KR101578467B1 - Nano-concentrated capsule composition containing biochanin-a of water-soluble active material and cosmetic composition using the same - Google Patents

Abstract

The present invention relates to a concentrated nanocapsule composition comprising a hydrophilic active material and a cosmetic composition containing the same. According to the concentrated nanocapsule composition of the present invention, a hydrophilic active material (biochanin-A) separated from Dalbergiae odoriferae Lignum is combined with a thermo-sensitive polymer lipid showing thermo-sensitivity at 32 to 37°C, a skin temperature at an optimal proportion and the hydrophilic active material (biochanin-A) is concentrated and captured in a water-phase part formed between water-phase and lipid bilayers at the innermost layer of a nanocapsule having an average particle size of 40-150 nm, thereby maximizing skin permeation of the hydrophilic active material which is not readily absorbed transdermally. In addition, the transdermal absorption of the hydrophilic active material (biochanin-A) is promoted and maintenance and stability of a nanocapsule are doubled, thereby enabling application of a concentrated nanocapsule composition containing a hydrophilic active material to be expanded from basic cosmetics to make-up cosmetics in various ways.

Description

TECHNICAL FIELD The present invention relates to a nanocapsule concentrating composition containing a hydrophilic active substance of biocanin A and a cosmetic composition containing the nanocapsule concentrate composition and a cosmetic composition containing the nanocapsule concentrate composition,

The present invention relates to a nanocapsule concentrating composition containing a hydrophilic active material and a cosmetic composition containing the nanocapsule. More particularly, the present invention relates to a nanocapsule concentrating composition containing a hydrophilic active material, The nanoparticles having an average particle size of 40 to 150 nm are mixed with the polymer lipid in an optimum amount to concentrate and collect the hydrophilic active material on the water layer formed between the innermost layer of the nanoparticles and the bilayer of the lipid, It is possible to maximize skin penetration of a hydrophilic active substance which is not susceptible to percutaneous absorption, and to provide a nanocapsule concentrate composition containing the hydrophilic active substance, which contains a hydrophilic active substance capable of variously extending from basic cosmetics to color cosmetics The present invention relates to a nano-capsule concentrating composition and a cosmetic composition containing the same.

In general, nanotechnology has been attracting attention as a future technology not only in the cosmetics industry but also in all industries such as pharmaceuticals, electronics, telecommunication, machinery, etc. for about 10 years. Has been proven.

In particular, the development and development of nanotechnology in the cosmetics industry, which pursues human beauty, and in the pharmaceutical industry, which scientifically realizes the treatment of human healthy life and disease, is remarkable.

In addition, most of the nanotechnology is a technique for efficiently carrying a drug concentration as effective as a nanoscale capsule in a nanoscale capsule, and is largely divided into an emulsion and a liposome, wherein the emulsion encapsulates a lipophilic substance, It is a technology to encapsulate a substance and transfer it to the skin, and it can be applied according to each characteristic.

While conventional microemulsions are based on thermodynamic stability, nanoemulsion nanoparticles have other mechanisms that are based on long-term stability, which is kinetic.

However, in manufacturing nanoparticles such as nano emulsion, the biggest problem at present is that the manufacturing cost is much higher than the conventional emulsification technique due to the expensive equipment and the large depreciation cost consumed in the process, and the mass production is difficult, It takes a long time to manufacture, which is economically problematic.

Most of the enrichment techniques to date have been performed by extracting plant and animal components using a suitable solvent as disclosed in Korean Patent Nos. 197353 and 126444, and freezing and then concentrating the components.

However, since the preservation and stability of the extract obtained by this method shows good results, when it is put into cosmetics, it is not encapsulated, so it is difficult to secure its stability. In order to encapsulate the capsule and transfer it to the skin, There is a problem in using nanotechnologies again.

In order to solve such a problem, Korean Patent Laid-Open Publication No. 2004-84240 discloses a method of nanoparticle-encapsulating a drug called Solid Lipid Nanoparticle using various lipids used in cosmetics, lyophilizing it to concentrate and stabilize it, Techniques for improving stability have been known.

However, the above technology also has complicated processes, and the problem of uniformity in freeze-drying in mass production and high cost, especially nano-sized particles formed by breaking or aggregation of particles due to moisture evaporation during lyophilization, And the like.

Therefore, the cosmetics containing nano-encapsulated hydrophilic materials are mostly used only for the production of very expensive cosmetic products due to problems of high cost, low efficiency and limitation of drug delivery efficiency involved in application of nanotechnology. Therefore, And a technique for enhancing drug delivery efficiency is required.

Also, unlike the encapsulation of lipophilic substances, when the hydrophilic active material composed of water phase including the hydrophilic active material is formed in the innermost layer as a capsule and put into a cosmetic material composed of an excess amount of water phase, electrostatic repulsion, It is necessary to develop a nanocapsule concentrate composition in which a nanocapsule concentrate composition that captures a metastable hydrophilic active material so that a capsule size is increased or destroyed or a hydrophilic active material is desorbed by the three dynamics of the hysteresis effect and hydration effect do.

