KR20010083712A - composition for liposome cosmetics and preparation method thereof - Google Patents

Abstract

PURPOSE: Provided is a cosmetic composition comprising liposome which can contain a large amount of active ingredients. Also, its preparation method is provided. CONSTITUTION: The cosmetic composition contains a liposome and encapsulates skin activating extract with the liposome stabilized by lecithine, ethanol, ester oil, propylene glycol, cholesterol or beta-sitosterol and vegetable oil. The method for preparing such liposome cosmetic composition comprises the following steps of: mixing 2 to 3wt% of lecithine, 10 to 15wt% of ethanol, 20 to 30wt% of ester oil, 5 to 10wt% of propylene glycol and purified water, and homogenizing the mixture by 3000 rpm at 70 deg.C; pressurizing the homogenized lecithine mixture under 800 atmosphere to form lecithine base; mixing 35 to 45wt% of the formed lecithine base, 15 to 40 wt% of effective extract and purified water, and pressurizing the mixture under 800 atmosphere; adding 0.1 to 0.6wt% of cholesterol or beta-sitosterol and 10 to 15wt% of vegetable oil and pressurizing the mixture under 800 atmosphere; if desired, adding 2 to 3wt% of ceramides to the mixture and pressurizing the mixture under 800 atmosphere. The composition can be applied transdermally as a patch form or can be directly coated on a human skin.

Description

Liposome cosmetic composition and method for preparing the same

The present invention relates to a liposome cosmetic composition containing a liposome encapsulated with an active ingredient and a method for preparing the same. In another aspect, the present invention by using a non-woven fabric containing a liposome cosmetic composition to increase the percutaneous absorption of the active ingredient to prevent skin wrinkles, whitening effect, soothing effect.

There are three pathways through the skin: absorption through the stratum corneum, absorption through the hair follicle and sebaceous glands, and absorption through the eccrine gland. As far as is known, absorption through the stratum corneum is the most important absorption pathway. Since the stratum corneum consists of nonpolar lipids in the stratum corneum, the polar substance is hardly absorbed and the lipophilic substance can be absorbed. have. In the case of polar substances, they are combined with the protein part in the cytoplasm or interstices by means of hydrogen bonding, and are not absorbed through the skin. Nonpolar substances, on the other hand, are primarily dissolved in the cell gap and sometimes cross the skin barrier. However, even through the stratum corneum, the solubility in the lower stratum corneum is less, it is prevented from being absorbed systemically by mechanisms such as enzymes that cause various metabolism and exfoliation of keratinocytes. On this principle, the stratum corneum protects the body from numerous external polar substances, but nonpolar poisons can be absorbed into the stratum corneum.

The greatest barrier to transdermal absorption is keratinocytes in the stratum corneum as described above and keratinocyte lipids therebetween. Since most of the active ingredients have a low percutaneous permeability due to the resistance of the stratum corneum, various methods are needed to overcome them and promote permeation of the active ingredients. The mixing of lipophilic substances with ethanol, propylene glycol, surfactants, fatty acids, etc. is a very effective method of transdermal delivery of components at the required speed and effective concentration. In addition, the use of liposomes made from the active ingredients such as lecithin or intercellular lipid components is a much more effective method of transdermal absorption.

Liposomes are described in detail as follows.

Liposomes are defined as spherical phospholipid becycloids of colloidal particles that associate themselves, and liposomes composed of amphiphilic molecules with water-soluble heads (hydrophilic groups) and insoluble tails (hydrophobic groups) spontaneously bind and form an ordered structure by their interaction. It is classified into Small Unilamellar Vesicle (SUV), Large Unilamellar Vesicle (LUV), and Multi Lamellar Vesicle (MLV) according to its size and lamellarity. The liposomes exhibiting various laminations are about 20 nm to several nm in size, and a double membrane having a structure similar to that of a cell membrane is used as a similar model of a biological membrane and has a thickness of about 4 nm. Liposomes made from natural lipids such as lecithin are more biodegradable and biocompatible than liposomes made from synthetic lipids, so the water-soluble component is in the aqueous core and the oil-soluble component is in the phospholipid membrane. It is solubilized to encapsulate both hydrophilic and lipophilic materials. Liposomes can contain many active substances, such as active ingredients, flavors, drugs, and vaccines, and the encapsulated materials will be released slowly over time. The release of encapsulated substances is enhanced by enhancing the rigidity of the double membrane. I can regulate it.

In conclusion, the fact that the skin active ingredient does not properly penetrate the stratum corneum and the cosmetic composition is very low in the percutaneous absorption.

