KR102004147B1 - Cosmetic composition contaning lioosome idebenone - Google Patents

Abstract

The present invention relates to a cosmetic composition comprising liposomalized ibebenone as an active ingredient, and more particularly to a cosmetic composition comprising liposomalized ibebenone as an active ingredient, wherein the liposomized ibebenone is selected from the group consisting of phospholipids, An active ingredient, and a moisturizing agent, and the active ingredient is a yeast extract, a collagen powder, and an aluminum powder. The cosmetic composition according to the present invention has an excellent transdermal absorption rate such as ibebone, yeast extract, collagen powder, and aluminum powder, and thus has an excellent effect of improving skin wrinkles and skin conditions, and is excellent in formulation stability and feeling have.

Description

TECHNICAL FIELD [0001] The present invention relates to a cosmetic composition comprising liposomalized ibebenone as an active ingredient,

The present invention relates to a cosmetic composition comprising liposomalized ibebenone as an active ingredient, and more particularly to a cosmetic composition containing liposomalized ibebenone as an active ingredient which enables the skin active ingredient to penetrate into the skin structurally more stably To a cosmetic composition.

Skin composed of epidermis, dermis, and subcutaneous fat is the largest organ of the human body and is a very important body that plays various roles such as temperature control function, excretion function, respiration function, human body protection function and barrier function.

However, as the age increases, the function of the skin suddenly deteriorates, resulting in various changes and aging. In particular, it is known that active oxygen and free radicals generated due to the increase of ultraviolet ray amount and air pollution and the excessive fatigue and stress of modern people act as a main cause of skin aging by oxidizing or denaturing biological components due to high reactivity So far, no definite cause has been identified.

As the aging process progresses, the skin undergoes various changes. First, the thickness of the epidermis, dermis, and subcutaneous tissue, which are constituents of the skin, is thinned, and the ECM (Extracellular matrix) component, which gives elasticity to the skin, is changed. Collagen fibers (collagen fibers), reticular fibers, elastic fibers (elastic fibers), and elastin fibers are among the connective tissue fibers of ECM. Collagen, which accounts for 70 ~ 80% of ECM, And the generation thereof is rapidly deteriorated, so that it is closely related to the generation of wrinkles. That is, since the synthesis of collagen is lowered or decomposition is promoted, skin aging phenomena such as skin sagging, loss of elasticity, and wrinkles of the skin occur.

Idebenone is known as an effective substance for preventing skin aging. The above-mentioned idebenone is a Ubiquinone-type antioxidant present in a living cell membrane, and it is an adenosine triphosphate (ATP) which is a cell energy in mitochondria. The chemical name is 2,3-dimethoxy-5-methyl-6- (10-hydroxydecyl) -1, which is a chemical substance having a structure similar to Coenzyme Q10 mainly involved in ETC (Electron Transfer Chain) Dimethoxy-5-methyl-6- (10-hydroxy decyl) -1,4-benzoquinone] and has a molecular weight of 338.44 and is known as a refined yellow crystalline powder material obtained mainly by chemical synthesis have.

According to the above-mentioned research reports, it has been reported that medicines and cosmetics for pharmaceutical use or cosmetics, which have such excellent efficacy in aging, have been reported in various academic papers.

In addition, itbenone is involved in ETC (Electron Transfer Chain) related to the production of ATP (Adenosinetriphosphate), which is a cell energy in mitochondria, and is effective for cell activation. In the mitochondria, ROS (Reactive Oxygen Species) Alzheimer ' s disease, which is a degenerative neurological disease that is problematic due to aging by promoting nerve growth factor (NGF) medically, preventing cerebrovascular disease (Cerebrovascular < RTI ID = disease and liver disease have also been reported.

However, one of these biologically active substances, ibebenone, has a complex structure such as a quinone group, a saturated hydrocarbon group and a hydroxyl group, has a high polarity and a low melting point, In the emulsion system, it is difficult to stabilize and penetrate into the skin, making it difficult to apply it to actual cosmetics.

That is, even if the emulsified particles are formed by once dissolving iidebenone, there is a problem in stability of the formulation and preservation of the activity of idebene when emulsifying techniques and emulsifiers are used. Particularly, when idebone is prepared as nanocapsule particles Unlike general micro droplets, nanoparticles are physically thin. In the case of a highly polar material such as i-de-neon, the nanoparticles are soluble in a continuous phase around the particle Solubility) and the stability is deteriorated by the phenomenon of Ostwald ripening (Ostwald ripening).

In addition, the molecular structure of the biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable polymer It is difficult to provide the desired wrinkle-improving effect to the skin. Thus, idebenone is very limited in its formulation stability as well as its efficient use in drug delivery into the skin.