Accordingly, the present inventors have made efforts to solve the problems of the prior art. As a result, the present inventors have found that a hydrophilic active material isolated from a strong tangle is blended with a temperature sensitive polymer lipid exhibiting temperature sensitivity at a skin temperature of 32 to 37 캜, The present invention relates to a nanocapsule concentrating composition which is capable of securing transparency and metastability through the nanocapsule concentrating composition and promoting transepidermal absorption of drugs of a hydrophilic active material to confirm skin penetration effect, Completed.

It is an object of the present invention to provide a nanocapsule concentrate composition containing an optimal amount of a hydrophilic active substance and a thermosensitive polymer lipid.

Another object of the present invention is to provide a cosmetic composition using the nanocapsule concentrating composition.

In order to achieve the above object, the present invention provides a hydrophilic active material part containing a hydrophilic active material represented by the following formula

And a lipid thickening part comprising a thermosensitive polymer lipid exhibiting temperature sensitivity at 32 to 37 캜 represented by the following formula (2).

Formula 1

(2)

Wherein R is selected from the group consisting of ceramides, lecithin, phosphatidylcholine, phytosphingosine and fatty acids, and both ends may be the same or different, l is 92 to 102, m is 60 to 70, n Lt; / RTI >

In the nanocapsule concentrate composition of the present invention, the hydrophilic active substance represented by the above-mentioned formula (1) is contained in an amount of 0.01 to 0.5% by weight.

In addition, the nanocapsule concentrate composition contains a lipid concentrate containing a thermosensitive polymer lipid exhibiting temperature sensitivity at 32 to 37 ° C, represented by the following formula (2), wherein the lipid thickener is prepared by adding 4.0 to 25.0% 0.5 to 2.0% by weight of a hydrophilic polymer lipid, 1.0 to 8.0% by weight of a phospholipid, 0.1 to 1.5% by weight of a ceramide, 0.1 to 1.5% by weight of a cholesterol, 0.05 to 1.0% by weight of a fatty acid and 0.01 to 0.5% by weight of a lipophilic antioxidant.

In the nanocapsule concentrate composition of the present invention, the hydrophilic active material represented by the above formula (1) is concentrated and collected in an aqueous phase formed between the innermost layer of the nanocapsules and the lipid bilayer having an average particle size of 40 to 150 nm.

The present invention provides a cosmetic composition comprising the above-mentioned nanocapsule concentrate composition or a diluent composition containing 2 to 10% by weight of the nanocapsule concentrate composition.

Preferably, the concentrated composition and the diluted composition have no particle size change even after 3 months at 45 deg. C, and their transparency and properties are maintained. Therefore, metastability is confirmed without accumulation of particles even at high temperature and long storage time, After the lapse of 12 hours at the temperature corresponding to the body temperature at the time of application of the diluted composition, at least 90% of the hydrophilic active substance represented by the formula (1) is eluted.

The present invention provides a nanocapsule concentrate composition in which a hydrophilic active substance isolated from a strong tangy incense is mixed with an optimal content of a thermosensitive polymer lipid exhibiting temperature sensitivity at a skin temperature of 32 to 37 ° C to concentrate and collect the hydrophilic active substance can do.

Wherein the nanocapsule concentrate composition has a uniform spherical shape and has a multilayered liposome structure and has a mean particle size of 40 to 150 nm, and the hydrophilic active material is contained in the water phase formed between the water phase and the lipid bilayer of the innermost layer of the nanocapsule, , The nanocapsule concentrate composition can be applied to a cosmetic composition composed mostly of water.

In addition, the nanocapsule concentrate composition of the present invention promotes transdermal absorption of a hydrophilic active substance which is insufficient in transdermal absorption into the skin, thereby maximizing penetration of the skin, thereby doubling the efficacy of the hydrophilic active substance have.

1 is a schematic view of a nanocapsule stabilized in a nanocapsule concentrate composition containing a hydrophilic active material of the present invention,
2 is an actual photograph of a nanocapsule concentrated composition (left side) containing a hydrophilic active material (biocanin A component) of Example 2 of the present invention and a sample 2 (right side) diluted with water,
FIG. 3 shows the results of the particle size analyzer between the nanocapsule concentrate composition containing the hydrophilic active material prepared according to the present invention and the diluent composition prepared therefrom,
FIG. 4 is a photograph showing the results of the dilution composition obtained from the nanocapsule concentrate composition containing the hydrophilic active material (the biocanin A component) prepared in Example 1 and Example 2 according to the present invention, The results of the particle size analysis,
Figure 5 The dilution composition obtained from the nanocapsule concentrate composition containing the hydrophilic active material (the biocanin A component) prepared in Comparative Example 5 according to the present invention exhibited a change in particle size immediately after preparation and after 1 week at high temperature (45 ° C) The results of the observed particle size analysis,
FIG. 6 shows the results of measurement of the elution amount of the hydrophilic active material in the nanocapsule concentrate composition containing the hydrophilic active material of the present invention.

