KR20180131876A - Stabilized ceramide complex using liposome technology and manufacturing process thereof and cosmetic composition containing the same - Google Patents

Abstract

The present invention relates to a ceramide complex using a liposome technology, a method for manufacturing the same, and a cosmetic composition containing the same. The ceramide complex comprises, based on 11.50 wt% of total weight, about 5.08 wt% of ceramide, about 0.025 wt% of cholesterol, about 0.18 wt% of free fatty acid, about 0.025 wt% of phytosphingosine, about 1 wt% of creatine, and about 5.00 wt% of lecithin, and thus effectively regenerates highly stable skin lipid barriers with no stimulus.

Description

TECHNICAL FIELD [0001] The present invention relates to a stabilized ceramide complex, a method of preparing the same, and a cosmetic composition containing the stabilized ceramide complex, a liposome technique,

The present invention relates to a stabilized ceramide complex using liposome technology, a method for producing the same, and a cosmetic composition containing the same. More particularly, the present invention relates to a cosmetic composition containing an excellent The present invention relates to a stabilized ceramide complex using liposome technology as a concentrated substance which is the same as skin lipids, a process for producing the same, and a cosmetic composition containing the same.

The skin system consists of epidermis, dermis and subcutaneous tissue. The majority of epidermis is keratinocyte and keratinocyte is divided into basal layer, visible layer, granular layer and stratum corneum according to differentiation stage. In order to protect such skin, we restore damaged stratum corneum and prevent skin damage Many studies have been conducted to promote and support epidermal growth by inducing skin lipid synthesis and epidermal differentiation to improve skin barrier function and activating the skin's natural moisture management system for skin regeneration.

In particular, the skin stratum corneum is composed of 'keratinocyte' and 'intercellular lipid' as the outer layer of the skin, and the cells generated in the basal layer are dead cells by keratinization. However, since there is a cell membrane, it blocks external harmful substances, This prevents the skin from evaporating outside, and its keratinocytes must be firmly connected to intercellular lipids so that the skin stratum corneum can act as a skin barrier. However, the skin stratum corneum, which consists of keratinocyte and intercellular lipids, is easily damaged when exposed to the dry environment and large daydreams of the seasons. Damage to the horny layer of the skin can easily evaporate the moisture of the skin and dry it. It can not easily protect the skin from external stimuli and can easily irritate the skin. In addition, the dried skin can not be removed properly and unnecessarily piled up may cause trouble.

What is needed is ceramide, cholesterol, fatty acids, amino acids and other skin lipids of the multi-lamellar structure which is the main component of the intercellular lipids constituting the stratum corneum of the skin. The physical barriers temporarily prevent moisture from leaving the skin while these multi-lamellar structures of ceramide, cholesterol, fatty acids, amino acids and other skin lipids form permanent barriers to skin moisture loss, To protect the skin against. Among them, ceramide is a very important ingredient that constitutes more than 50% of the lipid of the stratum corneum. It strengthens the skin barrier by sticking between the keratinocytes so that the moisture of the skin does not fly away.

The formation of lipid in the stratum corneum occurs naturally, but because ceramide is reduced in dry, sensitive, and aged or stressed skin, use of a ceramide component similar to skin lipids on the skin can help strengthen skin barrier, I will.

For this purpose, a technique relating to a cosmetic composition comprising ceramide components is known. However, since the ceramide component alone can not form a lamellar structure and the ceramide component is fat-soluble or insoluble, it is insoluble in water. Therefore, it can not be used in cosmetic formulations of water-based formulations containing only water such as skins, , A technique for forming an active ingredient capable of forming a lamellar structure, a technique for solubilizing other active ingredients similar to ceramide ingredients and skin lipids, and a technique for deeply delivering it to the skin are required.

Korean Registered Patent No. 10-0830153 (registered date 2008.05.09) Korean Registered Patent No. 10-1259452 (Registered on March 23, 2013)

SUMMARY OF THE INVENTION Accordingly, the present invention has been made in order to solve the problems of the prior art described above, and it is an object of the present invention to provide a composition containing ceramide complex, cholesterol, free fatty acid and phytosphingosine (also referred to collectively as lipid concentrate in the present application) Thereby forming a lamellar structure of the lamellar structure. In addition, it further contains creatine which increases cell energy conservation, thereby strengthening the cells. Further, lecithin having excellent skin affinity is further contained to form liposomes, The present invention is to provide a stabilized ceramide complex using liposome technology capable of regenerating skin lipids with high stability, irritation, and effective by coating and encapsulating water with lipids having excellent skin affinity, a method for producing the same, and a cosmetic composition containing the same.

