Cosmetic composition for enhancing skin absorption, comprising lipid nanoparticle having flexible structural characteristics

A cosmetic composition with ceramide-based nanoparticles and a hexagonal structure addresses the barrier-damaging issue of chemical enhancers, achieving effective and stable skin absorption.

WO2026054338A1PCT designated stage Publication Date: 2026-03-12COSMAX INC
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Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Filing Date
2025-08-05
Publication Date
2026-03-12

AI Technical Summary

Technical Problem

Existing chemical skin absorption enhancers damage the skin barrier by altering intercellular lipid structures, leading to irritation and ineffective delivery of physiologically active substances.

Method used

A cosmetic composition comprising nanoparticles made of ceramide or its derivatives, cetyl alcohol, and a glucoside surfactant, with a hexagonal crystal structure, promotes skin absorption without damaging the skin barrier.

Benefits of technology

The composition enhances skin absorption of physiologically active substances while maintaining the skin's integrity, offering superior penetration and stability across various formulations.

✦ Generated by Eureka AI based on patent content.

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Abstract

The present invention relates to a cosmetic composition containing nanoparticles comprising ceramide or a derivative thereof, cetyl alcohol and a glucoside-based surfactant. The cosmetic composition can stably support a high amount of ceramide or a derivative thereof and exhibits excellent skin absorption. In addition, the present invention has a small particle size, and thus can be broadly applied to an emulsion formulation and to a liquid formulation such as a toner.
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Description

Lipid nanoparticle cosmetic composition for enhancing skin absorption with flexible structural properties

[0001] The present invention relates to a cosmetic composition comprising lipid nanoparticles for enhancing skin absorption having flexible structural characteristics.

[0002] The skin barrier functions to prevent the absorption of external harmful substances and to suppress the evaporation of moisture from within the skin. This skin barrier function is attributed to the intercellular lipids of the stratum corneum. The intercellular lipids of the stratum corneum are known to be roughly composed of 50% ceramides, 20-25% cholesterol, 20-25% free fatty acids, 10% cholesterol esters, 1-2% cholesterol sulfate, and a small amount of phospholipids. Furthermore, these intercellular lipid components are known to be organized in a layered structure called a lamellar structure, which is a mixture of orthorhombic and hexagonal packing. Among these, the orthorhombic structure is a densely packed structure that inhibits the transport of substances through the intercellular lipids of the stratum corneum.

[0003] Therefore, chemical skin absorption enhancers are used to promote the skin absorption of bioactive substances. However, commonly used chemical skin absorption enhancers, such as alcohol, menthol, and urea, promote the skin absorption of effective ingredients by destroying intercellular lipid components in the stratum corneum or altering lipid structures. This can damage the skin barrier and cause various irritations and irritations due to the alteration of intercellular lipid components.

[0004] Therefore, there is a need to develop cosmetics that can promote the absorption of physiologically active substances into the skin without damaging the skin barrier by mimicking the structure of the skin without chemical skin absorption promoters.

[0005] One aspect is to provide a cosmetic composition containing nanoparticles comprising ceramide or a derivative thereof, cetyl alcohol and a glucoside surfactant.

[0006] One aspect provides a cosmetic composition containing nanoparticles comprising ceramide or a derivative thereof, cetyl alcohol and a glucoside surfactant.

[0007] In one specific embodiment, the size of the nanoparticles can be 50 to 300 nm, 50 to 250 nm, 50 to 200 nm, 50 to 190 nm, 50 to 180 nm, 50 to 170 nm, 50 to 160 nm, 100 to 300 nm, 100 to 250 nm, 100 to 200 nm, 100 to 190 nm, 100 to 180 nm, 100 to 170 nm, 100 to 160 nm, 130 to 300 nm, 130 to 250 nm, 130 to 200 nm, 130 to 190 nm, 130 to 180 nm, 130 to 170 nm, or 130 to 160 nm.

[0008] Since the above cosmetic composition contains nanoparticles with small particle sizes, it can be universally applied not only to emulsion formulations but also to liquid formulations such as toners. Specifically, if the size of the particles contained in the cosmetic composition is micron-sized, it can only be applied to emulsion formulations of the emulsified type, but if the size of the particles is nano-sized, it can also be applied to liquid formulations of the solubilized type.