Hereinafter, the present invention will be described in detail.

The present invention relates to a hydrophilic active material part containing a hydrophilic active material represented by the following general formula (1)

And a lipid thickening part comprising a thermosensitive polymer lipid exhibiting temperature sensitivity at 32 to 37 캜 represented by the following formula (2).

Formula 1

(2)

Wherein R is selected from the group consisting of ceramides, lecithin, phosphatidylcholine, phytosphingosine and fatty acids, and both ends may be the same or different, l is 92 to 102, m is 60 to 70, n Lt; / RTI >

The nanocapsule concentrate composition of the present invention will be described in detail by composition.

(a) a hydrophilic active material part

The hydrophilic active material portion contained in the nanocapsule concentrate composition of the present invention is a hydrophilic active material and is a 5,7-dihydroxy-3- (4-methoxyphenyl) -chroman 4-one compound, and the compound is hereinafter referred to as a biocanin A component.

Formula 1

The above-mentioned biocanin A component is separated from the core material of the root portion of Dalbergia odorifera (Acronychia pedunculata), and the above-mentioned toughness fragrance helps the ki, stops the bleeding, has analgesic effect Bleeding, bruising, swelling, and wind (风濕) due to the back and legs are used as medicines to treat sick symptoms.

In the nano-capsule concentrate composition of the present invention, the hydrophilic active material (biocanin A component) represented by Formula 1 is preferably contained in an amount of 0.01 to 0.5% by weight, and when the content is less than 0.01% by weight, , And when it is more than 0.5% by weight, the content of the hydrophilic active material (biocanin A component) is high and precipitation occurs.

In the aqueous phase of the hydrophilic active substance part, sodium metabisulfite, benzophenone-2, benzophenone-4, benzophenone-9 and a mixture of two or more thereof are contained as hydrophilic antioxidants in order to prevent oxidation.

(b) a lipid concentration unit

The lipid thickening part of the present invention contains a thermosensitive lipid-conjugated pluronic represented by the following formula (2).

Formula 1

Wherein R is selected from the group consisting of ceramides, lecithin, phosphatidylcholine, phytosphingosine and fatty acids, and both ends may be the same or different, l is 92 to 102, m is 60 to 70, n is 95 to 105.)

More specifically, in the lipid thickening part of the present invention, the content of the thermosensitive polymer lipid is in the range of 0.5 to 2.0 wt%, the phospholipid is in the range of 1.0 to 8.0 wt%, the ceramide is in the range of 0.1 to 1.5 wt%, the cholesterol is in the range of 0.1 to 1.5 wt% %, 0.05 to 1.0 wt% of fatty acid and 0.01 to 0.5 wt% of lipophilic antioxidant.

In an embodiment of the present invention, the thermosensitive polymer lipid in which both ends are substituted with ceramides is described as a preferred example, but may be substituted with the substituents exemplified above.

Lipids such as ceramide, lecithin, phosphatidylcolin and phytosphingosine, which are bonded to the ends of the thermosensitive polymer, are easily adsorbed due to a structure similar to that of skin phospholipids, The phenomenon is maximized and the temperature sensitive polymer lipid exhibiting temperature sensitivity at 32 to 37 DEG C is condensed on the nanoparticle wall at the skin temperature to increase the pressure, thereby increasing the penetrating phenomenon and increasing the hydrophilic active material (Biocanin A Component) in the skin.

That is, by containing the thermosensitive polymer lipid in the lipid thickening part of the present invention, it is possible to maximize the penetration of the hydrophilic active substance which is insufficient in percutaneous absorption into the skin, thereby promoting transepidermal absorption, Double the efficacy. Furthermore, the maintenance and stability of the concentrated capsules are doubled, so that a desired amount of the cosmetic composition can be sufficiently injected into various cosmetic compositions.

The preferred content of the lipid-conjugated pluronic contained in the lipid thickening part of the present invention is 0.5 to 2.0 wt% based on the total composition weight. When the content is less than 0.5 wt%, the temperature-sensitive polymeric lipid , Which is not preferable because it does not contribute to the percutaneous absorption of the drug. When the amount exceeds 2.0% by weight, there is a problem in stability at high temperature.