To attain the above object, the stabilized ceramide complex using the liposome technique of the present invention includes ceramides, cholesterol, free fatty acids, phytosphingosine, creatine and lecithin.

Preferably, the stabilized ceramide composite using the liposome technology of the present invention comprises about 5.08% by weight ceramides, about 0.025% by weight of cholesterol, about 0.18% by weight of free fatty acids, about 0.025% by weight of free fatty acids, About 1% by weight of creatine, and about 5.00% by weight of lecithin.

Meanwhile, a method for preparing a stabilized ceramide composite using the liposome technique of the present invention comprises mixing ceramide, cholesterol, free fatty acids, phytosphingosine, creatine and lecithin into a manufacturing kiln and injecting it; And completely dissolving the mixture by maintaining a predetermined temperature.

Preferably, the method for preparing a stabilized ceramide composite using the liposome technique of the present invention comprises the steps of: weakening the phospholipid bilayer of the dissolved mixture; And coating the liposomal material with the bilayer-weakened mixture at a temperature of less than 40 < 0 > C.

Preferably, the process for preparing a stabilized ceramide composite using the liposome technique of the present invention comprises mixing the mixture in an amount of about 5.08% by weight of ceramide, about 0.025% by weight of cholesterol, about 0.18% by weight of free fatty acid, About 0.025% by weight of phytosphingosine, about 1% by weight of creatine and about 5.00% by weight of lecithin.

In addition, the cosmetic composition containing the stabilized ceramide composite using the liposome technique of the present invention contains about 11.5% by weight of the stabilized ceramide composite using the liposome technique, based on 100% by weight of the total cosmetic composition.

Preferably, the cosmetic composition containing the stabilized ceramide complex using the liposome technique of the present invention comprises about 5.08% by weight of ceramide, about 0.025% by weight of cholesterol, about 0.18% by weight of free fatty acid, About 54.00% of glycerin, about 15.00% of octyldodecanol, about 0.25% of 1,2-hexanediol, and about 0.25% of 1,2-hexanediol in addition to the lipid concentrate of about 0.025% by weight of tospintosine, about 1% by weight of creatine and about 5.00% About 0.25% of capryliliglycol, about 0.50% of lactylate, about 0.15% of carbomer, about 0.15% of xanthan gum, about 0.27% of phenoxyethanol, and about 0.15% of ethylhexyl glycerin.

As described above, the stabilized ceramide complex using the liposome technique according to the present invention, the preparation method thereof and the cosmetic composition containing the ceramide complex, cholesterol, free fatty acid and phytosphingosine, In addition to forming a lamellar structure of lipid concentrate, it further strengthens the cells by including creatine which increases cell energy conservation. It is coated and encapsulated with lecithin which is excellent in skin affinity to form liposome, It is possible to improve the moisturization of the skin and to restore the protective barrier function of the skin by delivering more deeply to the skin without affecting the formulation while protecting the lipid soluble ceramide composition better.

BRIEF DESCRIPTION OF THE DRAWINGS FIG. 1 is a graph comparing skin barrier recovery rates of a mixture (B) of a ceramide complex (A) and a ceramide complex to which cholesterol, free fatty acid and phytosphingosine are added.
2 is a graph showing the skin moisture content of the mixtures prepared according to Experimental Examples 1 and 2 and Comparative Examples.

Hereinafter, the present invention will be described in detail.

The stabilized ceramide complex using the liposome technique of the present invention contains about 5.08% by weight of ceramide complex, about 0.025% by weight of cholesterol, about 0.025% by weight of free fatty acid, about 0.1% by weight of fatty acid, about 0.025% by weight of Phytosphingosine, about ± 1% by weight of Creatine and about 5.00% by weight of Lecithin.

The ceramide is a constituent of intercellular lipid that acts as a sticky bond between the keratinocytes so that the moisture of the skin does not fly. Using the ceramide composition similar to the skin lipid layer helps to strengthen the skin barrier, I can do it. This type of ceramide has the same stereochemical structure as the skin and has the same stereochemical structure as the skin in the wide distribution of the fatty acid side chains. The types of ceramide include ceramide I (ceramide EOP), ceramide II (ceramide NS), ceramide III (ceramide NP) In the illustrated embodiment, the ceramide composite of the present invention comprises about 0.005% ceramide I, about 0.025% ceramide I, and about 0.025% ceramide I, By weight of ceramide III, about 5.025% by weight ceramide IIIB and about 0.025% by weight ceramide VI.