In addition, the molecular structure of the biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable biodegradable polymer It is difficult to provide the desired wrinkle-improving effect to the skin.

Thus, idebenone has a very limited use in formulation stability as well as effective drug delivery into the skin.

Accordingly, there has been proposed a method of using nidecanone nanocapsules in order to stabilize the above-mentioned benbenone and increase the skin transferring effect. However, such nano-encapsulated ibebenone is applicable only to viscous cosmetic compositions and has a disadvantage that the penetration effect of the skin is not greatly improved.

KR 10-0810164 B1 KR 10-1671727 B1

Accordingly, an object of the present invention is to provide a cosmetic composition comprising liposomized idebenone as an active ingredient, which is excellent in skin penetration and can be stably preserved without loss of long-term activity.

It is also an object of the present invention to provide a cosmetic composition which is effective for preventing wrinkles such as aging.

To achieve the above object, the present invention provides a cosmetic composition comprising liposomalized ibebenone as an active ingredient, which comprises liposomized ibebenone as an active ingredient, wherein the liposomized ibebenone is selected from the group consisting of phospholipids , A surfactant, an active ingredient, and a moisturizing agent, and the active ingredient is a yeast extract, a collagen powder, and an aluminum powder.

The liposomized ibebenone further comprises an antioxidant, an oil sealant and a sequestering agent.

Wherein the active ingredient further comprises dipotenol, the humectant is glycerin, the antioxidant is tocopherol, the oil sealant is at least one of caprylic / capric triglyceride, squalane, argan oil, The sequestering agent is characterized in that disodium is dithia.

Wherein the liposomized ibebenone is selected from the group consisting of 1.0-5.0% by weight of ibebenone, 5.0-20.0% by weight of phospholipids, 0.1-10.0% by weight of surfactant, 1.6-40% by weight of active ingredient, 0.5-1.0% by weight of antioxidant, 0.01 to 10.0% by weight, a metal ion blocking agent in an amount of 0.01 to 0.2% by weight, and a residual amount of a moisturizing agent.

And 0.1 to 50.0% by weight of the liposomized idebenone based on 100% by weight of the cosmetic composition.

The cosmetic composition according to the present invention is excellent in transdermal absorption rate of idebone, yeast extract, collagen powder and the like, and thus has an excellent effect of improving skin wrinkles and improving skin condition, and is excellent in formulation stability and feeling of use.

1 and 2 are graphs showing particle distribution diagrams of Example 1 and Comparative Example 1 according to Test Example 1 of the present invention.
3 is a photomicrograph of a liposome composition according to Example 1 and Comparative Example 1 according to the present invention.
4 is a photograph of the liposome composition according to Example 1 and Comparative Example 2 of the present invention.

Hereinafter, the present invention will be described in detail.

The most remarkable feature of the present invention is to increase the absorption rate of idebene by making idebanone liposomes. In addition, in order to increase the stability of the liposomized ibuprofen, aluminum powder is used together as an active ingredient.

To this end, the cosmetic composition of the present invention comprises liposomized ibebenone as an active ingredient, wherein the liposomized ibebenone is liposomized by mixing ibebenone with a phospholipid, a surfactant, an active ingredient and a humectant, The active ingredient is characterized by being yeast extract, collagen powder and aluminum powder.

First, as described above, the above-mentioned idevone has excellent anti-aging effects such as wrinkle improvement, but is a component which is difficult to penetrate into skin as well as formulation stability. In the present invention, liposomalization of the above-mentioned ibebenone improves the formulation stability and enhances penetration into the skin.

For this purpose, phospholipids to be mixed together are used to form stable lipid membranes. They are natural phospholipids such as egg yolk lecithin, soybean lecithin and sphingomyelin, synthetic phospholipids such as dipalmitoylphostatidylcholine and hydrogenated lecithin Most preferably, lecithin is used.

The surfactant is used for the stabilization of liposomes, and an anionic surfactant, one or more kinds of natural surfactants, and most preferably two kinds of surfactants are used. The anionic surfactant may be sodium stearoyl glutamate or sodium oles-7 phosphate, and the natural surfactant may be polyglyceryl-3-ol Bait phosphate or polyglyceryl-3-cetearyl ether olivate.

The active ingredient is a component for stabilizing the formulation as well as a component showing the function of improving the condition of the skin through the interaction with ideverone, that is, moisturizing, elasticity, whitening and anti-aging. In the present invention, yeast extract, collagen powder and aluminum It is preferable to include all the powders.