[0009] Since the above cosmetic composition contains nanoparticles with small particle sizes, it may have superior skin absorption compared to microparticles.

[0010] The term "emulsion type" as used herein refers to a formulation that contains both water and oil and exists in the form of an oil-in-water (O / W) or water-in-oil (W / O) formulation. The emulsion type cosmetic composition may be in the form of a cream, gel, lotion, serum, or balm, but is not limited thereto.

[0011] The term “solubilized type” as used herein refers to a formulation that does not contain oil or a small amount of oil component is transparently dissolved in water, and is a formulation that exhibits transparency because the diameter of the oil drop is smaller than the wavelength of visible light and thus does not interfere with the straightness of light without scattering or reflection. The cosmetic composition of the solubilized type may be a skin, toner, lotion, cleansing water, or essence formulation, but is not limited thereto.

[0012] In one specific embodiment, the cosmetic composition may be in a liquid or emulsion form.

[0013] In one specific example, the cosmetic composition may be of a solubilized or emulsified type.

[0014] In one specific embodiment, the nanoparticles may not contain oil.

[0015] The above nanoparticles may be formed as nanoparticles by not including oils.

[0016] In one specific example, the oil may be, but is not limited to, caprylic / capric triglyceride.

[0017] In one specific example, the cosmetic composition may have a hexagonal crystal structure.

[0018] In this specification, the term "hexagonal system" is used interchangeably with "hexagonal structure", "hexagonal shape" or "hexagonal crystal system", and can mean a crystal structure in which substances such as surfactants in an emulsion are arranged. In addition, the hexagonal system includes a sharp single peak that appears from the hexagonal system on the cross-section side in a wide-angle region. Since the hexagonal structure typically has a loose or open crystal structure, the movement of molecules is large, so that polarization occurs easily, and it has high piezoelectric properties that can generate microcurrents, and has the effect of promoting skin absorption of a physiologically active substance. Therefore, the composition can promote skin absorption (transdermal delivery) of ceramide or a derivative thereof, or a physiologically active substance.

[0019] The term "ceramide" as used herein is used interchangeably with N-acylsphingosine and may include any compound composed of sphingosine and a fatty acid. Specific examples of the ceramide may include natural ceramide, synthetic ceramide, or derivatives thereof. The ceramide may be at least one selected from the group consisting of ceramide EOP, ceramide NG, ceramide NS, ceramide NP, ceramide AS, and ceramide AP. The ceramide derivative may include a known derivative having properties similar to ceramide.

[0020] The ceramide or its derivative may be included in an amount of 0.01 to 0.5 wt% relative to the total cosmetic composition. If the content of the ceramide or its derivative is less than 0.01 wt%, the skin absorption promotion effect may not be sufficient, and if it exceeds 0.5 wt%, the ceramide or its derivative may form a gel in water or be difficult to dissolve and may precipitate.

[0021] A cosmetic composition according to one aspect may stably support a high content of ceramide or a derivative thereof by including cetyl alcohol and may exhibit excellent skin absorption. In the cosmetic composition, cetyl alcohol may enhance the skin penetration of the cosmetic composition compared to other fatty alcohols, such as cetearyl alcohol or behenyl alcohol.

[0022] The above cetyl alcohol may be included in an amount of 0.1 to 1 wt% based on the total cosmetic composition. If the content of the above cetyl alcohol is less than 0.1 wt%, the composition may become unstable, and if it exceeds 1 wt%, it may cause a sticky feeling when used.

[0023] In one specific embodiment, the glucoside surfactant may be at least one selected from the group consisting of C10-20 alkyl glucoside, Decyl Glucoside, Coco-Glucoside, Lauryl Glucoside, Caprylyl / Capryl Glucoside, Hexyl Glucoside, Cetearyl Glucoside, Arachidyl Glucoside, Ascorbyl Glucoside, and Myristyl Glucoside. In a specific specific embodiment, the glucoside surfactant may be C10-20 alkyl glucoside.

[0024] The above glucoside surfactant may be included in an amount of 0.1 to 2 wt% based on the total cosmetic composition. If the content of the glucoside surfactant is less than 0.1 wt%, the composition may become unstable, and if it exceeds 2 wt%, the feeling of use may be unfavorable.