In the conventional composition of the cosmetic using a liposome, the amount of the active ingredient may be about 15% by weight, and it is also unstable, so that the liposome is broken before being absorbed by the skin, and thus the cosmetic composition including the liposome that is somewhat stable is not achieved. Even if the effective transdermal absorption method using the nonwoven fabric was not performed, the pharmacological effect could not be properly applied to the skin.

The present invention has developed a stable liposome that can contain a large amount of the active ingredient in order to solve the drawbacks of the conventional liposome composition which can contain only a small amount of the active ingredient and is unstable, and as a conventional method, by applying directly to the skin in general In addition to the method of absorption, using a transdermal application method using a nonwoven fabric, etc., the percutaneous absorption rate is increased to provide maximum pharmacological effect to the skin.

An object of the present invention is to prepare a stable liposome containing a large amount of the active ingredient and to provide a cosmetic composition containing the same. Moreover, this invention provides the patch using the nonwoven fabric etc. containing the said cosmetic composition.

It is another object of the present invention to provide a method for preparing a cosmetic composition containing a stable liposome containing a large amount of the active ingredient.

The inventors of the present invention first prepared liposomes of a more advanced form than the conventional liposomes, and also manufactured a cosmetic composition containing the same, and the result of experiments by attaching a certain amount to a non-woven fabric attached to the skin showed a distinct difference in the transdermal absorption of the cosmetic composition And it was found.

The cosmetic composition of the present invention is a ribosome cosmetic composition in which a skin active extract is encapsulated in liposomes stabilized using lecithin, ethanol, ester oil, propylene glycol, cholesterol or beta-sitosterol, and vegetable oil. The composition of the present invention may also contain ceramides.

Preferably, the present invention is a lecithin base prepared from 2-3 wt% of lecithin, 10-15 wt% of ethanol, 20-30 wt% of ester oil, 5-10 wt% of propylene glycol and purified water, based on the total weight of the composition. Thus, 35 to 45% by weight of the lecithin base, cucumber extracts containing amino acids, triterpenoids, vitamin C and vitamin A, lemon extracts containing sugar, vitamin C and inorganic salts, or kiwis containing vitamin C and amino acids It relates to a liposome cosmetic composition containing 15 to 40% by weight of the effective extract as an extract, and 0.1 to 0.6% by weight of cholesterol or beta-sitosterol. The liposome cosmetic composition of the present invention may further contain 2-3% by weight of ceramide.

The cosmetic composition of the present invention may further be added 0.01% by weight of butylated hydroxytoluene (BHT) and tocopherol acetate (α-Tocopherol acetate) as an antioxidant capable of improving the stability of the liposome cosmetic composition.

The present invention also relates to a process for preparing the composition.

The present invention comprises mixing 2 to 3% by weight of lecithin, 10 to 15% by weight of ethanol, 20 to 30% by weight of ester oil, 5 to 10% by weight of propylene glycol, purified water and homogenizing at 3000 rpm at 70 ° C., homogenized lecithin mixture To pressurized to 800 atm to form a lecithin base, 35 to 45% by weight of the lecithin base formed, cucumber extract including amino acids, triterpenoids, vitamin C and vitamin A, sugar, vitamin C and inorganic salts 15 to 40% by weight of an effective extract, which is a lemon extract or a kiwi extract containing vitamin C and amino acids, and purified water, and pressurized to 800 atm, and 0.1 to 0.6% by weight of cholesterol or beta-sitosterol and vegetable oil 10 To 15% by weight and again subjected to pressure treatment at 800 atm, optionally, 2-3% by weight of ceramide After the pressurization process to 800 atm, it relates to a method for producing a liposome cosmetic composition encapsulated with a large amount of the effective extract.

The liposome cosmetic composition of the present invention can be applied percutaneously in the form of a patch, such as applied directly to the skin of a person, or wetted onto a non-woven fabric, and adhered to the skin according to a conventional cosmetic application method, once or twice a day, or more Can be applied as

The liposome cosmetic composition of the present invention not only contains a large amount of the active ingredient by the liposome prepared by the method according to the present invention, but also has an effect of stably maintaining the activity of the active ingredient. When the liposome composition of the present invention is applied to the skin, it shows a remarkably excellent skin protection effect compared to the liposome composition according to the prior art.

It will be appreciated that the following examples are merely illustrative of the present invention, thereby limiting the present invention.