The yeast extract is a component that imparts elasticity to the skin, and when used in combination with ideverone, exhibits an excellent effect in preventing aging. The yeast extract may be any commercially available product.

The collagen powder is an excellent moisture-retaining agent and has an excellent moisturizing effect to maintain elasticity of skin cells and moisturize the skin. The kind of the collagen powder is not limited, and any of commercially available products can be used

The above aluminum powder is used for stabilizing the formulation of liposomized idebene. When the aluminum powder is not used, the liposomized idebenone can not be stabilized and it is difficult to store and use for a long period of time. RTI ID = 0.0 > liposomal < / RTI > The aluminum powder may be any commercially available product used as a raw material for a cosmetic composition.

 As the moisturizing agent, glycerin, which is ordinarily most commonly used in cosmetic compositions, can be used.

In addition, the liposomized ibebenone may further comprise an antioxidant, an oil sealant, and a sequestering agent.

The antioxidant restores damaged skin function and structure due to oxidation, and tocopherol, i.e. alpha tocopherol or vitamin E-tocopherol, can be used.

The oil sealant may exhibit a moisturizing effect by forming a film on the skin and sealing the skin. Any of natural oils and synthetic oils may be used, and examples thereof include caprylic / capric triglyceride, squalane, argan oil Can be used.

The sequestering agent is used to prevent precipitation of metal ions in the composition, and disodium edentate may be used.

Further, the active ingredient may further include D-Panthenol. The above-mentioned di-panthenol directly supplies insufficient water, activates the moisturizing function, and has an effect of improving the skin condition.

Wherein the liposomized ibebenone is selected from the group consisting of 1.0-5.0% by weight of ibebenone, 5.0-20.0% by weight of phospholipids, 0.1-10.0% by weight of surfactant, 1.6-40% by weight of active ingredient, 0.5-1.0% by weight of antioxidant, 0.01 to 10.0% by weight, a metal ion blocking agent of 0.01 to 0.2% by weight, and a residual amount of a moisturizing agent, considering stability of the liposome composition, prevention of aging, skin improvement effect and the like. The active ingredient may be used in a proportion of 0.5-10% by weight of yeast extract, 0.5-10% by weight of collagen powder, 0.5-10% by weight of aluminum powder and 0.1-10% by weight of di-panthenol.

In the present invention, the method for liposomizing ibebenone may be performed by any conventional method known in the art, and the practice thereof is not limited. That is, if the dehydenone, the phospholipid, the surfactant, the active ingredient, the antioxidant, the oil sealant, the sequestering agent and the remaining amount of the moisturizer are mixed and stirred, Collagen powder, and the like to form micelles. The liposomes are produced by using a high pressure homogenizer or the like, and the pressure and the number of the liposomes can be controlled according to the desired particle size. More preferably, the pressure is set to 600 to 1,200 bar and the high pressure homogenizer is passed through 1 to 5 times. At this time, the agitation temperature may be about 50 to 70 캜, and the liposomizing temperature may be about 30 to 55 캜, but the temperature is not limited.

As described above, liposomized ibebenone has a nano-sized particle size, uniform particle size distribution, and high skin permeability, and can exhibit the effects of improving elasticity, wrinkle, and moisturizing effect.

The cosmetic composition of the present invention may contain 0.1 to 50.0% by weight of liposomalized ibebenone based on the total weight of the cosmetic composition. If necessary, the liposomalized ibebenone may further contain the effect of the present invention A water-soluble component, a powder component, an oil component, a surfactant, a moisturizing agent, a viscosity adjusting agent, an antiseptic, an antioxidant, a perfume, a coloring matter and the like can be blended .

In addition, the cosmetic composition of the present invention may be prepared in any formulations conventionally produced in the cosmetics industry, and may be in the form of solutions, suspensions, pastes, gels, creams, lotions, powders, oils, powder foundations, emulsion foundation , A wax foundation, and a spray, but the present invention is not limited thereto. More particularly, it can be manufactured in the form of a flexible lotion (skin), a nutritional lotion (lotion), a nutritional cream, a massage cream, an essence, a pack, a spray, a soap or a powder.

Hereinafter, the present invention will be described in more detail with reference to more specific examples and examples, but the present invention is not limited thereto.

(Example 1)

The following ingredients were prepared in the same amounts as shown in Table 1 below, and the mixture was then homogenized at 50 ° C using a homomixer at a rotation speed of 1500 rpm at 10 ° C for 10 minutes. Min for 1 minute, and the high-pressure homogenizer was allowed to pass 2-3 times at a pressure of 700 to 800 bar at 40 DEG C to prepare a liposome composition.

