KR101961649B1 - Liposome compositions for accelerating percutaneous absorption - Google Patents

Abstract

The present invention relates to a transdermal absorption-promoting liposome composition which is characterized by containing hydrogeneate lecithin, phosphatidylcholine, polysorbate 80, lysolecithin, active ingredient and water, which is more stable than conventional liposome and nanoemulsion, It is excellent in penetration rate and penetration into the skin and has a high absorption rate, which has the effect of promoting transdermal absorption, which can provide a moisturizing and moisturizing sustained effect.

Description

TECHNICAL FIELD [0001] The present invention relates to a liposome composition for accelerating percutaneous absorption,

The present invention relates to a liposome composition for promoting transdermal absorption, and more particularly, to a liposome composition for promoting transdermal absorption, and more particularly, to a liposome composition for promoting transdermal absorption by preparing a liposome composition which is a lipid vesicle using hydrogeneate lecithin, phosphatidylcholine, polysorbate 80, The present invention relates to a liposome composition for promoting transdermal absorption, which is stable compared to an emulsion, has excellent bioavailability and penetration into the skin, and has a high absorption rate, thereby providing moisturizing and moisturizing sustained effects.

Two liquids that do not mix together are called dispersions in which one liquid is dispersed in the form of small particles in one liquid with the aid of a surfactant. Emulsions, solubilization, and microemulsions are popular liquid-liquid dispersions widely used in the industry. The colloid is classified into particle size and thermodynamic equilibrium state, and it can be roughly divided into emulsification and solubilization according to the particle size and thermodynamic stability of the dispersed phase, and can be divided into the intermediate form, microemulsion.

Efforts and studies have been actively conducted to utilize a transdermal delivery system (TDS) in functional cosmetics in order to stabilize an active substance having an effect and increase transcutaneous permeation efficiency. Such transdermal delivery systems include atomization, coexistence, spray coating, self-assembly, intercalation, phase separation, polyradiation, liposome, sol-gel method, and nano encapsulation method using encapsulation.

The transdermal delivery system using the double liposome is mainly made of a surfactant, a lipid, a polymer, and the like and is made into a vesicle containing an active substance. Especially, since phospholipid is a main component constituting a biological membrane, lipid is widely used as a cosmetic material .

Lipid is a compound that exists in the natural world. Phosphoglycerides (phosphoglycerides), sphingolipids (steroids) and sterols (sterols) are lipids that can be found mainly in the cell membrane. Phosphoglycerides and some sphingolipids belong to phospholipids, but sterols and some sphingolipids do not belong to phospholipids.

Phospholipids are amphipathic lipids with an amphipathic lipid with a head and a hydrophobic tail on the basis of a phosphate structure, There is amphipathic lipid.

Phosphoglyceride (phosphoglyceride) is derived from glycerol 3 phosphate and is the most abundant phospholipid in the cell membrane. Typical phosphoglyceride molecules are fatty acid based acyl chains that are attached to hydrophobic tails and phosphate groups that are esterified with two-OH groups of glycerol phosphate And a polar portion (head). Phosphoglycerides are classified according to the nature of the polar part, and phosphatidylcholine is the most abundant lipid found in the cell membrane. The polar moiety is choline, a positively charged alcohol, and is in the form of an ester reaction with a negatively charged phosphate group. Other types of phosphoglycerides are attached to the phosphate group, such as ethanolamine, serine, and inositol, molecules with -OH. Negatively charged phosphate moieties and polar moieties that are positively charged or have -OH readily interact with water. At neutral pH, some phosphoglycerides (ex: phosphatidylcholine, phosphatidylethanolamine) do not charge, while other molecules (ex: phosphatidylinositol, phosphatidylserine) have a negative charge of -1. All these molecules come together to form a bilayer structure. When a phospholipase reacts with phosphoglycerides, it produces a lysophospholipid, which is a molecule without one of the two acyl branches. Usually, lysophospholipids play a role in signal transduction between specific cells and can alter the physical properties of the membrane.

This material can provide high permeability to horny layer, liquid crystal forming ability, improvement of barrier function of skin, restoration of skin elasticity, stability of emulsion, and excellent feeling for skin care.