The phospholipid of the lipid-enriched part of the present invention is a component that basically has a multilayer liposome structure in the hydrophilic active material in the water phase and encapsulates the water phase between the innermost layer of the capsule and the multiple layers of lipid bilayers, Phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, and phosphatidylinositol may be used depending on the type of each functional group in the above two types of phospholipids. For example, phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, , Phosphatidylserine, and mixtures of two or more thereof, and is contained in an amount of 1.0 to 8.0% by weight. When the content of the phospholipid is less than 1.0% by weight, the effect of encapsulating the hydrophilic active material is insignificant. When the content of the phospholipid exceeds 8.0% by weight, dissolution of the phospholipid itself is very difficult, And it is impossible to obtain a nano-size even after the treatment.

0.1 to 1.5% by weight of ceramides contained in the lipid thickening part of the present invention, 0.1 to 1.5% by weight of cholesterol and 0.05 to 1.0% by weight of fatty acids are contained. If the content of each ingredient is below the indicated content, The role of glue filling up the phospholipid is insignificant and it does not help the percutaneous absorption of the drug because it loses similarity with the skin composition itself. On the other hand, when the content of each composition is exceeded, it is impossible to dissolve the composition substantially, and there is a problem that it is desorbed into its high crystallinity.

As the ceramide and cholesterol used in the present invention, materials conventionally used in the art can be used. At least one fatty acid selected from the group consisting of stearic acid, palmitic acid, oleic acid, linoleic acid and linoleic acid is used .

As a component contained in the lipid thickening part of the present invention, the lipophilic antioxidant is mostly composed of an aqueous phase component, but when some hydrophilic active substances are stabilized in water phase in which multiple layers of lipid are formed between the middle layers, oxidation of the hydrophilic active substances .

Thus, butylated hydroxytoluene, benzophenone-3, octyltriazone, octylmethoxycinnamate and mixtures of two or more thereof are preferably used. At this time, the preferred content of the lipophilic antioxidant is 0.01 to 0.5% by weight.

The solvent used in the lipid thickening part of the present invention is a solvent having a hydroxyl group (-OH) in order to completely dissolve poorly water-soluble lipids in most of the water and increase its efficiency.

Preferred examples include ethanol, 1,3-butylene glycol, propylene glycol, glycerin, 1,2-pentanediol, D-panthenol, dipropylene glycol, and mixtures of two or more thereof, which are conventionally used in the art , And it is preferable to use a use amount generally known according to the content of the lipids including the phospholipid.

The nanocapsule concentrate composition containing the hydrophilic active substance is completed by using water in the total composition except for (a) the hydrophilic active material portion and (b) the rest of the content except for the content of the lipid concentrate portion.

The nanocapsule concentrate composition of the present invention is characterized in that, in addition to the phospholipid used for maximizing the capsule wall wall reinforcement and transdermal absorption having similarity to the composition of the skin, a thermosensitive polymer lipid is used and an optimal blending ratio between these components is 10 times or more The concentration of the hydrophilic active substance is stabilized in a nano-sized capsule of 40 to 150 nm. The nanocapsule concentrate composition containing such a hydrophilic active substance promotes the percutaneous absorption of the hydrophilic active substance and doubles the maintenance and stability of the concentrated capsules so that a desired amount can be sufficiently injected into various kinds of cosmetic compositions.

FIG. 1 is a schematic view of a nanocapsule stabilized in a nanocapsule concentrate composition containing a hydrophilic active material according to the present invention, wherein a hydrophilic active material having a concentration of 10 times or more is dispersed in nanocapsules of 40 to 150 nm As the particles are collected and concentrated, the hydrophilic active material is encapsulated in a nano-sized concentrate in the water phase formed between the innermost layer and the multilayered bilayer. In accordance with an embodiment of the present invention, the biocanin A component as a hydrophilic active substance is concentrated to form a liposome form having an average particle size of 40 to 150 nm.

Here, when the nanocapsule concentrate composition of the present invention captures the hydrophilic active material, it is possible to obtain a composition containing a hydrophilic active material (a component of the biocanin A) when used as a base composition of a certain weight in various kinds of cosmetics, Similar structure In particular, lipid (ceramide, lecithin, phosphatidylcholine , phytosphingosine ) bound to both terminal ends of thermosensitive polymer lipid is easily adsorbed due to structure similar to skin phospholipid when applied to skin, thereby maximizing wetting phenomenon And the temperature sensitive polymer is condensed at the skin temperature of 32 to 37 DEG C in the wall of the nanoparticle to increase the pressure, thereby enhancing the penetrating phenomenon and improving the penetration efficiency of the hydrophilic active material (drug).