Example

Example 1

First, 2.5% by weight of lecithin, 13% by weight of ethanol, 25% by weight of ester oil, 7% by weight of propylene glycol, and purified water were homogenized at 70 ° C. at 3000 rpm for 10 minutes. Subsequently, the homogenized lecithin mixture was treated once with a microfludizer at 800 ° C. at 70 ° C. to form a lecithin base. Using the lecithin base formed as described above to prepare a liposome sealed with the effective extract. An effective extract that is 40% by weight of lecithin base, cucumber extract containing amino acids, triterpenoids, vitamin C and vitamin A, lemon extract containing sugar, vitamin C and mineral salts, or kiwi extract containing vitamin C and amino acids 30 3% by weight and purified water at 70 ° C. with a microfluidizer three times at 800 atm, followed by adding 0.1% by weight of cholesterol and 10% by weight of vegetable oil, and three times at 70 ° C. at 800 atm with a microfluidizer. The degree of treatment to prepare a liposome cosmetic composition.

In addition, a liposome composition was prepared by repeating the same method as described above, except that the amount of cholesterol was changed to 0.3% and 0.6% by weight, respectively, and the same amount of beta-sitosterol was used instead of cholesterol. The same procedure as described above was repeated except that the liposome composition was prepared.

In order to evaluate the stability of the prepared liposomes, the size of the liposomes was measured by using a dynamic light scattering method (DLS). The light scattering device used in the measurement is the Malvern System, a 50mw He-Ne laser with a wavelength of 633nm, PMT, Step Motor Controller, Correlator, Pump / It consists of a filter unit (Pump / Filter Unit) and temperature controller (Temperature Controller) and the light scattering data was analyzed by Malvern 4700 Software. In addition, the measurement temperature was kept constant at 25 ℃ and the measurement angle was set to 90 °. The particle size was measured three times to take an average value.

The stability measured when the liposome composition contains 0.1, 0.3, and 0.6% by weight of sterols, respectively, and the measured stability when the same amount of beta-sitosterol is substituted for cholesterol are shown in the table below.

TABLE 1

Raw material name Content (% by weight) Size change of liposomes 1 day 5 days 10 days 15th 20 days 25 days 30 days cholesterol 0.0 230 nm 300 nm 315 nm 335 nm 345 nm 360 nm 375 nm 0.1 260 nm 270 nm 280 nm 295 nm 310 nm 315 nm 330 nm 0.3 270 nm 270 nm 275 nm 295 nm 305 nm 305 nm 310 nm 0.6 320 nm 335 nm 340 nm 345 nm 350 nm 360 nm 370 nm

TABLE 2

Raw material name Content (% by weight) Size change of liposomes 1 day 5 days 10 days 15th 20 days 25 days 30 days Beta-sitosterol 0.0 240 nm 275 nm 320 nm 340 nm 345 nm 355 nm 370 nm 0.1 280 nm 300 nm 310 nm 335 nm 360 nm 390 nm 400 nm 0.3 330 nm 340 nm 360 nm 360 nm 370 nm 395 nm 400 nm 0.6 400 nm 425 nm 450 nm 450 nm 490 nm 525 nm 550 nm

Table 1 shows the particle size change of the liposome composition according to the amount of cholesterol, but the size of the liposome also increased slightly as the amount of cholesterol increased, but after 30 days did not show any change in size. Therefore, it can be seen that cholesterol affects bilayer strengthening by intercalating into the bilayer of liposomes similar to the biofilm.

Liposomes that do not contain cholesterol continue to increase in size because the particle size increases due to the aggregation of liposome particles to stabilize by decreasing the surface area.

Table 2 shows the change in the size of liposomes depending on the concentration of beta-sitosterol, a cholesterol-like structure. Beta-sitosterol also increased the size of the liposome particles and, like cholesterol, was inserted between the membranes to increase the size of the particles. However, after five days, the size of the particles continued to increase, unlike cholesterol, because the size of the particles continued to increase due to the lack of adhesion of beta-sitosterol to the membrane phospholipids in the double membrane. The size of liposomes is relatively large compared to 280 to 330 nm of cholesterol, about 280 to 550 nm, because the molecule of beta-sitosterol is larger than cholesterol.

Example 2

The physical stability of the liposomes was observed through the change in particle size over time. In order to observe the stabilization of the liposomes indirectly through the change in the amount of the active active ingredient (cucumber, lemon, or kiwi extract) with time, heat, Liposome compositions were prepared in the same manner as in Example 1 except for encapsulating ascorbic acid, which is sensitive to external environments such as light and air (oxygen) and readily decomposed to prepare liposome compositions, and observed their stability.

