results in phase separation and impairs the stability of the emulsion. In order to help disperse the components that are not easy to disperse, an emulsifier / dispersant having surfactant activity is generally used. In this case, when an emulsifier / dispersant used in general is used, the liquid crystal interacts with the amphiphilic substances forming the liquid crystal. Destroying the structure. In addition, the emulsifiers used to make oil-in-water emulsions also interact with the amphiphilic materials that make up liquid crystals, destroying the liquid crystal structure.

In the present invention, to solve this problem, the emulsifier used in dispersing the liquid crystal structure by using the surfactant in the polymer form and making the oil-in-water emulsion was also used the surfactant in the polymer form. In the case of the polymer surfactant, even though the molecular size is very large, it can minimize the destruction of the already formed liquid crystal structure. Polymeric surfactants usable in the present invention include polyethylene glycol / polypropylene glycol block copolymers, inulin lauryl carbamate or mixtures thereof, and specific examples thereof include BASF. And PEG / PPG block copolymers (poloxamers) from Corporation, but are not limited thereto.

The polymer surfactant of the present invention is contained 0.1 to 10% by weight based on the total weight of the composition. If the content is less than 0.1% by weight, the emulsion is unstable. If the content is more than 10% by weight, the liquid crystal structure is unstable and the application property is lowered, which is not suitable.

The water-soluble useful material used in the present invention can be applied in various ways, and most of the components having a property of dissolving in water are generally applicable. Specific examples include magnesium L-ascorbyl-2-phosphate, niacinamide, arbutin, adenosine, ascorbyl glucoside, cosciacid, caffeine, calcium panteinsulfonate, trisodium fructose diphosphate, aminopropyl ascorbyl Phosphate, sodium ascorbyl phosphate, and the like, but is not limited thereto.

The water-soluble useful substance of the present invention is contained in 0.01 to 13% by weight relative to the total weight of the composition. When the content is less than 0.01% by weight, the effect on the skin is insignificant, and when the content is more than 13% by weight, the liquid crystal structure is not contained therein, so that the effect of enhancing skin penetration is reduced.

The present invention produces an emulsion containing a liquid crystal composed of a hydrophilic useful component, an amphiphilic substance and a polymer surfactant, and then prepares a uniform and stable oil-in-water emulsion using a high pressure emulsifier.

The polygonal liquid crystal structure of the present invention is more preferably a reverse hexagonal phase liquid crystal structure.

The oil-in-water emulsion cosmetic composition containing the liquid crystal structure of the present invention is preferably suitable for products of functional creams and lotions containing water-soluble useful ingredients, but as general creams and lotions for skin moisturizing and protective functions using liquid crystal structures. It can be manufactured and used according to the use.

Hereinafter, an Example is given and this invention is demonstrated in detail. However, these embodiments are intended to illustrate the present invention in detail, and the scope of the present invention is not limited by these embodiments.

EXAMPLE 1 AND COMPARATIVE EXAMPLES 1-3

The emulsion formulations of Example 1 and Comparative Examples 1 to 3 were prepared according to the compositions shown in Table 1 below.

Example 1 of the present invention is prepared by using an amphiphilic glycerol ester to form an inverted hexagonal liquid crystal structure which is a system containing 10% by weight of a water-soluble useful component and can improve the skin permeation of the component by more than 88%, In order to keep the liquid crystal produced in the oil-in-water emulsion stable, high molecular weight inulin lauryl carbamake and PEG / PPG block copolymers were used as dispersion stabilizers and formulation emulsifiers. Photographed under a microscope (Cryo TEM) is shown in FIG. As can be seen in Figure 1, it was confirmed that the particle diameter of the dispersed liquid crystal structure is uniformly distributed to 200 ~ 250 nm.

Comparative Example 1 prepared a ceramide liquid crystal instead of a glycol ester, and mixed with magnesium L-ascorbyl-2-phosphate into the liquid crystal phase, Comparative Example 2 polysorb instead of inulin lauryl carbamate, PEG / PPG block copolymer Bait 60 and sorbitan stearate were added and emulsified. Comparative Example 3 was prepared in the same composition as in Example 1, but was prepared using only a homogenizer without a high pressure emulsifier process.

ingredient Example 1
(weight%) Comparative Example 1
(weight%) Comparative Example 2
(weight%) Comparative Example 3
(weight%) Awards Purified water to 100 to 100 to 100 to 100 glycerin 5 5 5 5 Butylene Glycol 5 5 5 5 Phenoxyethanol 0.5 0.5 0.5 0.5 Carbomer 0.1 0.1 0.1 0.1 Inulin Lauryl Carbamate 1.5 1.5 - 1.5 PEG / PPG Block Copolymer 1.5 1.5 - 1.5 Xanthan gum 0.2 0.2 0.2 0.2 Paid Hydrogenated C6-14 Olefin Polymer 3 3 3 3 Cetyloctanoate 3 3 3 3 Hydrogenated Jojoba Oil 3 3 3 3 Beads wax One One One One Cyclomethicone 5 5 5 5 Polysorbate 60 - - 1.5 - Sorbitan stearate - - 1.5 - LCD Magnesium L-ascorbyl-2-phosphate 10 10 10 10 Glycol ester 10 - 10 10 Ceramide liquid crystal - 10 - -

<Manufacturing Method>

1) The aqueous phase component was dissolved while heating to 70 ° C.

2) The oily ingredients were separately dissolved while heating to 70 ° C.