[0025] The above cosmetic composition may further include at least one selected from the group consisting of fatty acids, cholesterol, and lecithin.

[0026] The fatty acid may be a fatty acid having 16 to 22 carbon atoms. The fatty acid may be at least one selected from the group consisting of stearic acid, palmitic acid, arachidic acid, behenic acid, palmitoleic acid, oleic acid, linoleic acid, alpha-linolenic acid, arachidonic acid, eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA). In a specific embodiment, the fatty acid may be stearic acid.

[0027] The above cosmetic composition may have the effect of promoting skin absorption of a physiologically active substance or strengthening the skin barrier.

[0028] The term “physiologically active substance” in this specification means a substance that can be delivered through the skin as an ingredient that promotes or regulates the physiological activity of the skin to improve the skin condition or help perform a specific function, and may be used interchangeably with “effective ingredient,” “effective substance,” “active ingredient,” or “effective substance.”

[0029] The above physiologically active substance may be ceramide or a derivative thereof, or niacinamide, or may be a biological compound such as a low-molecular-weight drug, protein, peptide, enzyme, DNA, RNA, siRNA, antibody or fragment thereof, vitamin, mineral, or a combination thereof.

[0030] The above nanoparticles may further contain other physiologically active substances in addition to ceramide.

[0031] The term "lamellar structure" as used herein refers to a structure in which multiple layers of thin membranes are regularly arranged in biological and chemical systems, a layered structure similar to the lipid layer of the skin. This lamellar structure is effective in strengthening the skin barrier and preventing moisture loss. The more firmly the lamellar structure is observed on the skin when a cosmetic composition is applied to the skin, the more effective the cosmetic composition is in strengthening the skin barrier.

[0032] The above cosmetic composition may include an aqueous phase and an oil phase.

[0033] In one specific example, the water-soluble component may include, but is not limited to, one or more selected from purified water and polyol.

[0034] In one specific example, the oil phase may include ceramide or a derivative thereof, cetyl alcohol, and a glucoside surfactant. The oil phase may further include at least one selected from the group consisting of fatty acids, cholesterol, and lecithin.

[0035] In one specific embodiment, the water-soluble portion and / or the oil-soluble portion may further include a physiologically active substance.

[0036] The above cosmetic composition may include at least one selected from the group consisting of a moisturizer, a skin conditioning agent, a surfactant, a chelating agent, an antioxidant, a sterilizing agent, a lubricant, a solubilizer, a pH regulator, a viscosity regulator, a metal ion sequestering agent, and a solvent.

[0037] The above moisturizer may be at least one selected from the group consisting of glycerin, dipropylene glycol, butylene glycol, sodium hyaluronate, glucose, fructose, hydrolyzed hyaluronic acid, and beta-glucan, but is not limited thereto.

[0038] The above skin conditioning agent may be at least one selected from the group consisting of sodium lactate, panthenol, allantoin, polyglyceryl-10 laurate, polyglyceryl-10 myristate, caprylyl glycol, and ethylhexylglycerin, but is not limited thereto.

[0039] The pH regulator is not limited to an acidic or basic solution that can be selected by a person skilled in the art according to the purpose and use. The pH regulator may be at least one selected from the group consisting of tromethamine, citric acid, hydrochloric acid, and ammonia, but is not limited thereto.

[0040] The viscosity modifier may be one or more selected from the group consisting of carbomer, hydroxypropyl starch phosphate, sodium magnesium silicate, hydroxyethyl cellulose, and xanthan gum, but is not limited thereto.

[0041] The above metal ion sequestering agent may be, but is not limited to, disodium EDTA.

[0042] The above solvent may be at least one selected from the group consisting of purified water, 1,2-hexanediol, and ethanol, but is not limited thereto.

[0043] The above cosmetic composition may additionally include at least one selected from the group consisting of preservatives, fragrances, and additives, but is not limited thereto.

[0044] The above preservative may be at least one selected from the group consisting of pentylene glycol, 1,2-hexanediol, caprylyl glycol, phenoxyethanol, paraben, and ethylhexylglyceryl, but is not limited thereto.

[0045] The above fragrance may be one or more selected from the group consisting of artificial fragrances, essential oils, and plant-derived extracts with strong fragrances, but is not limited thereto.