In addition, the stratum corneum present in the outermost part of the skin is the primary barrier for barrier function, and the stratum corneum has the same shape as keratin cells stacked up like bricks and plays a role like a plaster to support these keratinocytes Keratinocyte quality. The stratum corneum is composed of about 40% protein, 40% water and 10-20% lipid, the structure of which consists of protein-rich keratinocytes and the lipid filling between them, .

As a method for infiltrating the active ingredients with such a stratum corneum, there has been proposed a method for expanding the area applied to the skin or to increase the permeability to the skin by using liposomes and liposomes composed of proliposomes and nonionic surfactant vesicles made of nioxides and proniosomes Nanoemulsion and liposomes are used, but they are still unable to pass through the stratum corneum membrane.

Thus, a method is employed in which the active material is enclosed in a transfer sample corresponding to a carrier in order to facilitate the permeation of the active substance into the stratum corneum by activating the substance to increase the force for independently moving the substance.

Transferosome is an extremely deformable endoplasmic reticulum with a nucleus containing water surrounded by a complex bilayer, with very good application force, pressure responsiveness and a complex skeleton. Such transferosomes penetrate into the stratum corneum through intracellular or intracellular pathways, and the flexibility of the transferosomes can be obtained by mixing appropriate surfactant components at the appropriate ratio. As a result, the risk of destroying the complete endoplasmic reticulum in the skin under non-occlusive conditions can be reduced, and the transferosome protects the encapsulated active substance from metabolic degradation, allowing them to slowly and gradually release their contents as a warehouse.

Also, the transferosome is usually 10 to 100 times larger than the standard lipid micelle, which is a conventional micellar carrier, so permeation is not linearly diffused, and the permeability increases nonuniformly or nonlinearly as the pressure increases. In addition, while micelles are merely one useful droplet structure, transferosomes have water-borne nuclei, so that transferosomes can carry not only liposoluble but also water-soluble, whereas micelles contain only lipidic substances.

Generally, in order to increase the stability of liposome and penetration of the skin, it is possible to use only saturated lecithin. However, since the particle size increases over time, penetration of the skin is not easy and stability of the emulsion is also deteriorated.

As a result of intensive studies, the Applicant has found that the liposome composition, which is a lipid vesicle prepared by using hydrogeneate lecithin, phosphatidylcholine, polysorbate 80 and lysolecithin, is more stable than conventional liposome and nanoemulsion, Skin penetration is excellent and absorption rate is high, and thus it has been found that a cosmetic composition containing the same can provide a moisturizing and moisturizing effect.

Korean Patent Publication No. 10-2012-0040822 Korean Patent Publication No. 10-2017-0023295

Accordingly, it is an object of the present invention to provide liposomes, which are lipid vesicles, by using hydrogeneate lecithin, phosphatidylcholine, polysorbate 80, lysolecithin and active ingredients to produce liposomes which are more stable than conventional liposomes and nanoemulsions, And a liposome composition for accelerating transdermal absorption which is capable of imparting a moisturizing and moisturizing sustainable effect due to its high penetration and high absorption rate.

To achieve the above object, the present invention provides a liposome composition for promoting percutaneous absorption, which comprises hydrogeneate lecithin, phosphatidylcholine, polysorbate 80, lysolecithin, an active ingredient, and water in a residual amount.

The present invention also provides a cosmetic comprising the liposome composition.

Herein, the liposome is a spherical vesicle composed of a lipid bilayer, and the liposome composition according to the present invention includes hydrogeneate lecithin, phosphatidylcholine, polysorbate 80, and lysozyme The transdermal absorption is promoted because it has a flexible ability to pass through the liposome shape after passing through the stratum corneum, and then return to its original shape.

In addition, the liposome composition of the present invention comprises 0.01 to 10% by weight, preferably 0.5 to 8% by weight, more preferably 1 to 5% by weight of the hydrogeneate lecithin. In the present invention, the hydrogeneate lecithin forms a lipid bilayer of liposomes as a kind of phospholipids which are both affinity lipids. In the present invention, when the content of hydrogeneate lecithin is less than 0.01% by weight, there may be a problem in forming liposomes. When the content of liposomes is more than 10% by weight, excess amount of active ingredient in the liposome decreases There may be a problem.