3) The liquid crystal phase components were mixed evenly until viscous in a separate container.

4) The oily liquid mixture of 2) was added to the aqueous liquid mixture of 1) and emulsified with a homogenizer.

5) The emulsified mixture of 4) was cooled to 45 ° C.

6) The liquid crystal mixture of 3) was added to the mixture of 5) and dispersed in a homogenizer.

7) The evenly dispersed mixed solution of 6) was dispersed and stabilized at a high pressure using an APV Homogeizer.

Test Example 1 Skin Permeation Measurement

The skin permeability of magnesium L-ascorbyl-2-phosphate as a water-soluble useful ingredient of the emulsions prepared in Examples 1 and Comparative Examples 1 to 3 was measured. As a first method, skin permeability was measured using an artificial skin model obtained by culturing from skin cells. Magnesium L-ascorbyl-2-phosphate was added to the artificial skin model, incubated at 32 ° C for 24 hours, and after washing, the amount of magnesium L-ascorbyl-2-phosphate in the dermis and epidermis was measured. Skin permeability was calculated. In the second method, 30 mg / cm2 of cosmetic composition was absorbed into the forearm of five men, and after 3 hours, the amount of magnesium L-ascorbyl-2-phosphate absorbed by using a tape stripping method was measured. Measured.

Magnesium L-ascorbyl-2-phosphate recovery (μg) division Artificial skin model method Tate peeling method Example 1 178 543 Comparative Example 1 108 416 Comparative Example 2 87 389 Comparative Example 3 131 490

Looking at the results of Table 2, it was confirmed that the magnesium L- ascorbyl-2- phosphate of the larger amount of Example 1 penetrated the skin compared to Comparative Examples 1 to 3 immediately after the experiment. This shows that in the case of Example 1, the inverted hexagonal liquid crystal was stably dispersed in the oil-in-water emulsion to enhance skin permeation of magnesium L-ascorbyl-2-phosphate, a water-soluble useful ingredient. Unlike Example 1, in Comparative Example 1 using a ceramide liquid crystal rather than an inverted hexagonal liquid crystal, skin permeability of the useful component was confirmed to be inferior. In addition, the inverted hexagonal liquid crystal was formed, but Comparative Example 2 using a common surfactant other than the polymeric surfactant and Comparative Example 3, in which the stability was lowered by not undergoing a high-pressure emulsification process, also confirmed that the water permeability of the water-soluble useful component is poor. Could.

[Test Example 2]

In the emulsion prepared in Example 1 and Comparative Examples 1 to 3 it was confirmed whether the stability of the formulation and the liquid crystal structure is maintained. Formulation stability measurement of the emulsion was determined by observing the oil separation and emulsion breakdown of the sample compared to the room temperature storage samples by storing for 4 weeks at a constant temperature of 30 ℃, 45 ℃. The liquid crystal structure was measured using transmission electron microscope (Cryo TEM) and SAXS after 4 weeks storage under the above conditions.

division Oil painting stability Liquid crystal structure 30 ℃ 45 ° C 30 ℃ 45 ° C Example 1 good good has exist has exist Comparative Example 1 good usually none none Comparative Example 2 good usually none none Comparative Example 3 Bad Bad has exist none

Looking at the results of Table 3, in the case of Example 1, Comparative Examples 1 and 2 except for Comparative Example 3, it was confirmed that the emulsion stability is all present in a good state, but in Example 1 only in the inverted hexagonal liquid crystal In Comparative Examples 1-2, it was confirmed that the liquid crystal structure was destroyed. In addition, in the case of Comparative Example 3, there is a liquid crystal structure, but at a high temperature, the liquid crystal is broken and stability is not good, so it is difficult to use it as a cosmetic composition.

Claims (9)

Oil-in-water cosmetic composition stabilized polyhedral liquid crystal structure by containing a water-soluble useful material, an amphiphilic material and a polymer surfactant as an active ingredient. The method of claim 1, wherein the water-soluble useful substance is magnesium L- ascorbyl-2-phosphate, niacinamide, arbutin, adenosine, ascorbyl glucoside, coscides, caffeine, calcium panteinsulfonate, trisodium fructose di Oil-in-water cosmetic composition, characterized in that at least one member selected from the group consisting of phosphate, aminopropyl ascorbyl phosphate and sodium ascorbyl phosphate. The oil-in-water cosmetic composition according to claim 1, wherein the amphiphilic substance is at least one selected from the group consisting of oleic acid monoglycerides, butanetriol and glycerol esters. The oil-in-water cosmetic composition according to claim 1, wherein the polymer surfactant is polyethylene glycol / polypropylene glycol block copolymer, inulin lauryl carbamate or a mixture thereof. The oil-in-water cosmetic composition according to claim 1, wherein the water-soluble useful substance is contained in an amount of 0.01 to 13% by weight based on the total weight of the composition. The oil-in-water cosmetic composition according to claim 1, wherein the amphiphilic material is contained in an amount of 5 to 20% by weight based on the total weight of the composition. The oil-in-water cosmetic composition according to claim 1, wherein the polymer surfactant is contained in an amount of 0.1 to 10% by weight based on the total weight of the composition. The oil-in-water cosmetic composition according to claim 1, wherein the liquid crystal structure is stabilized and manufactured by using a high pressure emulsifier. The oil-in-water cosmetic composition according to claim 1, wherein the polygonal liquid crystal structure is inverted hexagonal shape.

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