[0046] The above additive may be for improving the usability, and may be, for example, but is not limited to, silica.

[0047] The above cosmetic composition may additionally include commonly used auxiliary agents and carriers, and may include, for example, one or more selected from the group consisting of stabilizers, solubilizers, vitamins, and pigments, but is not limited thereto.

[0048]

[0049] Another aspect provides a method for preparing a cosmetic composition containing nanoparticles.

[0050] The method may include a step of preparing an oil phase by dissolving ceramide or a derivative thereof, cetyl alcohol, and a glucoside surfactant under heating; a step of preparing an aqueous phase by mixing water and a polyol; a step of heating the aqueous phase; a step of adding the oil phase to the heated aqueous phase and stirring to prepare a mixed solution of the oil phase and the aqueous phase; and a step of applying ultrasonic waves.

[0051] In the step of manufacturing the above-mentioned oil phase, the heating and dissolution may be performed at a temperature of 60 to 100°C, 60 to 90°C, 60 to 80°C, 70 to 100°C, 70 to 90°C, or 70 to 80°C.

[0052] In the step of manufacturing the above-mentioned water-based component, the heating may be performed at a temperature of 60 to 100°C, 60 to 90°C, 60 to 80°C, 70 to 100°C, 70 to 90°C, or 70 to 80°C.

[0053] In the step of treating the ultrasound, the ultrasound may be treated for 5 to 30 minutes, 5 to 25 minutes, 5 to 20 minutes, 10 to 30 minutes, 10 to 25 minutes, or 10 to 20 minutes.

[0054] Nanoparticles can be formed through the above method, and since the cosmetic composition contains nanoparticles with small particle sizes, it can be universally applied not only to emulsion formulations but also to liquid formulations such as toners, and can have superior skin absorption compared to microparticles.

[0055] The description related to the components of the above cosmetic composition is as described above, and duplicate descriptions are omitted to avoid excessive complexity of the specification.

[0056] The present invention relates to a cosmetic composition containing nanoparticles comprising ceramide or a derivative thereof, cetyl alcohol, and a glucoside surfactant. The cosmetic composition can stably support a high content of ceramide or a derivative thereof and has excellent skin absorption. Furthermore, due to its small particle size, the composition can be universally applied not only to emulsion formulations but also to liquid formulations such as toners.

[0057] Figure 1 shows the appearance of a cosmetic composition according to one specific example.

[0058] Figure 2 is an image of a cosmetic composition according to one specific example observed using a low-temperature transmission microscope.

[0059] Figure 3 is a graph measuring wide-angle X-ray scattering (WAXS) of a cosmetic composition according to one specific example.

[0060] Figure 4 is an image of the skin penetration area observed using a fluorescence microscope after applying a cosmetic composition according to one specific example onto artificial skin.

[0061] Figure 5 is a graph showing the amount of niacinamide (5a) and ceramide (5b) eluted by conducting a Franz cell dissolution test after applying a cosmetic composition according to one specific example on an artificial membrane.

[0062] Figure 6 is a graph showing small-angle X-ray scattering (SAXS) measurements taken after applying a cosmetic composition according to one specific example onto artificial skin.

[0063] Figure 7a is an image of a cross-section observed under an optical microscope after applying a cosmetic composition according to one specific example on artificial skin and then dyeing it.

[0064] Figure 7b is a graph quantifying the area of ​​the melanin portion after applying a cosmetic composition according to one specific example onto artificial skin.

[0065] Figure 8a is an image of the front surface of artificial skin observed under an optical microscope 7 days after applying a cosmetic composition according to one specific example onto artificial skin.

[0066] Figure 8b is a graph showing the L value measured using a colorimeter 7 days after applying a cosmetic composition according to one specific example onto artificial skin.

[0067] Hereinafter, preferred examples are presented to aid in understanding the present invention. However, the following examples are provided solely to facilitate a better understanding of the present invention, and the scope of the present invention is not limited by the following examples.

[0068]

[0069] Manufacturing Example 1: Manufacturing of a cosmetic composition

[0070] Cosmetic compositions of comparative examples and examples having the components and contents (weight %) shown in Table 1 below were prepared. Specifically, the oil phase was heated to about 80°C to completely melt, and then added to the water phase heated to about 80°C. After stirring for 20 minutes at 140 to 147 rpm using an azimuth mixer, ultrasonic treatment was performed for a total of 15 minutes using pulse sonication.