(Comparative Example 1)

A liposome composition was prepared in the same manner as in Example 1, except that the ingredients in the amounts shown in Table 1 were used without using the yeast extract, the yeast extract, and the aluminum powder.

(Comparative Example 2)

A liposome composition was prepared in the same manner as in Example 1 except that aluminum powder was not used and ingredients having the same contents as in Table 1 below were used.

(% By weight) of Example 1 and Comparative Examples 1 and 2, division Example 1 Comparative Example 1 Comparative Example 1 Idebenon 3.0 0.0 3.0 Phospholipids Lyso lecithin
(Lysolecithin) 10.0 10.0 10.0 Surfactants
Anionic surfactant
(Sodium stearoyl glutamate) 3.0 1.0 3.0 Naturally derived surfactant
(Polyglyceryl-3-olivate phosphate) 3.0 1.0 3.0 Active ingredient

Yeast extract 4.0 0 4.0 Collagen powder 5.0 5.0 5.0 Aluminum powder 0.5 0 0 Antioxidant Alpha tocopherol 0.1 0.1 0.1 Oil
Sealant

Caprylic / Capric Triglyceride (Caprylic / Capric Triglyceride) 4.5 4.5 4.5 Squalane 0.2 0.2 0.2 Argan Oil 0.1 0.1 0.1 Metal ion sequestrant Disodium EDTA < RTI ID = 0.0 > 0.1 0.1 0.1 Moisturizer glycerin to 100 to 100 to 100 * IDEEBONON: (Product name: IDEBENONE, Manufacturer: NATURAL (China))
* Yeast extract: (Product name: Celldetox /, manufacturer: SILAB (France))
* Collagen Powder: (Product Name: Fish Collagen, Manufacturer: Geltech (Korea))
* Aluminum powder (product name: aluminum powder, Importer: Risselab)

(Test Example 1): Analysis of particle characteristics

The characteristics of the particles prepared according to Example 1 and Comparative Example 1 were analyzed and shown in FIG. 1 and FIG. Here, FIG. 1 is a particle distribution diagram of Example 1, and FIG. 2 is a particle distribution diagram of Comparative Example 1.

NANO-ZS90 (manufactured by Malvern Korea) was used as the light scattering measurement instrument and the measurement conditions were as shown in Table 2 below. The particle size (average diameter) and the particle size distribution were analyzed using light scattering measurement equipment.

Tube scattering measurement conditions. division Example 1 Comparative Example 1 Temperature 23.0 DEG C 22.9 ° C Solvent Name water water Refractive Index 1.3315 1.3315

As can be seen from Figs. 1 and 2, it was confirmed that the liposome particles of Example 1 had a smaller average diameter and a more uniform particle size distribution than that of Comparative Example 1.

FIG. 3 is a microscope photograph of the liposome composition according to Example 1 and Comparative Example 1, showing that the composition of Example 1 according to the present invention has a uniform particle size and a stable property as compared with the composition of Comparative Example 1 there was.

FIG. 4 is a photograph of the liposome composition according to Example 1 and Comparative Example 2, wherein the composition of Example 1 is a clear liquid, whereas the composition of Comparative Example 2 containing no aluminum powder is a lucid liquid As a result, it was confirmed that the composition of Example 1 was more stable than the composition of Comparative Example 1.

(Example 2): Preparation of cosmetic formulations

Various formulations of cosmetics were prepared with the compositions shown in Table 3 below. Here, the reason why the fruit acid is added is to check whether the skin is stimulated. Each formulation was called T1 (skin), T2 (lotion), T3 (essence), T4 (cream), T5 (pack).

The ingredient content of Example 2 ingredient T1 (skin) T2 (lotion) T3 (Essence) T4 (cream) T5 (pack) Example 1 2.0 2.0 2.0 2.0 2.0 glycerin One 2 3 4 5 Butylene glycol One 4 4 4 6 PIGGY-60 Hydrogenated Castor Oil 0.2 0.1 0.1 0.2 0.3 Carbomer 0 0.07 0.1 0.2 0.3 Stearic acid 0 0.15 0.3 1.2 1.5 Cetearyl alcohol 0 0.05 0 1.5 2 Squalane 0.5 1.0 2.0 3.0 4.0 Sheer butter 0 0.05 0 1.5 2.0 Beads wax 0 1.0 2.0 3.0 2.0 Glyceryl stearate 0 0.5 1.0 1.5 2.0 FAGE -100 stearate 0 0.5 0 One One Sorbitan sesquioleate 0 0.2 0 0.8 1.5 Triethanolamine 0 0.05 0.08 0.2 0.3 Hyaluronic acid 1.0 1.5 2.0 2.0 1.0 Fruit acid 0.2 0.2 0.2 0.2 0.2 1,2-hexanediol 2 2 2 2 2 Spices 0.02 0.02 0.02 0.02 0.02 Purified water to 100 to 100 to 100 to 100 to 100

(Comparative Example 3): Preparation of cosmetic formulations

Comparative Example 1 was used in place of Example 1, while the same procedure as in Example 2 was carried out. At this time, each of the formulations was referred to as S1 (skin), S2 (lotion), S3 (essence), S4 (cream), S5 (pack).