In addition, the liposome composition of the present invention contains 0.01 to 10% by weight, preferably 0.1 to 6% by weight, more preferably 0.3 to 2% by weight of phosphatidylcholine. Phosphatidylcholine is a type of bean lecithin and egg lecithin that has stability, combined emulsification and solubilization properties, and is faster in innocuous substances than most synthetic surfactants. My metabolism tends to be. In the present invention, if the content of phosphatidylcholine is less than 0.01% by weight, there is a problem in stability of the liposome, and if it exceeds 10% by weight, liposome formation may be a problem.

In addition, the liposome composition of the present invention comprises 0.01 to 5% by weight, preferably 0.05 to 3% by weight, more preferably 0.1 to 1% by weight of polysorbate 80. In the present invention, polysorbate 80 is a nonionic cosurfactant and serves as an emulsifying and solubilizing agent for the liposome composition. If the content of polysorbate 80 is less than 0.01% by weight, the emulsion stability of the liposome is deteriorated. If the amount of the polysorbate 80 is more than 5% by weight, liposome formation may be a problem.

In addition, the liposome composition of the present invention comprises 0.01-5% by weight, preferably 0.05-3% by weight, more preferably 0.1-1% by weight of lysolecithin. In lyso lecithin, the term lyso- refers to dissolution, in which the fatty acid at position 2 is removed from lecithin. In the present invention, lyso lecithin is introduced between bilayers of lecithin to aid in the deformation of liposomes. In the present invention, if less than 0.01% by weight of the liposecretion is contained, the effect of the liposecretion upon the formation of the liposome may be weakened, and if it exceeds 5% by weight, the liposome may become unstable.

The liposome composition of the present invention contains 0.01 to 40% by weight, preferably 0.05 to 35% by weight, more preferably 0.1 to 30% by weight of the active ingredient. If the active ingredient is contained in an amount of less than 0.01% by weight, the effect of the active ingredient may be weakened when the liposome is formed. If the active ingredient is contained in excess of 40% by weight, liposome formation may be unstable due to excessive active ingredients.

There is no particular limitation on the active ingredient that can be contained in the liposome composition of the present invention. The active ingredient in which the liposome of the present invention can be utilized includes, for example, natural extracts, oils, moisturizers, whitening agents, wrinkle remedies, acne modifiers, atopic emollients, sunscreens, hair restorers, vitamins, amino acids or polypeptides, But is not limited to, at least one selected from the group consisting of hormones, keratolytic agents, fungicides, flavanol, allantoin, yeast extract, collagen, elastin, DHA, EPA, ceramide, perfume and the like.

Here, the oil used in the liposome composition of the present invention is not particularly limited, but may be one or more selected from the group consisting of oils, waxes, hydrocarbon oils, higher fatty acid ester oils, higher alcohol oils, Or more can be used.

Herein, the fat is preferably, but not limited to, a fatty acid and triglyceride as a main ingredient, more preferably macadamia nut oil, olive oil, jojoba oil, almond oil, apricot seed oil, green tea oil, Sunflower oil, argan oil, camellia oil, avocado oil, soybean oil, grapeseed oil, castor oil, rice bran oil, and the like.

The wax is not particularly limited, but is preferably an ester of a higher fatty acid and a higher alcohol, and more preferably a wax such as carnauba wax, candelilla wax, jojoba oil, beeswax, lanolin, soybean wax, rice wax, May be used.

The hydrocarbon-based oil is not particularly limited, and at least one selected from the group consisting of liquid paraffin, paraffin, vaseline, ceresin, microcrystalline wax, squalane, etc. may be used.

The higher fatty acid ester (higher fatty acid ROOH, in this case, R: saturated alkyl group, unsaturated alkynyl group) type oil is not particularly limited, but may be lauric acid, myristic acid , Palmitic acid, stearic acid, isostearic acid, and the like.

Further, the higher alcohol-based oil is not particularly limited, and it may be a 1-ethylhexanoate derivative selected from the group consisting of cetyl alcohol, stearyl alcohol, isostearyl alcohol, 2-octyldodecyl, 2-ethylhexanetetracarboxylic acid, More than species can be used.

The butter is not particularly limited, but at least one selected from the group consisting of shea butter, soy butter, and mango butter can be used.