[0071] Ingredient Comparison Example 1 Comparison Example 2 Example 1 Water phase Unpurified water To 100 To 100 To 100 Preservative (pentylene glycol) 111 Preservative (1,2-hexanediol) 111 Polyol (glycerin) 101010 Oil phase Butyl alcohol 000.3 Behenyl alcohol 00.404140 Lecithin 0.010.010.01 C12-20 alkyl glucoside 0.50.50.5 Ceramide 0.10.10.1 Cholesterol 0.050.050.05 Stearic acid 0.10.10.1

[0072]

[0073] Experimental Example 1-1: Appearance Analysis of Cosmetic Composition of Manufacturing Example 1

[0074] The appearance of each comparative example and example cosmetic composition manufactured in Manufacturing Example 1 is shown in Fig. 1. As can be seen in Fig. 1, all cosmetic compositions were manufactured in a translucent liquid formulation, and in the case of Comparative Example 1, which did not contain fatty alcohol, it was confirmed that the components within the formulation were precipitated.

[0075]

[0076] Experimental Example 1-2: Formulation stability analysis of the cosmetic composition of Manufacturing Example 1

[0077] In order to observe the particle morphology of each cosmetic composition manufactured in Manufacturing Example 1, cryogenic transmission electron microscopy (Cryo-TEM) analysis was performed using the FEI Tecnai F20 model (Fig. 2).

[0078] As can be seen in Fig. 2, Comparative Example 1, which does not contain fatty alcohol, observed both spherical particles and rod-shaped particles, which are expected to be ceramides that were not stabilized within the formulation. On the other hand, Comparative Example 2 and Example 1, which contain fatty alcohol, were confirmed to stably contain ceramides.

[0079]

[0080] Experimental Example 1-3: Particle size analysis of the cosmetic composition of Manufacturing Example 1

[0081] To analyze the particle size of each cosmetic composition manufactured in Manufacturing Example 1, dynamic light scattering (DLS) analysis was performed. The instrument used was a Horiba Particle Size Analyzer Model SZ-100. The particle size results for the 0th and 4th weeks of manufacturing are shown in Table 2.

[0082] Comparative Example 1 Comparative Example 2 Example 1 Particle size (nm) 0 Week 144.33 135.87 146.23 4 Week 161.63 147.33 157.83 Particle size change rate (%) 11.98 64 200 18.43 45 337.93 27 087

[0083]

[0084] As can be seen in Table 2, the particle size change rate after 4 weeks of Comparative Example 1, which does not include fatty alcohol, was measured to be approximately 11.99%, the particle size change rate after 4 weeks of Comparative Example 2, which includes behenyl alcohol as the fatty alcohol, was measured to be approximately 8.43%, and the particle size change rate after 4 weeks of Example 1, which includes cetyl alcohol as the fatty alcohol, was measured to be approximately 7.93%, confirming that Example 1 was the most stable.

[0085]

[0086] Experimental Example 1-4: Analysis of molecular arrangement structure of cosmetic composition of Manufacturing Example 1

[0087] The molecular arrangement structure of each cosmetic composition manufactured in Manufacturing Example 1 was analyzed. Wide-angle X-ray scattering (WAXS) of each cosmetic composition was measured at the 4C beamline of the 3rd generation synchrotron radiation accelerator at Pohang Accelerator Laboratory (PAL) (Fig. 3). The molecular arrangement structure at the colloidal interface, such as the lateral packing of lipids, was analyzed through WAXS measurements. The X value where the peak appears was substituted into Bragg's equation (d = 2π / q) to obtain the d-spacing, which represents the size of the structure.