Hereinafter, a method for producing a nanocapsule concentrate composition in which a hydrophilic active material (biocanin A component) is captured will be described. More specifically,

(a) 0.5 to 2.0 wt% of thermosensitive lipid-conjugated pluronic, 1.0 to 8.0 wt% of phospholipid, 0.1 to 1.5 wt% of ceramide, 0.1 to 1.5 wt% of cholesterol, 0.05 to 1.0% by weight of fatty acid and 0.01 to 0.5% by weight of lipophilic antioxidant at 55 to 75 占 폚 to prepare a lipid concentrate;

(b) 0.4 to 20.0% by weight of a hydrophilic active substance (a component of the biocanin A) is dissolved in a predetermined amount of water by heating the hydrophilic antioxidant at a temperature of 35 to 55 占 폚 to prepare a hydrophilic active material portion;

(c) adding a hydrophilic active material of (b) and water to the lipid thickening part of (a) and mixing to form a first concentrated phase that bulk-homogenizes the hydrophilic active material;

(d) stirring the first concentrated phase of (c) at a temperature of 40 to 75 ° C for 30 minutes to 2 hours to hydrate the first concentrated phase;

(e) treating the hydrated first concentrated phase of (d) at a temperature of 40 to 75 DEG C and a pressure of 700 to 1,500 bar to form nanocapsule particles having a particle size of 40 to 150 nm, Forming a second nano-enriched phase containing the material; And

(f) cooling the second concentrate to 25-40 < 0 > C.

In the step (a), dissolving the lipid thickener in the temperature range of 55 to 75 ° C is an easy temperature range for sufficiently dissolving each of the thermosensitive polymer lipids and lipids, and the step (b) The hydrophilic active material part is dissolved by warming in the temperature range of 35 to 55 캜 for safety of the active material.

Thereafter, in step (c), the hydrophilic active material is added to the lipid thickening part and stirred with a conventional agitator at a rotation speed of 1,000 to 2,000 rpm to homogeneously mix the hydrophilic active material And stirred at a rotation speed of 1,000 to 2,000 rpm again to uniformly mix them, thereby forming the first nano-enriched phase within a predetermined time with only simple agitation.

The step (d) comprises hydration of the first concentrate, wherein the phospholipid and the thermosensitive polymer lipid, which form the basis of the liposome structure having a plurality of lipid bilayers mainly composed of particle walls in the aqueous phase, To maximize its efficiency and to provide a nonuniform composition resulting from the concentration gradient of phospholipids and intercellular components at the interface through the most regular interfacial orientation with the lipids of the lipid enriched portion It is an important process to not have.

(d) is preferably stirred for 30 minutes to 2 hours. If the reaction is carried out at a time of less than 30 minutes, hydration is not sufficiently carried out, resulting in a concentration gradient at the interface and poor long-term stability. On the other hand, If it exceeds 2 hours, there is a disadvantage that the hydrophilicity of the phospholipid is promoted by promoting the hydrolysis of the phospholipid in the water.

In the manufacturing method of the present invention, the second concentrated phase forming step (e) has a nano size of 40-150 nm in the hydrated first concentrated phase and maximizes the encapsulation efficiency of the hydrophilic active material by maximizing the inner surface area .

(e), the treatment temperature is preferably 40 to 75 ° C. If the temperature is lower than 40 ° C., the solubilization temperature of the ceramide, cholesterol, and fatty acid including the phospholipid itself is lower than that of the high- If the temperature is higher than 75 ° C, the hydrophilic active material itself may be broken due to the high temperature in addition to the energy applied in the high pressure emulsifier, and gelation may occur due to high energy and high lipid concentration. So that the desired viscosity can not be obtained.

In addition, the treatment pressure in step (e) is preferably an important factor for the energy applied to prepare the nanocapsule concentrate composition, and is performed at 700 to 1,500 bar. If the processing pressure is less than 700 bar, it is difficult to form homogeneous nano-concentrated particles at 30-150 nm. If the pressure exceeds 1,500 bar, the temperature rises sharply due to friction due to too strong force, And cholesterol, ceramide, and fatty acids are eliminated, resulting in decreased stability.

The high-pressure type emulsifier used in step (e) applies a very high pressure to the pressurizing pump, passes it through an interaction chamber made of a diamond having a minute size such as a pipe to change the high pressure to high speed, Is a device that can make nano-sized particles using a vacuum phenomenon called a cavitation and a crushing effect due to collision. The force for crushing particles is much stronger than that of a conventional mixer.

Thereafter, the method of producing a nanocapsule concentrate composition of the present invention comprises cooling the second concentrated phase formed in the step to 25 to 40 ° C through step (f), thereby stabilizing the second concentrated phase.

The nanocapsule concentrate composition of the present invention can be prepared by concentrating a hydrophilic active material into a stabilized nanoscale capsule using specific components having a skin-like structure and a thermosensitive polymer lipid, It is possible to solve the problem of increasing the drug delivery efficiency and cost, which is the biggest problem in applying the technology.

In addition, the method of producing a nanocapsule concentrate composition by capturing a hydrophilic active material of the present invention can easily obtain nano-capsules of a hydrophilic active material having a skin-like composition and structure by simple stirring, Provide feeling.

