JPH08183726A - Skin preparation for external use - Google Patents

Abstract

PURPOSE: To obtain a skin preparation for the external use, having remarkably excellent humectant effect beautifying and antioxidizing effects. CONSTITUTION: The skin preparation for the external use comprises a liposome- containing aqueous dispersion containing (a) 0.1-5wt.% of a phospholipid and (b) 0.1-5wt.% of cholesterol and/or 5-40wt.% of 1,3-butylene glycol at a (a)/(b) ratio of 1/0.1 to 1/1, and a humectant, a beautifying agent and an antioxidizing agent.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a skin external preparation, and more specifically, it contains a liposome-containing aqueous dispersion composed of specific components, a moisturizing agent, a whitening agent, and an antioxidant. The present invention relates to an external preparation for skin which has remarkably good moisturizing, whitening and antioxidant effects.

[0002]

2. Description of the Related Art Liposomes, which are closed vesicles composed of bilayer membranes of phospholipids, which are the main constituents of biological membranes, have been used for research as a model of biological membranes, and have long been used as microcapsules for pharmaceuticals and cosmetics. Was being attempted. In the cosmetics field, in particular, it has attracted attention because it has a valuable form as a microcapsule, and the phospholipid itself, which is a constituent component of the liposome, is a highly safe amphipathic substance derived from a biological membrane. Was there.

[0003]

There has been an urgent need to develop not only the application of these liposomes to cosmetics but also the function of the liposomes, and the cosmetics and external preparations for skin having remarkable effects which have never been obtained. .

[0004]

Means for Solving the Problems As a result of earnest research, the present inventors have found that a liposome-containing aqueous dispersion composed of specific components, a moisturizing agent, a whitening agent, and an antioxidant are contained.
The inventors have found that an external preparation for skin in which the respective effects are dramatically improved can be obtained, and completed the present invention. That is,
The present invention provides (a) phospholipids 0.1 to 5% by weight, (b)
0.1 to 5% by weight of cholesterol and / or a derivative thereof, (c) glycerin and / or 5 to 40% by weight of 1,3-butylene glycol, and (a):
A skin external preparation characterized in that (b) contains a liposome-containing aqueous dispersion having a ratio of 1: 0.1 to 1: 1 and a specific moisturizing agent, whitening agent, and antioxidant.

Examples of the phospholipid of the component (a) used in the present invention include natural phospholipids such as phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylinositol, lysophosphatidylcholine, sphingomyelin, egg yolk lecithin and soybean lecithin; Synthetic phospholipids such as oleoylphosphatidylcholine, or hydrogenated phospholipids obtained by saturating unsaturated carbon chains of naturally-derived phospholipids with hydrogen, and other phospholipids extracted from microorganisms such as Escherichia coli.
These can be used alone or in combination of two or more.

Among these, one or more selected from hydrogenated soybean phospholipid, hydrogenated egg yolk phospholipid, hydrogenated phosphatidylcholine and hydrogenated phosphatidylserine are preferable, and the compounding amount is 0.1 to 5% by weight (hereinafter , Simply indicated by "%"). If it is less than 0.1%, the liposome production rate will be low, and if it exceeds 5%, gelation will occur, which is not preferable.

Examples of the cholesterol and / or its derivative as the component (b) include cholesterol, cholesteryl stearate, cholesteryl palmitate and the like, and these can be used alone or in combination of two or more kinds.

The blending amount is preferably 0.1 to 5%,
If it is less than 1%, the stability of the liposome will be poor, and if it exceeds 5%, the component (b) will precipitate over time.

Component (c) glycerin and / or 1,3
The amount of butylene glycol is 5-40%. 5
If it is less than 40%, the dispersibility and stability of the liposome will be poor, and if it exceeds 40%, stickiness will occur, which is not preferable in terms of sensory properties.

Further, it is essential that the weight ratio of the component (a) to the component (b) is (a) :( b) = 1: 0.1 to 1: 1. Within this range, a liposome-containing aqueous dispersion having good stability can be obtained.