[0088] As can be seen in Fig. 3, in the case of Comparative Example 1, two strong peaks were observed, and the d-spacing was calculated to be 0.409 nm (▼) and 0.378 nm (▽), respectively, from which it was confirmed that it had an orthorhombic arrangement. In addition, three weak peaks were observed, and the d-spacing was calculated to be 0.421 nm (*1), 0.403 nm (*2), and 0.399 nm (*3), respectively, from which it was confirmed that it was an unstable formulation in which precipitation was expected. In the case of Comparative Example 2, two strong peaks were observed, and the d-spacing was calculated to be 0.410 nm (▼) and 0.374 nm (▽), respectively, from which it was confirmed that it had an orthorhombic arrangement. In the case of Example 1, one strong peak was observed, and the d-spacing was calculated to be 0.403 nm (▼), from which it was confirmed that it had a hexagonal arrangement, which is a more flexible arrangement than the orthorhombic arrangement. In other words, it was confirmed that Example 1 had a flexible interface structure while stably including ceramide and various components.

[0089]

[0090] Manufacturing Example 2: Manufacturing of a cosmetic composition

[0091] To analyze skin penetration, cosmetic compositions of comparative examples and examples having the components and contents (weight %) shown in Table 3 below were prepared. Specifically, the oil phase was heated to approximately 80°C until completely melted, and then added to the water phase, which had also been heated to approximately 80°C. After stirring for 20 minutes at 140-147 rpm using an Azimixer, ultrasonic treatment was performed for a total of 15 minutes using pulse sonication. Next, a fluorescent substance dissolved in ethanol was mixed.

[0092] Ingredient Comparison Example 3 Comparison Example 4 Example 2 Water phase Unpurified water To 100 To 100 To 100 Polyol (glycerin) 10 10 10 Oil phase Butyl alcohol 00 0.3 Cetearyl alcohol 00 350 Behenyl alcohol 0.40 41 400 Lecithin 0.01 0.01 0.01 C12-20 alkyl glucoside 0.5 0.5 0.5 Ceramide 0.10 10.1 Cholesterol 0.05 0.05 0.05 Stearic acid 0.10 10.1 Fluorescent FITC (in ethanol) (concentration: 10 mg / 1 mL) 0.3 0.3 0.3

[0093]

[0094] Experimental Example 2: Analysis of Skin Penetration of Cosmetic Composition of Manufacturing Example 2

[0095] The skin absorption efficacy of the cosmetic composition manufactured in Manufacturing Example 2 was analyzed using a human skin model MatTek EpiDerm EPI-200 3D skin model. Each cosmetic composition was applied onto artificial skin, fixed with formalin, and then DAPI stained and sections were prepared and observed under a fluorescence microscope (Fig. 4).

[0096] As can be seen in Fig. 4, the penetration area was observed to be the widest in Example 2 when observed under a fluorescence microscope, confirming that the skin penetration ability was the best.

[0097] In addition, as a result of calculating the relative penetration area of ​​each comparative example and embodiment in the above Fig. 4 using the imageJ program, the penetration area of ​​Comparative Example 3 was calculated to be 6116, the penetration area of ​​Comparative Example 4 was calculated to be 7273, and the penetration area of ​​Example 2 was calculated to be 9794, so that the penetration area of ​​Example 2 was calculated to be approximately 1.60 times that of Comparative Example 3 and approximately 1.34 times that of Comparative Example 4. In other words, it was confirmed that Example 2, which has a more flexible interface structure, had the best skin penetration ability.

[0098]

[0099] Manufacturing Example 3: Manufacturing of a cosmetic composition

[0100] For skin permeability analysis, comparative and exemplary cosmetic compositions were prepared in the same manner as in Manufacturing Example 1. The specific components and contents (weight %) of each cosmetic composition are as shown in Table 4 below.

[0101] Ingredient Comparison Example 5 Comparison Example 6 Example 3 Water phase Unpurified water To 100 To 100 To 100 Preservative (pentylene glycol) 111 Preservative (1,2-hexanediol) 111 Polyol (glycerin) 101010 Niacinamide 222 Oil phase Butyl alcohol 000.3 Behenyl alcohol 00.404140 Lecithin 0.010.010.01 C12-20 alkyl glucoside 0.50.50.5 Ceramide 0.10.10.1 Cholesterol 0.050.050.05 Stearic acid 0.10.10.1

[0102]

[0103] Experimental Example 3: Skin penetration rate analysis of the cosmetic composition of Preparation Example 3

[0104] The skin permeation rate of the cosmetic compositions manufactured in Manufacturing Example 3 was analyzed using a 25 mm Merck Start-M membrane, Transdermal diffusion test model. Each cosmetic composition was applied onto the artificial membrane, and a Franz cell dissolution test was performed using a 1:1 PBS:ethanol solvent. The solvent was extracted 2, 4, 8, and 24 hours after application and quantified by HPLC analysis. The data were the average of three replicates. The effective substances (niacinamide, ceramide) eluted through the artificial membrane were identified and the skin permeation rate was compared (Fig. 5).