The silicone oil is not particularly limited, but at least one selected from the group consisting of dimethicone, cyclomatic cone, silicone polymer, and the like can be used.

In addition, the ester-based oil is not particularly limited, but may be selected from the group consisting of cyclohexylhexanoate, diglyceryl triisostearate, capric / caprylic triglyceride, glyceryl tri-2-ethylhexanoate, Octyldodecyl myristate, pentaerythrityl tetrahexylhexanoate, octyldodecylmyristate, octyldodecylmyristate, pentaerythrityl tetrahexylhexanoate, octyldodecylmyristate, octyldodecylmyristate, At least one selected from the group consisting of pentaerythrityl tetraisostearate, isotrientylisononanoate, trimethylolpropane triisostearate, squalane and the like may be used.

The moisturizing agent is not particularly limited, but may be at least one selected from the group consisting of sodium lactate, hydro-proline, sodium 2-pitolipo-5-carboxylate, hyaluronic acid, sodium hyaluronate, ceramide, phytosterol, cholesterol, Can be used.

The ultraviolet screening agent is not particularly limited, but at least one selected from the group consisting of a benzophenone derivative, a p-aminobenzoic acid derivative, a methoxy cinnamic acid derivative, and a salicylic acid derivative may be used.

The whitening agent is not particularly limited, but at least one selected from the group consisting of arbutin, arbutin derivatives, kojic acid, vitamin C and vitamin C derivatives can be used.

The hair restoring agent is not particularly limited, but a blood circulation promoting agent and / or local irritant are preferable. Preferably, the blood circulation accelerator is one selected from the group consisting of moon herb extract, sepharastatin, vitamin E and its derivatives, gamma oryzanol, and proteoglycan. Examples of the topical stimulants include red pepper tincture, ginger tincture, kantaridin tincture and nicotinic acid benzyl ester Is preferable.

There is no particular limitation on the vitamins and their derivatives. Among them, vitamin A and its derivatives, vitamins B1, B2, B6, E and its derivatives, vitamin D, H, K, pantothenic acid and its derivatives, biotin and panthenol One or more members selected from the group consisting of < RTI ID = 0.0 >

The amino acid is not particularly limited but may be selected from cystine, cysteine, methionine, serine, leucine, tryptophan, amino acid extract, EGF (Epidermal Growth Factor), IGF (insulin- Fibroblast Growth Factor (FGF), and kappa peptides can be used.

The anti-inflammatory agent is not particularly limited, and at least one selected from the group consisting of beta-glycyrrhizic acid, glycyrrhizic acid derivative, aprene, aminocaproic acid, hydrocortisone, betaglucan, and lycorus may be used.

There is no particular limitation on the acne remedy, but at least one selected from the group consisting of estradiol, estro, ethinyl estraliol, tricric acid, and azelic acid may be used.

There is no particular limitation on the fungicide, but at least one selected from the group consisting of benzalkonium chloride, benzyltannol chloride, and halokalane can be used.

The female hormone agent is not particularly limited, but estrogen is suitable, and estrogen is preferably estradiol, ethinyl estradiol, isoflavone such as phytoestrogen.

There is no particular limitation on the exfoliating agent, but at least one selected from the group consisting of sulfur, salicylic acid, ahah, baja, and resorcinol may be used.

There is no particular limitation on the natural extract as long as it is an extract of plant or animal, marine animal or marine algae, or a component obtained therefrom (a functional ingredient having an effect such as moisturizing, moisture, pore, trouble, whitening, elasticity moisturizing, Among them, it is possible to use it as a herbal extract, a marigold extract, a young woman, a birch sap, etc. And at least one selected from the group consisting of natural extracts obtained by the above method can be used. The extracts from the Arctic Circle / Antarctic Circle / Iceland / Northern Europe, such as Ascophyllum Nodosum Extract, Icelandic Phuops Glacier, Deep Sea Microbe (such as Thermus thermophilus fermentation), Antarctic microorganism, Extracts, arctic yeasts, sea parsley (Dulse) and picea abies (nidiformis) extracts in the Arctic sea.

The liposomal compositions of the present invention may comprise residual water in a solvent, for example, from 1 to 99.95% by weight of water.