Furthermore, the present invention relates to a nanocapsule concentrate composition containing the above-mentioned hydrophilic active substance or

And a diluent composition containing 2 to 10% by weight of the nanocapsule concentrate composition.

More specifically, the nanocapsule concentrate composition of the present invention employs a thermosensitive polymer lipid to maximize the penetration of the hydrophilic active substance into the skin. In particular, the amount of the hydrophilic active material to be used due to the concentration effect can be easily controlled by concentrating and stabilizing the hydrophilic active material at a concentration of about 10 times or more the effective amount in the nanocapsules of 40 to 150 nm, Is maintained.

Therefore, the amount of the hydrophilic active material can be easily adjusted by simple stirring to the cosmetic composition to which the nanocapsule concentrate composition is applied, and at the same time, a desired amount can be sufficiently supplied.

2 is a photograph of a sample 2 (right side) of a diluted nanocapsule composition (left side) containing a hydrophilic active material (biocanin A component) of Example 2 of the present invention and a diluted composition diluted with water, In all cases, transparency is confirmed, and this transparency is maintained even after three months.

On the other hand, when the content of the hydrophilic active substance (biocanin A component) is more than 0.5% by weight in the preparation of the nanocapsule concentrate composition of the present invention, transparency becomes turbid or milky white with time .

FIG. 3 is a graph showing the results of measurement of the particle size analyzer between the nanocapsule concentrate composition containing the hydrophilic active material prepared according to the present invention and the diluent composition prepared therefrom, Meta-stability.

Fig. 4 also shows that the diluted composition obtained from the nanocapsule concentrate composition containing the hydrophilic active material (the biocanin A component) prepared in Example 1 and Example 2 according to the present invention was prepared immediately after preparation and at a high temperature And particle size changes after 3 months. As a result, even after three months at 45 캜, there was no change in particle size, and transparency and retention of properties were confirmed. Thus, it can be confirmed that even when stored at high temperature and for a long time, it is kept very stable without intergranular agglomeration.

5 , The dilution composition obtained from the nanocapsule concentrate composition containing the hydrophilic active material (the biocanin A component) prepared in Comparative Example 5 according to the present invention exhibited a change in particle size immediately after preparation and after 1 week at high temperature (45 ° C) As a result of the observed particle size analysis, a poor stability result can be confirmed.

Therefore, the nanocapsule concentrate composition containing the hydrophilic active material of the present invention or its diluent composition has excellent metastability such as particle size and transparency of the nanocapsule, and thus can be applied to a cosmetic composition composed mostly of water, It is easy to apply to conventional cosmetic compositions, so that it can be easily applied not only to basic cosmetics but also to color cosmetics.

FIG. 6 is a graph showing the results of measurement of the elution amount of the hydrophilic active material in the nanocapsule concentrate composition containing the hydrophilic active material of the present invention, showing that 90% or more of the hydrophilic active material (Biocanin A Component) can be confirmed.

Accordingly, the cosmetic composition containing the nanocapsule concentrate composition can promote the transepidermal absorption of the hydrophilic active material during skin transfer, thereby doubling the effectiveness of the hydrophilic active material.

Hereinafter, the present invention will be described in more detail with reference to Examples.

The present invention is intended to more specifically illustrate the present invention, and the scope of the present invention is not limited to these embodiments.

< Example  1>

Nanocapsule concentrate compositions containing biocanin A were prepared according to the compositions shown in Table 1 below. More specifically, the lipid thickening portion was added to the dissolution tank in the content shown in Table 1, heated to 70 DEG C to dissolve, and the portion of the hydrophilic active material was added to the dissolution tank in the content shown in Table 1 and heated to 45 DEG C to dissolve Respectively. The dissolution tank containing the prepared lipid concentrate was stirred at a rate of 1,500 rpm for 5 minutes while being maintained at 50 ° C, and a hydrophilic active substance was added thereto. Using a stirrer, the mixture was stirred at a speed of 1,500 rpm For 5 minutes to homogenize biocanin A to prepare a first concentrated phase.

While maintaining the first concentrated phase at 50 ° C, the first concentrated phase was sufficiently hydrated by stirring at 500 rpm for 1 hour using an agitator. The hydrated first concentrated phase was added to a high-pressure emulsifier (Microfluidics, Model: M-110F) at 50 ° C and treated twice at a pressure of 9,000 bar to remove the biocanin A component from the innermost layer And the second concentrated phase was formed by enrichment encapsulation in the nano-size while being located in the water phase formed between the water phase and the lipid bilayer.

Thereafter, the mixture was cooled and stabilized with stirring at a speed of 500 rpm in a stirrer at 28 ° C with gentle stirring to prepare a nanocapsule concentrate composition containing the biocanin A component.

< Example  2 to 3>

A nanocapsule concentrate composition containing a biocanin A component was prepared in the same manner as in Example 1, except that a lipid concentrate and a hydrophilic active material were prepared according to the composition shown in Table 1 below.