[0105] Analysis of the content of effective ingredients in the Franz cell extract showed that both niacinamide (Fig. 5a) and ceramide (Fig. 5b) had high content of extract in Example 3 (Example 3 > Comparative Example 6 > Comparative Example 5). This confirmed that Example 3, in which the effective ingredients were stably loaded into the formulation and the interface had a flexible structure, had the highest artificial membrane permeability.

[0106]

[0107] Manufacturing Example 4: Manufacturing of a cosmetic composition

[0108] To analyze the skin barrier strengthening efficacy, comparative and exemplary cosmetic compositions were prepared in the same manner as in Manufacturing Example 1. The specific components and contents (weight %) of each cosmetic composition are as shown in Table 5 below.

[0109] Ingredient Comparison Example 7 Example 4 Water phase Unpurified water To 100 To 100 Polyol (glycerin) 1010 Oil phase Butyl alcohol 00.3 Behenyl alcohol 0.40 4140 Lecithin 0.01 0.01 C12-20 alkyl glucoside 0.5 0.5 Ceramide 0.10.1 Cholesterol 0.05 0.05 Stearic acid 0.10.1

[0110]

[0111] Experimental Example 4: Analysis of the skin barrier strengthening efficacy of the cosmetic composition of Manufacturing Example 4.

[0112] The skin barrier strengthening efficacy of the cosmetic composition manufactured in Manufacturing Example 4 was analyzed using a human skin model, MatTek EpiDerm EPI-200 3D skin model. Each cosmetic composition was applied to artificial skin and fixed with formalin to prepare a sample. Small-angle X-ray scattering (SAXS) was measured at the 4C beamline of the 3rd generation synchrotron radiation accelerator at Pohang Accelerator Laboratory (PAL) (Fig. 6). The lamellar structure of intercellular lipids known to affect the skin barrier was analyzed through SAXS measurements. The X value where the peak appears was substituted into Bragg's equation (d = 2π / q) to obtain the d-spacing (lamellar interlayer distance), which represents the size of the structure. The more solid the lamellar structure, the better the skin barrier strengthening effect.

[0113] As a result, the lamellar structure was clearly observed in the artificial skin applied with the formulation compared to the untreated sample. The lamellar structure with a 1:2:3… q ratio of approximately 13 nm was observed in all artificial skins, and in particular, the most distinct peak appeared in Example 4 with a flexible interface structure. This means that when Example 4 with a flexible interface structure was applied to the artificial skin, the intercellular lipid structure of the artificial skin had the most robust lamellar structure. This confirmed that when Example 4 with a flexible structure was applied to the artificial skin, the skin barrier strengthening effect was the most excellent.

[0114]

[0115] Manufacturing Example 5: Manufacturing of a cosmetic composition

[0116] To analyze the skin whitening (melanin migration inhibition) efficacy, comparative and exemplary cosmetic compositions were prepared in the same manner as in Manufacturing Example 1. The specific components and contents (weight %) of each cosmetic composition are as shown in Table 6 below.

[0117] Ingredient Comparison Example 8 Example 5 Water phase Unpurified water To 100 To 100 Polyol (glycerin) 10 10 Niacinamide 2 2 Oil phase Butyl alcohol 0 0.3 Behenyl alcohol 0.4 0 4 140 Lecithin 0.01 0.01 C12-20 alkyl glucoside 0.5 0.5 Ceramide 0.10.1 Cholesterol 0.05 0.05 Stearic acid 0.10.1

[0118]

[0119] Experimental Example 5: Analysis of the skin whitening efficacy of the cosmetic composition of Preparation Example 5.

[0120] The skin whitening (melanin migration inhibition) efficacy of the cosmetic composition manufactured in Manufacturing Example 5 was analyzed using the human skin model EPISKIN RHPE (Reconstructed Human Pigmented Epidermis) - Brown (Phototype Ⅵskin model). Each cosmetic composition was applied onto the artificial skin and fixed with formalin. Short-term experiments (1 day after application) and long-term experiments (7 days after application) were simultaneously conducted using the following method.