The particle diameter of the liposome in the present invention is preferably 100 to 300 nm.

According to another aspect of the present invention, there is provided a cosmetic comprising the liposome composition of the present invention. In cosmetics, the liposome composition according to the present invention preferably comprises 1 to 40% by weight, more preferably 2 to 35% by weight.

In the present invention, if the cosmetic contains less than 1% by weight of the liposome composition, the effect provided by the active ingredient may be impaired and the effect provided by the active ingredient may be increased in proportion to its addition even if it exceeds 40% It is difficult to expect any more, and it is not economically desirable.

The liposome composition according to the present invention may be applied to other categories that can impart moisturization to existing products in addition to essence, lotion, cream, wash-off or leave-on products, depending on the content or use method. It is possible to use it as an additive of a moisturizing and moisturizing cosmetic composition which can be applied.

The cosmetics according to the present invention can be prepared in any conventional formulation as well as in lotion or lip make-up. Additives such as a softening agent, a flavoring, a pigment, an antioxidant, a pH adjuster, etc., Of course it is.

The liposome composition provided by the present invention is more stable than the conventional liposome and nano emulsion, has excellent bioavailability and penetration into the skin, and has a high absorption rate, so that it has a transdermal absorption promoting effect capable of moisturizing and sustaining moisturizing effect.

1 shows the results of measurement of the particle diameter of the liposome of the present invention using Photal ELS-Z. As a result,
Fig. 2 is a photograph of the liposome composition of the present invention taken in a magnified photograph using a frozen electron microscope,
FIG. 3 is a graph showing the result of measurement of skin moisturizing effect,
4 is a graph showing the results of measurement of transepidermal water loss (TEWL).

BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, the present invention will be described in detail with reference to the drawings, examples and experimental examples. It is needless to say that the following drawings, examples and experimental examples are illustrative of the present invention, but the content of the present invention is not limited thereto. In addition, a description of a conventional measurement experiment in an experimental procedure for measuring efficacy is omitted.

Examples 1 to 17: Preparation of Liposome Composition Containing Active Ingredients

The components were mixed in the following Tables 1 to 17, and the mixture was passed through the high pressure micro emulsifier 5 times continuously at 1,000 bar to obtain a liposome composition.

≪ Example 1 > Liposome composition containing natural extract and Antarctic microbial extract

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Iceland's NotiDrag extract
(Ascophyllum Nodosum Extract)
Antarctic microbial extract
Mourea fluviatilis extract
water 3.00
0.50
0.50
0.50
5.00

10.00
20.00
to 100 Sum 100

Example 2: Liposome composition containing plant extract

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Wild radish extract
Clown mustache extract
Licorice extract
Aloe extract
water 3.00
0.50
0.50
0.50
5.00
10.00
10.00
5.00
to 100 Sum 100

Example 3: Liposome composition containing oil

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Sunflower oil
Jojoba oil
Almond oil
Apricot seed oil
Green tea oil
Methofoam oil
Argan oil
water 5.00
1.00
1.00
0.50
5.00
5.00
5.00
2.00
2.00
2.00
2.00
to 100 Sum 100

Example 4: Liposome composition containing wax

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Beads wax
Jojoba oil
Candela wax
water 2.00
0.50
0.10
0.50
5.00
5.00
5.00
to 100 Sum 100

Example 5: Liposome composition containing butter

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Plant sterol
Sheer butter
Mango butter
Bean butter
water 5.00
0.01
0.50
1.00
0.01
5.00
5.00
5.00
to 100 Sum 100

Example 6: Hydrocarbon-containing liposome composition

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Liquid paraffin
water 3.00
0.50
0.50
0.50
30.00
to 100 Sum 100

Example 7 Liposome Composition Containing High Fatty Acids

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Stearic acid
water 3.00
0.50
0.50
0.50
10.00
to 100 Sum 100

Example 8: Liposome composition containing ester

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Seven Seven Nuclear Sanoates
Plant snow squalane
water 3.00
0.50
0.50
0.50
10.00
10.00
to 100 Sum 100

<Example 9> Liposome composition containing silicon

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Dimethicone
Cyclomachicone
water 4.00
0.40
0.80
0.03
20.00
10.00
to 100 Sum 100