In the present invention, the liposome-containing aqueous dispersion containing the above components is prepared by a generally known method, for example, the vortexing method (AD Bangham,
J. Mol. Biol. , 13, 238 (196
5)), sonication method (C. Huang, Bioc
hem. , 8, 344 (1969)), a pre-vesicle method (H. Trauble, Neurosci. Res. P.
log. Bull. , 9, 273 (1971)), ethanol injection method (S. Batzri, Biochem. B.
iophys. Acta. , 298, 1015 (197)
3)), French press extrusion method (Y. Barenhol
z, FEBS Lett. , 99, 210 (197
9)), cholic acid removal method (Y. Kawagawa, J. Bi.
ol. Chem. , 246, 5477 (1971)),
Triton X-100 Batch Method (WJ Gerrits
en, Eur. J. Biochem. , 85, 255
(1978)), Ca ²⁺ fusion method (D. Papahado
jopoulos, Biochem. Biophys.
Acta. , 394, 483 (1975)), an ether injection method (D. Deazer, Biochem. Biop.
hys. Acta. , 443, 629 (1976)),
Annealing method (R. Lawaczeck, Bioch
em. Biophys. Acta. , 443, 313
(1976)), a freeze-thaw fusion method (M. Kasahar.
a, J. Biol. Chem. , 252, 7384 (1
977)), W / O / W emulsion method (S. Mats
umoto, J .; Colloid Interface
Sci. , 62, 149 (1977)), reverse phase evaporation method (F. Szoka, Proc. Natl. Acad. S.
ci. USA, 75, 4194 (1978)), polyhydric alcohol method (JP-A-60-7932) and the like.

The amount of the above liposome-containing aqueous dispersion compounded in the external preparation for skin of the present invention is not particularly limited, but is preferably 1.0 to 90%. Furthermore, the external preparation for skin of the present invention can be obtained by using together with a moisturizing agent, a whitening agent and an antioxidant described later.

As the humectant, one kind or two or more kinds selected from hyaluronic acid, collagen and elastin can be appropriately selected and blended. The blending amount of the moisturizer is not particularly limited, but is preferably 0.001 to 5%. When used in this range, the moisturizing effect of the product of the present invention becomes more remarkable.

As the whitening agent, one or more selected from placenta extract, ascorbic acid and its derivatives can be appropriately selected and blended. Examples of the ascorbic acid derivative include L-ascorbyl magnesium phosphate, disodium L-ascorbate sulfate, and ascorbyl dipalmitate. The amount of the whitening agent is not particularly limited, but is preferably 0.0
It is 01 to 5%. When used in this range, the whitening effect of the product of the present invention becomes more remarkable.

As the antioxidant, one or more selected from lactoferrin, malt root extract and mocca extract can be appropriately selected and blended. The blending amount of the antioxidant is not particularly limited, but the dry solid content is preferably 0.0001 to 5%. When used in this range, the antioxidant effect of the product of the present invention becomes more remarkable.

The above moisturizers, whitening agents and antioxidants may be of natural origin, microbial origin or chemically synthesized products, and in the case of natural origin, extraction method and purification treatment method, etc. There is no particular limitation.

The external preparation for skin of the present invention is a moisturizer as described above,
It can be obtained by blending a whitening agent and an antioxidant with the liposome-containing aqueous dispersion described above.
It may be added to and mixed with the prepared liposome-containing aqueous dispersion, or may be added in advance when preparing the liposome-containing aqueous solution.

The external preparation for skin of the present invention comprises, in addition to the above-mentioned essential components, components to be added to the external preparation for skin and cosmetics, for example,
Oil agent, surfactant, powder, pigment, dye, water-soluble polymer,
An ultraviolet absorber, an antiseptic, a fragrance and the like can be added within a range not impairing the effects of the present invention.

[0019]

EXAMPLES Next, the present invention will be described in more detail with reference to examples, but the present invention is not limited to these examples.

Production Examples 1 to 3 and Comparative Production Examples 4 to 6 Liposome-containing aqueous dispersions A liposome-containing aqueous dispersion having the composition shown in Table 1 below was produced.

[0021]

[Table 1]

(Production Method) A: Components 1 to 3 are hydrated with a part of the component 6, and then dispersed in the rest of the component 6. B: A is processed with a microfluidizer. C: Components 4 and 5 are added to B to obtain a liposome-containing aqueous dispersion.

When the aqueous dispersion containing liposomes obtained as described above was observed with a transmission electron microscope, Production Examples 1 to 3 according to the present invention showed better liposome morphology than Comparative Production Examples 4 to 6. And stability was also good.

Examples 1 to 4 and Comparative Examples 1 to 5 Emulsion An emulsion having the composition shown in Table 2 below was produced, and its moisturizing effect was evaluated. The moisturizing effect was evaluated by measuring the amount of keratin water content and the effect of improving desquamation.

[0025]

[Table 2]

(Production Method) A: Components 1 to 5 are heated and mixed to 70 ° C. B: Components 6 to 11 and 15 are heated and mixed to 70 ° C. C: B was added to A and emulsified and mixed, component 12 was added and then cooled, components 13 and 14 were added, and uniformly mixed to obtain an emulsion.