The cholesterol is a substance necessary for achieving a lamellar structure in the skin lipid layer, and may preferably be non-animal in the present invention.

The free fatty acid is a substance necessary for achieving a lamellar structure in the skin lipid layer. In the present invention, the free fatty acid may preferably be an optimal chain length thereof, such as Behenic Acid, which is a normal chain saturated fatty acid having 22 carbon atoms.

The above-mentioned phytosphingosine is a precursor of a ceramide component which is an intercellular lipid of the skin. It helps to restrain the growth of microorganisms on the skin to restore a damaged skin to a healthy state, thereby effectively reducing skin acne, flushing and inflammation symptoms, Once absorbed, it promotes the synthesis of ceramide, restoring the skin's lipid layer to prevent water evaporation, and it strengthens skin barrier function and helps skin elasticity.

A mixture of these ceramide complexes (in the illustrated embodiment, preferably ceramide I, ceramide III, ceramide IIIB and ceramide VI), cholesterol, free fatty acids, and phytosphingosine (i. E., Lipid concentrate) Unlike the single ceramide, it forms a lamellar structure, which produces a synergy effect in restoring the skin barrier. Twenty hours after application of mixture (B) with cholesterol, free fatty acid and phytosphingosine added to ceramide complex (A) and ceramide complex after wiping skin with acetone, TEWL (transepidermal water loss, loss of moisture through skin ) Were measured, and the results are shown in Fig.

The creatine is an essential component of skin and the most powerful moisturizing factor naturally present. It is a derivative of an amino acid that binds water (H ₂ O) to the skin by storing energy for storage ATP production in the form of creatine phosphate (For example, 1 g of creatine can bind 23 ml of water), thereby stimulating the activity of mitochondrial cells in the cell energy metabolism by maintaining moisture in the skin, thereby allowing ADP to be synthesized by ATP, Promotes DNA recombination.

Such creatine, as described above, plays a role in strengthening the cells through the mitochondria prior to restoring the skin's lipid layer, so that when creatine is added to the lipid concentrate, only the lipid concentrate is used There is an advantage that the loss of skin moisture can be much lower than that of the case where the skin moisture loss is reduced.

According to the EU standardized description of lecithin, lecithin is known as a mixture of polar and non-polar lipids containing at least 60% of polar lipids One lipid, "phospholipid", is the polar lipid part of lecithin.

Such lecithin is believed to have the property that the phospholipids contained therein automatically gather in the aqueous medium to form a multi-lamellar structure, such as a concentric mono-or oligo-lamellar layer, on the skin, It maintains better smoothness and suppleness and has strong moisture-binding ability to improve the moisture balance of the skin.

The lecithin containing the phospholipid therein can emulsify the lipid-soluble active ingredient such as ceramide due to the amphiphilic molecular structure having hydrophilic and lipophilic properties at the same time as described above. As a result, Emulsifiers that make the drops effective as a means of transporting the fat soluble active ingredient and can also surround the water soluble part and thus also function as liposome forming materials ideal for transporting water soluble active ingredients.

Also, the high-purity lecithin concentrate in ethanol can be prepared by dissolving or dissolving an oil-soluble, fat-soluble or poorly soluble substance (for example, ceramide, long chain Fatty acid triglycerides, etc.) can be converted into a water-soluble form and dissolved in water, thus serving as a solubilizer which makes it possible to use such a solution as an oil phase as well as in an aqueous formulation.

The liposome made of the phospholipid, which is a cell membrane constituting material, is a small vesicle in the form of a spherical capsule composed of one or several lipid layers and can not act on the skin itself. However, the active substance is coated with liposome When it is applied to the skin, it is made into a phospholipid most similar to the skin cell, and nutrients that are difficult to penetrate into the skin are carried on the liposome and penetrate deep into the skin cell where the fat absorption rate is high, such as deep in the skin, Height is the delivery system. This is demonstrated by the experimental example described below with reference to FIG. Fig. 2 shows the result of the topical application of the active substance (see Example 1) without encapsulation of the concentration of the active substance in the upper layer of the epidermis applied locally to the active substance surrounded by the liposome form (see Example 2). Further methods for producing such lecithin as a liposome will be described below.

As described above, the stabilized ceramide complex using the liposome technique of the present invention contains all the compounds required to construct a layered structure such as a multi-lamellar structure of skin lipids occurring naturally in human skin, And thus provides skin protection, prevention and regeneration function for dry, sensitive and aged skin based on multi-lamellar structure, that is, it induces skin lipid formation to function as an improved skin barrier, stabilizes the cell membrane , And energizes cellular energy metabolism to promote skin recovery through elasticity and moisturizing, and activates the skin 's natural moisture management system.