Example 10 Liposome composition containing moisturizing agent

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Plant sterol
Ceramide
water 5.00
1.00
0.50
1.00
0.01
5.00
to 100 Sum 100

Example 11: Liposome composition containing a whitening agent

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Arbutin
water 3.00
0.50
0.50
0.50
20.00
to 100 Sum 100

Example 12: Liposome composition containing an ultraviolet screening agent

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Octylmethoxycinnamate
water 3.00
0.50
0.50
0.50
20.00
to 100 Sum 100

Example 13 Liposome Composition Containing Vitamins

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Vitamin A (retinol)
Vitamin C
water 1.00
0.50
1.50
0.50
5.00
0.50
to 100 Sum 100

Example 14: Liposome composition containing amino acid

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Cystine
EGF
water 3.00
0.50
0.50
0.50
20.00
0.0001
to 100 Sum 100

Example 15 Liposome composition containing anti-inflammatory agent

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Hydrocortisone
water 3.00
0.50
0.50
0.50
5.00
to 100 Sum 100

Example 16 Liposome composition containing acne treatment agent

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Plant sterol
Azelic acid
water 3.00
0.50
0.50
0.50
0.01
20.00
to 100 Sum 100

Example 17: Liposome composition containing a bactericide

ingredient Content (% by weight) Hydrogeneate lecithin
Phosphatidylcholine
Polysorbate 80
Lysolecithin
Halo Calvan
water 3.00
0.50
0.50
0.50
40.00
to 100 Sum 100

For the liposomes thus prepared, the particle distribution, formation, transdermal absorption promoting effect, skin moisturizing ability and transdermal water loss degree were confirmed through Experimental Examples 1 to 5 below.

<Experimental Example 1> Measurement of particle distribution of liposome

The particle distribution of the liposome of Example 1 was measured using Photal and ELS-Z and is shown in Fig. As a result, it was found that the average diameter of the particles was 273.6 nm as shown in Fig.

Experimental Example 2 Measurement of formation of liposome

The liposome prepared in Example 1 was photographed. Since the particle size of the liposome is too small to be measured by a general optical microscope, it is photographed using a freezing electron microscope and is shown in Fig. As a result, it was found that the liposome was well formed to a uniform size as shown in FIG.

&Lt; Experimental Example 3 >

Retinol-containing penetrating liposomes and general liposomes were prepared by the composition of the following [Table 18].

Retinol-containing penetration liposome Retinol-containing normal liposome Polysorbate 80 1.00 - Hydrogeneate lecithin 3.00 3.00 Lysolecithin 0.50 - Phosphatidylcholine 1.00 - Olive oil 10.00 10.00 Retinol 5.00 5.00 water to 100 to 100

Neoderm (TegoScience), an artificial skin, was attached to a Franz-type diffusion cell (Lab fine instruments, Korea). 50 mM phosphate buffer (pH 7.4, 0.1 M NaCl) was added to the receptor container of Franz-type diffusion cell (5 ml), and diffusion cells were mixed and dispersed at 32 ° C and 600 rpm. Containing penetration liposomes and 50 쨉 l of common liposomes were placed in donor containers. Absorbed and diffused according to the predetermined time, and the skin on which the absorption diffusion occurred was made to be 0.64 cm ² . After absorption diffusion of the active ingredient is completed, the emulsion remaining on the skin is absorbed by the dried kimwipes or 10 ml of ethanol, and the active ingredient is absorbed by using a tip-type homogenizer After spreading the skin, the retinol absorbed into the skin was extracted with 4 ml of dichloromethane. Thereafter, the extract was filtered through a 0.45 탆 nylon membrane filtration membrane, and its content was measured by the HPLC method under the following conditions. The results are shown in Table 19.

- Column: C18 (4.6 x 200 mm, 5 m)

- mobile phase: methanol: hexane = 2: 1

- flow rate: 0.8 ml / min

Detector: UV 275 nm

Percutaneous absorption (㎍) Percutaneous absorption increase rate (%) Retinol-containing penetration liposome 0.3545 51.52 Retinol-containing normal liposome 0.2343 -

As can be seen from the above Table 19, it was confirmed that the penetrating liposome of the present invention can efficiently deliver the active ingredient into the skin.