1. Measurement of water content of keratin 54 panels (22 to 54 years old: 6 milk emulsions of each test) in which bilaterally symmetrical rough skin was observed in the test site (forearm) were targeted. An appropriate amount of the test emulsion was applied to the left side of the test site twice daily in the morning and evening, and the right side was not applied, and was used as a control for 4 weeks continuously.
The left and right water contents were measured with CON-200 (manufactured by IBS). The rate of increase in keratin water content of each panel was calculated from the following formula and averaged.

[0028]

Embedded image

2. Scalping improvement effect 54 panelists (22 to 54 years old: 6 test milk emulsions each) were found to have similar scaling in the left and right controls at the test site (extension side of the lower leg). Appropriate amount of test emulsion was applied to the left side of the test site twice daily in the morning and evening, and the right side was not applied as a control, and after 4 weeks of continuous use, the test site was observed and the effect of improving desquamation of the applied part compared to the control was observed. The following criteria were evaluated. (Evaluation Criteria) Effective: Desquamation is clearly inconspicuous. Slightly effective: Scaling became less noticeable. Ineffective: No change. The evaluation results are shown in Table 3.

[0030]

[Table 3]

As is clear from the above results, the emulsion according to the present invention has an excellent effect of retaining keratin water and an effect of improving desquamation, has a remarkable moisturizing effect, and is extremely effective in improving rough skin.

Examples 5 to 8 and Comparative Examples 6 to 9 Creams Creams having the compositions shown in Table 4 below were produced and their whitening effect was evaluated. The evaluation method is shown below.

[0033]

[Table 4]

(Manufacturing Method) A: Components 1 to 7 are mixed by heating to 70 ° C. B: Components 8 to 11 and 14 are heated and mixed to 70 ° C. C: B was added to A, and the mixture was emulsified and mixed, followed by cooling and the component 1
2 and 13 were added and mixed uniformly to obtain a cream.

1. Whitening Effect (A) The whitening effect of the test cream was examined by utilizing the fact that the back of colored guinea pigs was shaved and ultraviolet rays were irradiated to cause pigmentation. Ten colored guinea pigs were used for each cream to be tested, and at four points (2 × 2 ×) on the back of the guinea pig 24 hours before, immediately after, and 24 hours after the ultraviolet irradiation.
2 cm) was thoroughly rubbed with 0.2 ml of the test cream and irradiated. However, the application site was thoroughly washed with warm water before irradiation. For the UV irradiation, FL20S / BLB lamps and FL20S / E30 lamps (each manufactured by Toshiba Corp.) were used to irradiate three of each at the same time, and the UV amount was 4.8 × 1.
It was set to 0 ⁶ erg / cm ² . Each site was observed 7 days after irradiation, and the pigmentation and whitening effect were evaluated according to the following criteria.

(Pigmentation Rating) 0: No pigmentation is observed. 1: Very slight pigmentation is observed. 2: Pigmentation is observed, but the boundary with the non-irradiated site is unclear. 3: Pigmentation was observed, and the boundary with the non-irradiated site was clear.

(Whitening Effect) Guinea pigs with a pigmentation score of 1 point or less 8 out of 10: excellent effect 6 to less than 8 animals: effective 4 to 6 animals: slightly effective 3 or less: ineffective

2. Whitening effect (B) 15 women aged 23 to 44 years were used as a panel, and a test cream was applied twice a day, twice a day, morning and noon, to each person for two weeks, and an appropriate amount of the test cream was applied to the face for 6 weeks. The evaluation was performed according to the following criteria. (Evaluation Criteria) Effective: Spots and freckles disappeared. Slightly effective: Spots and freckles are less noticeable. Ineffective: No change. Table 5 shows the evaluation results.

[0039]

[Table 5]

As is clear from the above results, the cream according to the present invention had an effect of suppressing pigmentation and an excellent whitening effect.

Examples 9 to 12 and Comparative Examples 10 to 13 Creams Creams having the compositions shown in Table 6 below were produced, the lipid peroxide concentration was measured, and the skin beautifying effect and the skin aging preventing effect were evaluated.

[0042]

[Table 6]

(Manufacturing Method) A: Components 1 to 7 are mixed by heating to 70 ° C. B: Components 8 to 12 and 15 are mixed by heating to 70 ° C. C: B is added to A, emulsified and mixed, and after cooling, components 13 and 1
4 was added and mixed uniformly to obtain a cream.