(Test Example 2)

The following sensory evaluations were performed to evaluate the skin moisturizing feeling, feeling of use, feeling of firmness, improvement of skin condition, feeling of after use, and skin irritation effect of the cosmetic formulations prepared according to Example 2 and Comparative Example 3.

First, 30 women aged 21 to 40 years old were selected as subjects to be tested. After washing the face of the subject to be tested cleanly, 0.1 g to 0.2 g of the content of Example 2 was uniformly applied to the face half, And the other half of the opposite face was coated uniformly with 0.1 g to 0.2 g of the contents of Comparative Example 3.

At this time, each experiment was performed for 7 days. After 7 days, use was discontinued for 7 days. The subjects were subjected to sensory evaluations of skin moisturizing, feelings on feeling, feeling of firmness, improvement of skin condition, feeling after use, and skin irritation after each 7 days, and the results are shown in Table 4 below. At this time, the evaluation was evaluated as 5 points when the effect to be felt is excellent, and 6 points when it is not felt at all.

Test Example 2 Results evaluation
Item Example 2 Comparative Example 3 T1 T2 T3 T4 T5 S1 S2 S3 S4 S5 Moisturizing 4.5 4.5 5.0 5.0 5.0 3.0 3.0 3.0 3.0 3.0 Feeling 4.5 4.5 4.5 4.5 4.5 3.5 3.0 3.0 3.5 3.0 A sense of urgency 4.5 5.0 5.0 4.5 4.5 3.5 3.5 3.5 3.0 3.5 Improved skin condition 4.0 4.5 4.5 4.5 4.5 3.5 3.5 3.5 3.5 3.0 After use feeling 4.0 4.5 4.5 5.0 4.0 4.0 3.5 3.5 3.5 3.5 Skin irritation 0 0 0 0 0 0 0 0 0 0 Skin clear 4.5 4.5 5.0 4.5 4.5 3.0 3.0 3.5 3.0 3.0

As can be seen from the above Table 4, all of the formulations of Example 2 and Comparative Example 3 were free of skin irritation, but all of the formulations of Example 2 had a moisturizing feeling, a feeling of use, a sense of elasticity, Of all formulations.

(Test Example 3)

Ten women in their thirties or older who are undergoing skin aging were instructed to use T3 of Example 2 and S3 of Comparative Example 2 on the left and right faces respectively for 12 weeks and then measure the depth of the wrinkles Respectively. The depth of the wrinkles was measured using a skin wrinkle measuring device (SV-600, C + K, Germany).

As a result, it was confirmed that the wrinkle depth reduction ratio of Example 2 was 6.1% and the wrinkle depth reduction ratio of Comparative Example 3 was 1.1% after 12 weeks.

While the present invention has been particularly shown and described with reference to exemplary embodiments thereof, it is to be understood that the scope of the present invention is not limited to the disclosed exemplary embodiments. It will also be appreciated that many modifications and variations will be apparent to those skilled in the art without departing from the scope of the invention.

Claims (5)

Which comprises liposomized idebanone as an active ingredient,
Wherein the surfactant is used in an amount of 1.0 to 5.0% by weight, the phospholipid 5.0 to 20.0% by weight, the surfactant 0.1-10.0% by weight, the active ingredient 1.6-40% by weight, the antioxidant 0.5-1.0% And 0.01 to 0.2% by weight of liposomal lidocaine as an active ingredient.
delete The method according to claim 1,
The active ingredient is used in a proportion of 0.5-10 wt% of yeast extract, 0.5-10 wt% of collagen powder, 0.5-10 wt% of aluminum powder, 0.1-10 wt% of di-panthenol,
The antioxidant is tocopherol,
The oil sealant is at least one of caprylic / capric triglyceride, squalane, and argan oil,
Wherein the sequestering agent is disodium EDTA. The cosmetic composition according to claim 1, wherein the disintegrant is disodium EDTA.
delete The method according to claim 1 or 3,
Based on 100% by weight of the cosmetic composition,
And 0.1 to 50.0% by weight of the liposomalized ibebenone. Description: CLAIMS 1. A cosmetic composition comprising liposomalized ibebenone as an active ingredient.

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