< Comparative Example  1 to 3>

A nanocapsule concentrate composition containing a biocanin A component was prepared in the same manner as in Example 1, except that a lipid thickener and a hydrophilic active material were prepared according to the composition shown in Table 1 below.

Experimental Example  1> Evaluation of Properties and Transparency

The nanocapsule concentrate composition prepared in Examples 1 to 3 containing the biocanin A component was photographed by a conventional optical microscope and as a result, it was impossible to observe it because of its extremely fine size.

Thus, the concentrated compositions of Comparative Examples 1 to 3, which were prepared by including 0.7% by weight, 1.0% by weight and 1.5% by weight of the biocanin A component in the concentrated compositions of Examples 1 to 3 and the compositions of the above- 2% by weight was added to the weight%, and the mixture was diluted to prepare Sample 1 to Sample 6.

As shown in Table 2 below, the morphology and morphology of the nanoparticles of the compositions were observed using a freezing electron microscope. As a result, in the concentrated compositions of Examples 1 to 3, the structure of a very uniform spherical liposome was confirmed , And it was confirmed that the average particle size was formed in a distribution of 40 to 150 nm.

FIG. 2 is a photograph of the nanocapsule concentrate composition (left side) containing 0.025% by weight of the biocanin component A of Example 2 and the sample 2 (right side) diluted with water. In both cases, transparency was maintained.

These results are also confirmed in the case of Samples 1 to 3 of Table 2. The transparency tends to be lowered when the samples 1 to 3 are transparent and the sample 4 becomes translucent. Samples 5 to 6 are translucent and milky white The change was confirmed

These results are also confirmed in the case of Samples 1 to 3 of Table 2. In the case of Samples 4 to 6, the transparency is maintained at the time of 3 months, As shown in Fig.

From the above, as shown in Fig. 1, in the case of the nanocapsule concentrate composition containing the biocanin A component prepared in Examples 1 to 3, the biocanin A component as the hydrophilic active substance was concentrated to have an average particle size of 40 Shaped nanoparticles stabilized between the innermost layer and the multilayer structure of the particles having a particle diameter of 150 nm to 150 nm were formed and the particle size was examined by a freezing electron microscope. As a result, the average particle sizes of Examples 1 to 3 were 43, 51, It was confirmed that very uniform nanoparticles were formed.

< Experimental Example  2> Stability evaluation

The diluted samples (B, D) from the concentrated compositions (A, C) prepared in Examples 1 and 2 and the respective concentrated compositions were applied to a particle size analyzer (NANOPHOX ).

FIG. 3 is a graph showing the result of measurement of the particle size analyzer between the concentrated composition containing the biocanin A component prepared in the present invention and the diluent composition obtained therefrom. As a result of the analysis of the particle size in the concentrated composition and the diluted composition, -stability).

Figure 4 shows that the nanocapsule concentrate composition containing the biocanin A component prepared from Example 1 (A) and Example 2 (B) according to the present invention was stirred in an excess of water and then stirred at high temperature (45 캜) for 3 As a result of particle size analysis after observation of the particle size after the passage of time, there was no change in the particle size even after observation for 3 months at 45 ° C. and by confirming the transparency and keeping the property, And it was confirmed that it remained very stable.

On the other hand, when the nanocapsule concentrate composition of Comparative Example 1 containing 0.7% by weight of the biocanin A component was applied to 98% by weight of water, the particles were completely diluted and poor in metastability.

Fig. 5 is a graph showing the results of measurement of a diluent composition obtained from a nanocapsule concentrate composition containing a hydrophilic active material (a biocanin A component) prepared from Comparative Example 5 containing 1.0% by weight of a biocanin A component, As a result of particle size analysis after one week of the change in particle size, the nanocapsule-concentrated composition of Comparative Example 5 showed poor stability due to overcharging at 2 weeks at room temperature and 2 months at room temperature It looked.

In the case of the sample 6 in which the nanocapsule concentrate composition of Comparative Example 6 containing 1.5% by weight of the biocanin A component was diluted with water, the content of the biocanin A component was high and precipitation occurred.

As shown in the above Table 2, in order to actually apply the nanocapsule concentrate composition of the biocanin A component to the cosmetic composition in the continuous phase, the particle size of the nanocapsule concentrate composition itself, its transparency and Proper metastability to the dynamics such as electrostatic repulsion, steric hindrance, hydration effect is very important.

On the other hand, the concentrated compositions of Comparative Examples 1 to 3 had turbidity in the nanocapsule-concentrated composition itself immediately after preparation, the particle size was not formed in the nano-scale, or the nanocapsule could not secure its metastability even once it was formed, In addition, as shown in Table 2, the desorption phenomenon of the hydrophilic active substances concentrated in the dispersion in water can easily occur, and the liposome particles encapsulating the hydrophilic substance in the nanoscale can not be obtained because the formulation itself is separated, none.