1. Measurement of Lipid Peroxide Concentration The cream obtained as described above was placed in a constant temperature bath at 40 ° C for 4 hours.
After being stored for a week, it was diluted to 1% with purified water to obtain a sample solution. As a reagent, use trichloroacetic acid 15 g, thiobarbituric acid 0.375 g, 1N hydrochloric acid 25 ml and ethanol solution 3 ml containing 2% of butylhydroxyanisole to make 100 ml by adding purified water (hereinafter referred to as TBA reagent). I was there. 1 ml of the sample solution was taken in a test tube, 2 ml of the above-mentioned TBA reagent was added to and mixed with the test tube, the test tube was sealed, heated at 95 ° C. for 15 minutes, and then rapidly cooled to room temperature. Then, after centrifuging at 2500 rpm for 10 minutes, the supernatant liquid is collected and 535 nm
The absorbance of was measured. As a standard solution, 1, 1, 3, 3
-Using tetraethoxypropane solution, the same operation was performed to prepare a calibration curve, and the lipid peroxide concentration was determined from this calibration curve.

2. Beautiful skin and skin aging prevention effect 15 female evaluation panels aged 28 to 58, 2 products for each person, twice daily in the morning and noon twice, for 6 weeks, after washing for 6 weeks, an appropriate amount of the test cream was applied to the face. Was observed. The following criteria evaluated the beautiful skin and the skin aging prevention effect by application.

<Beautiful Skin Effect> (Evaluation) (Contents) Effective: Dullness of the skin is not noticeable. Somewhat effective: The dullness of the skin became less noticeable. Ineffective: No change from before use. <Effect of preventing skin aging> (Evaluation) (Details) Effective: The skin's elasticity and gloss were improved. Slightly effective: The skin's elasticity and gloss were slightly improved. Ineffective: No change from before use. Table 7 shows the evaluation results.

[0047]

[Table 7]

As is clear from the above evaluation results, the cream according to the present invention has antioxidative ability and is excellent in the skin beautifying effect and the skin aging preventing effect.

[0049]

As described above, the external preparation for skin of the present invention contains a liposome-containing aqueous dispersion having a specific composition and various drugs to remarkably improve the effect of each drug. It is extremely useful in beauty and medicine.

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁶ Identification code Office reference number FI technical display area A61K 7/00 X

Claims (9)

[Claims] 1. The following components (a), (b) and (c); (a) phospholipid 0.1 to 5% by weight (b) cholesterol and / or its derivative 0.1 to 5% by weight (c ) Glycerin and / or 1,3-butylene glycol is contained in an amount of 5 to 40% by weight, and (a) :( b) is 1: 0.1 to 1: 1.
An external preparation for skin comprising the liposome-containing aqueous dispersion, which is, and one or more moisturizers selected from hyaluronic acid, collagen, and elastin. 2. The skin according to claim 1, wherein the phospholipid is one or more selected from hydrogenated egg yolk phospholipid, hydrogenated soybean phospholipid, hydrogenated phosphatidylcholine and hydrogenated phosphatidylserine. Topical agent. 3. The content of the moisturizer according to claim 1 is 0.00.
The external preparation for skin according to claim 1, which is 1 to 5% by weight. 4. The following components (a), (b) and (c): (a) Phospholipid 0.1 to 5% by weight (b) Cholesterol and / or its derivative 0.1 to 5% by weight (c ) Glycerin and / or 1,3-butylene glycol is contained in an amount of 5 to 40% by weight, and (a) :( b) is 1: 0.1 to 1: 1.
An aqueous dispersion containing liposomes, which is a placenta extract,
One or two selected from ascorbic acid and its derivatives
A skin external preparation characterized by containing at least one kind of whitening agent. 5. The skin according to claim 4, wherein the phospholipid is one or more selected from hydrogenated egg yolk phospholipid, hydrogenated soybean phospholipid, hydrogenated phosphatidylcholine and hydrogenated phosphatidylserine. Topical agent. 6. The content of the whitening agent according to claim 4 is 0.00.
The external preparation for skin according to claim 4, which is 1 to 5% by weight. 7. The following components (a), (b) and (c); (a) phospholipid 0.1 to 5% by weight (b) cholesterol and / or its derivative 0.1 to 5% by weight (c ) Glycerin and / or 1,3-butylene glycol is contained in an amount of 5 to 40% by weight, and (a) :( b) is 1: 0.1 to 1: 1.
The external preparation for skin comprising the liposome-containing aqueous dispersion which is 1. and one or more antioxidants selected from lactoferrin, malt root extract, and mocca extract. 8. The skin according to claim 7, wherein the phospholipid is one or more selected from hydrogenated egg yolk phospholipid, hydrogenated soybean phospholipid, hydrogenated phosphatidylcholine and hydrogenated phosphatidylserine. Topical agent. 9. The external preparation for skin according to claim 7, wherein the content of the antioxidant according to claim 7 is 0.0001 to 5% by weight as a dry solid content.