<Experimental Example 4> Measurement of skin moisturization using liposome

In order to examine the moisturizing effect of the liposome according to the present invention, a lotion cosmetic containing 10% by weight of the liposome of Example 10 was prepared as shown in Table 20 below, and the moisture resistance was measured with a Corneometer CM850.

General Lotion (% by weight) Infiltration Liposome (Example 10) Addition Lotion
(weight%) Polyglycerin-3 stearate / citrate 3.00 3.00 Sheer butter 0.80 0.80 Olive oil 5.00 5.00 Capric / caprylic triglyceride 5.00 5.00 Silicone oil 4.00 4.00 glycerin 5.00 5.00 Carbopol 0.10 0.10 Penetration liposome - 10.00 Ceramide 1.00 - water to 100 to 100

The results are shown in FIG. 3, and as shown in FIG. 3, the moisturizing power of the lotion containing the penetrating liposome of the present invention is superior to that of the lotion not containing the lotion.

<Experimental Example 5> Measurement of transdermal water loss

After applying the lotion containing the common lotion and liposome prepared in the above [Table 20], the transepidermal water loss (TEWL, Trans Epidermal Water Loss) was measured using TEWAMETER TM 250 (Courage + Khazaka electronic GmbH, Germany) The results are shown in Fig. As shown in Fig. 4, the lotion to which the liposome of the present invention is added is a liposome It was found that the skin transdermal water loss was much lower than that of the conventional general lotion not added.

As described above, the liposomes prepared according to the present invention had a particle size of 273.6 nm and showed excellent effects due to penetration into the skin very quickly as a result of the transdermal absorption promotion experiment. As a result of the particle photograph, I could. In addition, it was found that the moisture resistance was also excellent.

The components constituting the composition of the cosmetic composition introduced in the present invention are representative components of the formulations having the characteristics of the respective components and may be replaced with other components having the feature.

Although the present invention has been described in connection with the preferred embodiments set forth above, it will be appreciated that various other modifications and variations can be made without departing from the spirit and scope of the invention, And variations.

Claims (9)

0.01 to 10% by weight of hydrogeneate lecithin, 0.01 to 10% by weight of phosphatidylcholine, 0.01 to 5% by weight of polysorbate 80, 0.01 to 5% by weight of lysolecithin, active ingredient and water in a residual amount, By weight of the liposome composition for promoting percutaneous absorption.
delete The method according to claim 1,
Wherein the active ingredient is contained in an amount of 0.01 to 40% by weight.
The method according to claim 1,
The active ingredient may be at least one selected from the group consisting of natural extracts, oils, moisturizers, whitening agents, wrinkle remedies, acne remedies, atopic emollients, sunscreens, hair restorers, vitamins, amino acids or polypeptides, antiinflammatory agents, , Yeast extract, collagen, elastin, DHA, EPA, ceramide, perfume, and the like.
5. The method of claim 4,
Wherein the oil is at least one selected from the group consisting of fat, wax, hydrocarbon oil, higher fatty acid ester oil, higher alcohol oil, butter and silicone oil.
5. The method of claim 4,
The natural extract is an extract of an animal or plant, a marine animal or a seaweed extract or a component obtained from the extract. The natural extract may be selected from the group consisting of a herbal extract, a clown beard, a white lily, a royal jelly, licorice, aloe, chamomile, rosehip, hinokitiol, maronie, Cucumber extract, seaweed extract, juvenile female, birch sap, or the extract of at least one selected from the group consisting of
Ascophyllum Nodosum Extract from Iceland, deep sea microorganism, Antarctic microorganism, Mourea fluvialis extract, arctic yeast, sea bream sea pomelo (Dulse), picea abies (nidiformis) One or more selected extracts, or
A liposome composition for promoting transdermal absorption, which is a fermented product of Thermus thermophilus.
The method according to claim 1,
Wherein the liposome has a diameter ranging from 100 to 300 nm.
8. A cosmetic comprising the liposome composition for promoting percutaneous absorption according to any one of claims 1 to 7.
9. The method of claim 8,
A cosmetic for enhancing transdermal absorption, characterized by containing 1 to 40% by weight of the liposome composition for promoting percutaneous absorption and absorption.

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