< Experimental Example  3> Biocanin  A component Percutaneous absorption  evaluation

The formulation of the nanocapsule concentrate compositions of Examples 1 to 3 and the nanocapsule concentrate composition of Comparative Example 2, which showed excellent meta-stability, was diluted with an excess amount of water and the samples 1 to 3 and 5 of Table 2 were applied to the skin , And the percutaneous absorption amount of the biocanin A component which is the hydrophilic active substance (drug) used was measured.

The percutaneous absorption experiment showing the skin penetration effect of the biocanin A component was carried out by adding 0.25 g of the samples 1 to 3 in the same amount to a dissolution tester (ERWEKA DT800 Dissolution Tester, Germany) (Enhancer cell, ERWEKA, Germany) equipped with a 65-year-old man's back plate (Hans Biomed) was charged with 500 ml of a buffer solution of about pH 7.0 with sodium chloride and the temperature was adjusted to 37 Deg.] C, and the elution amount of each biocanin A component was periodically measured for 12 hours using high performance liquid chromatography (HPLC, Shimadzu, LC-10VP, Japan).

Figure 6 is a elution Measurement of specific non-Oka A component in a nanocapsule concentrate composition containing non-A non-Oka components of the present invention, in the case of samples 1 to 3 after a lapse of 12 hours, for the initial injected amount, respectively, 99.9% , 99%, and 94.5% of the biocanin A component. From the above results, it was confirmed that the elution amount of the active material generally obtained is very excellent. On the other hand, in the case of sample 5, as a result of percutaneous absorption test, biocanin A did not permeate due to precipitation and remained on the surface, showing only 32% of percutaneous absorption.

As described above, the present invention is characterized in that a hydrophilic active material (Biocanin A) isolated from a strong-smelling fragrance is blended at an optimum content with a thermosensitive polymer lipid exhibiting temperature sensitivity at a skin temperature of 32 to 37 DEG C, To provide a nanocapsule concentrate composition wherein the substance (biocanin A) is concentrated and captured.

The nanocapsule concentrate composition has a uniform spherical shape and has a multilayered liposome structure and has an average particle size of 40 to 150 nm. The nanocapsule has a hydrophilic active material Nin A) is concentrated and collected, the transdermal absorption of the hydrophilic active substance (biocanin A) is promoted, thereby maximizing the penetration of the skin, thereby doubling the efficacy of the hydrophilic active substance.

Accordingly, the nanocapsule concentrate composition of the present invention can easily obtain nano-capsules of a hydrophilic active material having a skin-like composition and structure by simple stirring, and is economical as well as excellent in transparency and mat stability of concentrated capsules. Of the cosmetic composition of the present invention.

While the invention has been shown and described with reference to certain exemplary embodiments thereof, it will be understood by those skilled in the art that various changes and modifications may be made without departing from the spirit and scope of the invention as defined by the appended claims.

Claims (6)

A hydrophilic active material part containing a hydrophilic active material represented by the following formula
A liposome concentrate comprising a temperature-sensitive polymer lipid exhibiting temperature sensitivity at 32 to 37 占 폚 represented by the following formula (2):
Formula 1

(2)

Wherein R is selected from the group consisting of ceramides, lecithin, phosphatidylcholine, phytosphingosine and fatty acids, and both ends may be the same or different, l is 92 to 102, m is 60 to 70, n Lt; / RTI &gt; The nanocapsule concentrate composition according to claim 1, wherein the nanocapsule concentrate composition contains 0.01 to 0.5% by weight of the hydrophilic active material represented by the general formula (1). The nanocapsule concentrate composition according to claim 1, wherein said nanocapsule concentrate composition comprises 0.5 to 2.0 wt% of a thermosensitive polymer lipid, 1.0 to 8.0 wt% of a phospholipid, 0.1 to 1.5 wt% of a ceramide, 0.1 to 1.5 wt% of a cholesterol, 1.5 to 1.5% by weight of fatty acid, 0.05 to 1.0% by weight of fatty acid and 0.01 to 0.5% by weight of a lipophilic antioxidant. 2. The nanocapsule concentrate composition according to claim 1, wherein the hydrophilic active material represented by Formula 1 is concentrated and collected in an aqueous phase formed between an innermost layer of a nanocapsule having an average particle size of 40 to 150 nm and a bilayer of lipid bilayer . The nanocapsule concentrate composition of any one of claims 1 to 4,
And a diluent composition containing 2 to 10% by weight of the nano-capsule concentrate composition. [Claim 5] The cosmetic composition according to claim 5, wherein the diluent composition is elongated at a temperature corresponding to body temperature at the time of skin application, wherein at least 90% of the hydrophilic active substance represented by Formula 1 is eluted after 12 hours.

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