In particular, the stabilized ceramide composite using the liposome technology of the present invention can be produced by coating and treating a concentrated substance, which is the same as the above-mentioned skin lipids, with a liposome material excellent in skin affinity so that the active ingredient is delivered to a desired site during the absorption process, A signaling molecule (SM), for example, is combined with Sphingokines ^® to protect the active ingredient and to penetrate the skin much more deeply into the stratum corneum than conventional ceramides. Thus, stabilized ceramide complexes using the liposome technology of the present invention can maximize the effect of ceramides.

Next, a method for producing a stabilized ceramide composite using the liposome technique of the present invention comprises mixing the ceramides, cholesterol, free fatty acids, phytosphingosine, creatine and lecithin, preferably in the composition ratio described above, And completely dissolving the mixture while maintaining the predetermined temperature, preferably weakening the dissolved phospholipid bilayer of the mixture; And coating the liposomal material with the bilayer-weakened mixture at a temperature of less than 40 < 0 > C. It should be noted that the liposome may break when the liposome is added at a high temperature of 40 ° C or higher.

And preparing the liposome in the lecithin, the process preferably comprises dispersing high purity Unsaturated Lecithins in water or in an aqueous solution of the active ingredient; Reducing the bubble size and particle size distribution through high pressure homogenization or similar processes; Replacing the unsaturated lecithin with saturated (or hydrogenated) lecithin; And homogenizing the saturated lecithin to a high pressure above the phase transition temperature (> 55 ° C). Through these steps, particles of 100 nm to 300 nm in size can be obtained.

Examples of unsaturated lecithin include, but are not limited to, LIPOID S 20, LIPOID S 40, LIPOID S 75, and LIPOID S 100 (where LIPOID is the company name, alphabetic initial is the source And the number is the content (%) of phosphatidyl choline), and the saturated lecithin is LIPOID 2 75-3 and LIPOID S 100-3 from LIPOID, LIPOID is the name of the company, alphabetic initial is the source, and the number is the content of phosphatidylcholine (%) - the maximum iodine) can be used to make cosmetic liposomes. The quality of the liposome dispersion depends on the manufacturing method and the lecithin used.

Finally, it is preferred that the cosmetic composition containing the stabilized ceramide composite using the liposome technique of the present invention comprises about 11.5% by weight of the liposome treated ceramide composite relative to 100% of the total weight of the cosmetic composition.

And the cosmetic composition containing the stabilized ceramide complex using the liposome technique of the present invention preferably contains about 5.08% by weight of ceramide, about 0.025% by weight of cholesterol, about 0.18% by weight of free fatty acid, About 54.00% of glycerin, about 15.00% of octyldodecanol, about 0.25% of 1,2-hexanediol, and about 0.25% of 1,2-hexanediol in addition to the lipid concentrate of about 0.025% by weight of tospintosine, about 1% by weight of creatine and about 5.00% About 0.25% of capryliliglycol, about 0.50% of lactylate, about 0.15% of carbomer, about 0.15% of xanthan gum, about 0.27% of phenoxyethanol, and about 0.15% of ethylhexyl glycerin.

In the manufacture of cosmetics containing lecithin, the unsaturated lecithin is dissolved in the oil and dispersed in water. The easiest process is to disperse the unsaturated lecithin in water at room temperature and this dispersion will be easily added to the surfactant (detergent). For the emulsion (o / w or w / o) it is added directly to the water during the production of the cream or lotion. Lecithin with a low concentration of phosphatidylcholine (LIPOID S 20, LIPOID S 40) is not as well soluble in oil as high purity lecithin (LIPOID S 75, LIPOID S 100). Dissolving unsaturated lecithin in oil is often time consuming and requires high temperature conditions.

When preparing by adding saturated lecithin to the emulsion, it is possible to add lecithin to the oil phase or water phase, the simplest method being to add to the water phase at 60 ° C to 80 ° C and stir for 15 minutes to 30 minutes until the lecithin is completely dispersed . The emulsion can then be obtained by mixing and homogenizing with the oil phase.