[0121] 1) Short-term experiment (cross-sectional observation, side-view)

[0122] * Visual evaluation: 1 day after application of the formulation, sections were prepared by staining with Fontana Masson and observed under an optical microscope.

[0123] * Quantitative evaluation: The area of ​​the melanin part was quantified using the ImageJ program in the cross-sectional photograph, and quantified as the total area of ​​the artificial skin / melanin area.

[0124] 2) Long-term experiment (frontal observation, top-view)

[0125] * Visual evaluation: The frontal direction of the artificial skin fixed in formalin was observed using an optical microscope 7 days after application of the formulation.

[0126] * Quantitative evaluation: L value was measured using a colorimeter and compared before and 7 days after application of the formulation to quantify, and the experiment was repeated with 3 artificial skins.

[0127]

[0128] As a result of the short-term experiment, Example 5 was observed to have the greatest inhibition of melanin migration in visual evaluation (Fig. 7a), and when the total area / melanin area value of untreated artificial skin was set to 100 in quantitative evaluation and compared, the melanin migration inhibition effect was best in the order of Example 5, Comparative Example 8, and niacinamide aqueous solution (Fig. 7b).

[0129] As a result of the long-term experiment, Example 5 was observed to be the brightest in the visual evaluation (Fig. 8a), and in the quantitative evaluation, when the L Value was quantified using a colorimeter, it was confirmed that Example 5 had the highest rate of change (Fig. 8b).

[0130] This confirmed that Example 5, which has a flexible interface structure, effectively delivers the active ingredient to the skin.

[0131]

[0132] The foregoing description of the present invention is provided for illustrative purposes only. Those skilled in the art will readily appreciate that the present invention can be readily modified into other specific forms without altering the technical spirit or essential characteristics of the present invention. Therefore, the embodiments described above should be understood as illustrative in all respects and not restrictive.

Claims

1. A cosmetic composition containing nanoparticles comprising ceramide or a derivative thereof, cetyl alcohol and a glucoside surfactant.

2. A cosmetic composition according to claim 1, wherein the ceramide derivative is any one selected from the group consisting of ceramide EOP, ceramide NG, ceramide NS, ceramide NP, ceramide AS, and ceramide AP.

3. A cosmetic composition according to claim 1, wherein the ceramide or its derivative is contained in an amount of 0.01 to 0.5 wt% based on the total cosmetic composition.

4. A cosmetic composition according to claim 1, wherein the cetyl alcohol is contained in an amount of 0.1 to 1 wt% based on the total cosmetic composition.

5. A cosmetic composition according to claim 1, wherein the glucoside surfactant is at least one selected from the group consisting of C10-20 alkyl glucoside, decyl glucoside, coco-glucoside, lauryl glucoside, caprylyl / capryl glucoside, hexyl glucoside, cetearyl glucoside, arachidyl glucoside, ascorbyl glucoside, and myristyl glucoside.

6. A cosmetic composition according to claim 1, wherein the glucoside surfactant is contained in an amount of 0.1 to 2 wt% based on the total cosmetic composition.

7. A cosmetic composition according to claim 1, wherein the nanoparticles do not contain oils.

8. A cosmetic composition according to claim 1, wherein the particle size of the nanoparticles is 50 to 300 nm.

9. A cosmetic composition according to claim 1, wherein the cosmetic composition is of a solubilized or emulsified type.

10. A cosmetic composition according to claim 1, wherein the cosmetic composition has an effect of promoting skin absorption of a physiologically active substance or strengthening a skin barrier.

Citation Information

Patent Citations

  • NANO gel emulsion having similar structure with cell membrane using self-assembled gel characteristics and osmetic composition using the same

    KR101633639B1

  • Skin care formulations

    KR1020120067351A

  • O / w nano-emulsion with high emulsion stability, preparation method thereof, and cosmetic composition comprising the same

    KR1020130051705A

  • Preparing methods nano emulsion

    KR1020150022434A

  • Structure of emulsions for enhancing the skin penetration and method of producing the same

    KR102022230B1