TABLE 3

Raw material name Content (% by weight) Change in content of ascorbic acid (% by weight), 25 ° C 5 days 10 days 15th 20 days 25 days 30 days cholesterol 0.0 70 50 45 40 30 10 0.1 82 75 72 71 69 68 0.3 82 77 74 73 73 74 0.6 85 80 76 75 75 73

TABLE 4

Raw material name Content (% by weight) Change in content of ascorbic acid (% by weight), 25 ° C 5 days 10 days 15th 20 days 25 days 30 days Beta-stosterol 0.0 70 50 46 39 29 10 0.1 81 75 72 70 71 71 0.3 82 78 75 72 72 72 0.6 84 80 76 75 74 71

Table 3 and Table 4 show the change over time of the amount of ascorbic acid encapsulated according to the concentration of cholesterol or beta-sitosterol. When comparing liposomes containing an ascorbic acid solution and an ascorbic acid solution, liposomes showed superior stability of ascorbic acid as compared to an ascorbic acid aqueous solution. This is the result of ascorbic acid is easily oxidized and decomposed in aqueous solution, liposomes as a result of the role of inhibiting oxidation and degradation by encapsulating ascorbic acid to reduce contact with foreign substances. In addition, liposomes containing cholesterol or beta-sitosterol showed less loss of ascorbic acid than liposomes containing no cholesterol or beta-sitosterol. By affecting the properties, a more stable liposome composition is formed.

As a result of the above experiment, cholesterol or beta-sitosterol than active liposomes inhibits the release, oxidation and degradation of active active ingredients (cucumber, lemon, or kiwi extract) encapsulated by strengthening the double membrane of liposomes. Lemon, or kiwi extract). In addition, when the concentration of cholesterol 0.3% by weight than beta-sitosterol, the most stable liposome composition was produced.

Example 3

In order to prepare liposomes containing 0.3 wt% of cholesterol more stably, 2.0 wt% of ceramide was added to the liposomes prepared in Example 2, and the results were obtained as shown in Tables 5 and 6.

TABLE 5

Raw material name Content (% by weight) Size change of liposomes (with time; 1-30 days) Ceramide 0.0 260 nm to 310 nm 2.0 250 nm to 260 nm

TABLE 6

Raw material name Content (% by weight) Change in content of ascorbic acid (% by weight), 25 ° C 5 days 10 days 15th 20 days 25 days 30 days Ceramide 0.0 82 77 74 73 73 74 2.0 85 80 79 79 77 78

Table 5 and Table 6 shows that ceramide stabilizes the encapsulated active ingredient by further strengthening the double membrane of liposomes.

Example 4

Liposomes containing the active ingredient (cucumber, lemon, or kiwi extract) were used in the formulation of the essence pack composition as follows.

In order to make the liposome more stable in the essence pack composition, an antioxidant was prepared by adding 0.01% by weight of butylated hydroxytoluene (BHT) and 0.2% by weight of α-Tocopherol acetate. For example, it will be described in detail as follows. Raw material names, addition amounts and preparation methods are shown in Table 7 below.

TABLE 7

Raw material name Content (% by weight) Remarks Purified water Remaining amount (to 100% by weight) A glycerin 10.0 Carboxy Vinyl Polymer 0.08 ethanol 2.0 B Emulsifier (HCO-60) 0.5 BHT 0.01 Tocopherol Acetate 0.2 antiseptic Quantity Spices Quantity Liposomal composition (cucumber, lemon, kiwi extract) 15 C

The component A was warmed to about 50 ° C., and then heated to 50 ° C. and dissolved in the component B, solubilized with a stirrer, and then the component C was added and slowly stirred to mix. The stability of the liposomes with the cosmetic composition prepared above and the cosmetic composition made of BHT and a composition other than tocopherol acetate was measured.

1) Experiment Method

The stability of the liposomes contained in the essence pack composition was measured by the color of the oxidation degree of the liposomes by the temperature change. Temperature conditions are 5 ℃, Room Temperature (RT), 37 ℃, 45 ℃, 55 ℃, constant temperature and humidity (-10 ℃ to 45 ℃, repeated twice every 24 hours).

The color was set at 10 as the standard and 1 at which the liposome was completely oxidized to brown.