The cosmetic composition containing the stabilized ceramide complex using the liposome technology provided by the present invention is not particularly limited in its formulation through liposome treatment and can be used for skin, mucous membrane, scalp or hair. For example, but not limited to, softeners, nutritional lotions, foundation cosmetics such as lotions, creams, packs, gels, and patches, color cosmetics such as lipsticks, makeup bases, and foundation, shampoos, rinse body cleansers, toothpastes, Detergents such as detergents, hair tonics, gels, mousse, etc., hair tonic, and hair dye. In addition, it can be widely applied to medicines such as lotion, ointment, gel, cream patch or spray, and quasi drugs.

Hereinafter, preferred embodiments of the present invention will be described in order to facilitate understanding of the present invention. However, the following examples are provided to better understand the present invention, and the scope of the present invention is not limited by the embodiments described in the present invention.

Example  1 and 2

In Example 1, ceramides, cholesterol, free fatty acids, phytosphingosine, creatine and lecithin were mixed and added to a manufacturing kiln according to the composition shown in Table 1 below, followed by completely dissolving the mixture at a predetermined temperature.

Example 2 weakened the phospholipid bilayer of the mixture completely dissolved in Example 1 and then the bilayer weakened mixture was coated with the liposomal material at a temperature of less than 40 ° C.

Comparative Example

The ceramide composite of the comparative example was prepared by the same method as in Example 1 except for the composition of Table 1 above.

Raw material name Content (% by weight) Example 1 Example 2 Comparative Example Ceramide
Complex Ceramide I 0.005 0.005 0.001 Ceramide III 0.025 0.025 0.5 Ceramide IIIB 5.025 5.025 0.5 Ceramide VI 0.025 0.025 0.5 cholesterol 0.025 0.025 0.5 Free fatty acid ± 0.18 ± 0.18 ± 3.5 Phytosphingosine 0.025 0.025 0.5 Creatine ± 1.00 ± 1.00 - lecithin - 5.00

Experimental Example  : Absorption experiment of ceramide complex by skin

(20 ° C to 22 ° C, relative humidity 40%) were prepared by preparing the materials of Example 1 (active substance without encapsulation), Example 2 (active substance surrounded by liposome) To 60%) of the subject's skin was wiped with acetone and the effect of the ceramide was measured 20 hours after uniformly applying 1.0 mg / ml of the prepared sample.

The effect of ceramides according to Experimental Example is shown in Fig. As shown in Figure 2, Example 1 increased the effect of ceramide by about 35% compared to the Comparative Example, and Example 2 also increased the effect of ceramide by about 38% when compared to Example 1 I could.

While the present invention has been particularly shown and described with reference to exemplary embodiments thereof, it is to be understood that the present invention is not limited to the disclosed exemplary embodiments, but various modifications may be made without departing from the spirit of the invention.

Claims (8)

Ceramide, cholesterol, free fatty acids, phytosphingosine, creatine and lecithin. The method according to claim 1,
Wherein the composition ratio of the ceramide composite is 5.08% by weight of ceramides, 0.025% by weight of cholesterol, 0.18% by weight of free fatty acids, 0.025% by weight of phytosphingosine, 1% by weight of creatine and 5.00% by weight of lecithin, Ceramide complex. Mixing ceramide, cholesterol, free fatty acids, phytosphingosine, creatine and lecithin into a manufacturing kiln and injecting it; And
And completely dissolving the mixture by maintaining a predetermined temperature. The method of claim 3,
Weakening the phospholipid bilayer of the dissolved mixture; And coating the bilayer with the weakened liposomal material at a temperature of less than 40 < 0 > C. The method according to claim 3 or 4,
Wherein the composition has a composition ratio of ceramide of 5.08% by weight, ceramide of 0.025% by weight, free fatty acid of 0.18% by weight, phytosphingosine of 0.025% by weight, creatine of 1% by weight and lecithin of 5.00% by weight based on the total weight of 11.50% ≪ / RTI > A cosmetic composition comprising the ceramide complex of claim 1 or 2. The method of claim 6,
Wherein the content of the ceramide composite is 11.5% by weight based on 100% by weight of the total weight of the cosmetic composition. The method of claim 7,
The cosmetic composition of the present invention is characterized in that the cosmetic composition comprises 5.08% by weight of ceramide, 0.025% by weight of cholesterol, 0.18% by weight of free fatty acid, 0.025% by weight of phytosphingosine, 1% by weight of creatine and 5.00% In addition to the concentrate, a mixture of 54.00% of glycerin, 15.00% of octyldodecanol, 0.25% of 1,2-hexanediol, 0.25% of caprylyl glycol, 0.50% of lactylate, 0.15% of carbomer, 0.15% 0.27% of ethanol, and 0.15% of ethylhexyl glycerin.

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