2) Experiment result

TABLE 8

Color change at 55 ° C that can most likely inhibit the stability of liposomes

contents Color change over time Remarks 5 days 10 days 15th 20 days 25 days 30 days Antioxidant (BHT, Tocopherol added composition) 10 10 9 9 8 8 Antioxidants (compositions except BHT, tocopherol acetate) 10 9 9 8 8 7

Example 5

Essence pack composition 0.5 on the nonwoven fabric instead of directly immersing the essence pack composition containing the liposomes containing the active active ingredient (cucumber, lemon, or kiwi extract) prepared in Example 4 on the surface of the skin in the conventional method To 1.0% was wetted and adhered to the skin for percutaneous absorption.

The effect on the skin moisturizing and elasticity of the essence pack composition directly applied to the skin surface and the non-woven fabric soaked with the essence pack composition was measured.

1) Experiment Method

In order to compare the difference between the essence pack composition directly applied to the skin surface and the effect of soaking the essence pack composition in the nonwoven fabric, the essence pack composition was directly applied to the skin surface twice a day at the edge of the left eye of 20 people. The right eye edge was applied twice a day with a nonwoven fabric moistened with an essence pack composition. After 7 days the skin elasticity of the skin surface was measured by Corneometer CM 820 and Cortometer SEM 474. The skin moisturization measurement by the Corneometer CM 820 showed the increased moisturizing power in% compared to the direct application on the skin and the average value of 20 subjects was shown in the results. Skin elasticity measurement by cutometer SEM 474 is a measure of the depth of wrinkles, the smaller the value is the better elasticity. The elasticity value was expressed as a percentage decrease compared to the direct application on the skin, and the average value of 20 subjects is shown in the following table.

2) Experiment result

TABLE 9

Effect of Essence Pack Composition on Skin Surface Moisturizing and Elasticity

Subject Skin moisturizing effect (%) Skin elasticity effect (%) One 23 20 2 24 25 3 23 25 4 25 24 5 25 26 6 27 25 7 28 28 8 25 20 9 26 24 10 30 26 11 32 25 12 25 25 13 34 28 14 35 22 15 26 20 16 25 27 17 24 28 18 23 29 19 35 25 20 27 30

The said Example was mentioned about the method of increasing the pharmacological effect of an active ingredient by percutaneously absorbing the essence pack composition containing the stabilized liposome in a nonwoven fabric. Therefore, it can be seen that the liposome stabilization method of the present invention and the preparation of a composition having the antioxidant power of liposomes, and the liposome-added composition is wetted with a nonwoven fabric to increase the percutaneous absorption ability to bring intensive efficacy effects.

Claims (6)

Lecithin base prepared from 2-3% by weight of lecithin, 10-15% by weight of ethanol, 20-30% by weight of ester oil, 5-10% by weight of propylene glycol and purified water, based on the total weight of the composition, 45 to 40% by weight, effective extract 15 to 40 which is an amino acid, triterpenoids, cucumber extracts containing vitamin C and vitamin A, sugar extracts containing sugar, vitamin C and inorganic salts, or kiwi extracts containing vitamin C and amino acids A transdermal liposome cosmetic composition containing% by weight, and 0.1 to 0.6% by weight of cholesterol or beta-sitosterol, and 10 to 15% by weight of vegetable oil. The liposome cosmetic composition according to claim 1, further comprising 2 to 3% by weight of ceramide, based on the total weight of the composition. The liposome according to claim 1, further comprising 2-3 wt% of ceramide based on the total weight of the composition, and 0.01 to 0.05 wt% of BHT and 0.1 to 0.5 wt% of tocopherol acetate as antioxidants. Cosmetic composition. Mixing 2 to 3% by weight of lecithin, 10 to 15% by weight of ethanol, 20 to 30% by weight of ester oil, 5 to 10% by weight of propylene glycol, purified water and homogenizing at 3000 rpm at 70 ° C., homogenizing the lecithin mixture to 800 atm Pressing to form a lecithin base, 35 to 45 wt% of the lecithin base formed, cucumber extract including amino acids, triterpenoids, vitamin C and vitamin A, lemon extract including sugar, vitamin C and inorganic salts, Or 15 to 40% by weight of an effective extract, which is a kiwi extract including vitamin C and amino acids, and purified water, and pressurized to 800 atm, and 0.1 to 0.6% by weight of cholesterol or beta-sitosterol and 10 to 15% by weight of vegetable oil. Liposomal makeup encapsulated with a large amount of active extracts, including the step of adding% and pressure treatment at 800 atm again. How to prepare the compositions. 4. The method of claim 3, further comprising pressurizing to 800 atm after adding 2-3% by weight of ceramide. A transdermal nonwoven patch containing the liposome cosmetic composition of any one of claims 1 to 3.