JP2008094808A - Vesicle composition and its manufacturing method, and cosmetic comprising vesicle composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a technique for enhancing stability of a vesicle that exhibits excellent stability though having a refreshing feeling without stickiness and causes effective ingredients such as drugs or beautifying components to effectively penetrate into the skin thereby bringing about excellent effects on the skin. <P>SOLUTION: The vesicle composition comprises one or two or more vesicle film-forming substances, selected from among phospholipids, sucrose fatty acid esters and acylamino acid metal salts, and a water-soluble polymer, and is prepared by a vesicle formation treatment under high pressure in the presence of the water-soluble polymer. <P>COPYRIGHT: (C)2008,JPO&INPIT

Description

  The present invention relates to a vesicle composition, a method for producing the same, and a cosmetic composition containing the vesicle composition. More specifically, the vesicle composition is obtained by allowing a vesicle film-forming substance and a water-soluble polymer to be present at the time of vesicle formation and by high-pressure treatment. The present invention relates to a vesicle composition, a method for producing the vesicle composition, and a cosmetic containing the vesicle composition.

  A vesicle composed of a multilayer film of a surfactant can encapsulate active ingredients such as drugs and cosmetic ingredients between the films, and thus has been conventionally used as a cosmetic or the like as a carrier for an active ingredient in a living body. .

  This vesicle is usually prepared by dispersing a vesicle main component and a target drug in a solvent and then sonicating. However, since the vesicle body is composed of a surfactant, the stability of the vesicle itself depends on the intermolecular force of the surfactant. Therefore, the preparation of a vesicle that is easily affected by the external environment and excellent in stability has been desired.

  As a technique for increasing the stability of vesicles, a method using a special surfactant (Patent Document 1), a method using a combination of various surfactants (Patent Document 2), when preparing a vesicle, A method of adding a large amount of water-soluble polymer to the outer phase part of the prepared vesicle (Patent Document 3) has been known.

However, there is still a problem in stability only by using various surfactants in combination, and the method of adding a polymer to the outer phase part has a stickiness peculiar to the polymer in the outer phase part. There was a problem with. Furthermore, as a phenomenon that occurs because the vesicle itself is a surfactant, there is a problem that the stability of the system of the product itself in which the vesicle is blended is deteriorated.
JP 2006-124378 A Japanese Patent Laid-Open No. 7-285827 JP 2001-342108 A

  Therefore, there is no problem in touch such as stickiness during use, the stability of the system can be maintained, and effective ingredients such as drugs and beauty ingredients can be effectively penetrated to bring about a high effect on the skin. There was a need for the development of technology that would increase the stability of vesicles that can be produced.

  As a result of researches to solve the above problems, the present inventors have made a water-soluble polymer present together with a vesicle film-forming substance at the time of vesicle formation, and further prepared by high-pressure treatment, so that the polymer is present in the vesicle. By doing so, the stability of the vesicles will be improved, there will be no stickiness during use, the skin will penetrate into the skin (penetration), the skin will be moisturized (moisturation), and the skin will have a cosmetic effect. As a result, the present invention was completed.

  That is, the present invention provides a vesicle composition comprising one or more vesicle film-forming substances selected from phospholipids, sucrose fatty acid esters and acylamino acid metal salts, and a water-soluble polymer, It is a vesicle composition obtained by forming a water-soluble polymer together with a vesicle film-forming substance at the time of formation and performing high-pressure treatment.

  Moreover, this invention is a vesicle composition combination cosmetics which mix | blends the said vesicle composition.

  Furthermore, the present invention is characterized in that one or more vesicle film-forming substances selected from phospholipids, sucrose fatty acid esters and acylamino acid metal salts and a water-soluble polymer are subjected to high-pressure treatment in an aqueous medium. This is a method for producing a vesicle composition.

  The vesicle composition of the present invention can exist stably even in an external environment in which the stability of the vesicle is poor, such as the presence of an electrolyte or the low viscosity of the outer phase of the vesicle.

  Therefore, the vesicle composition of the present invention and the cosmetics containing the composition are excellent in stability, particularly in a low viscosity region, and have a good feeling that is not sticky and refreshed when applied to the skin. Since the active ingredient is inherently retained, it has excellent storage properties (long-term stability) and sustained release properties, and also has excellent skin penetration and moisturizing properties and skin beauty effects.

  The vesicle composition of the present invention contains a vesicle film-forming substance selected from phospholipids, sucrose fatty acid esters, and acylamino acid metal salts, and a water-soluble polymer.

  There are no particular restrictions on the phospholipid, sucrose fatty acid ester, and acylamino acid metal salt of this film-forming substance, but examples of the phospholipid include egg yolk phospholipid, soybean phospholipid, and hydrogenated products thereof. It is done. The sucrose fatty acid ester is preferably a sucrose fatty acid ester having a C12 to C22 carbon chain, and specific examples include sucrose stearic acid and sucrose lauric acid. The acylamino acid metal salt is preferably an acylamino acid metal salt having a C12 to C22 carbon chain, and specific examples include N-lauroyl-L glutamate sodium and N-stearoyl-L glutamate sodium. These film-forming substances can be used alone or in combination of two or more. Among these, phospholipids are particularly preferred because of their high affinity for the skin.

  Examples of commercially available film-forming substances include hydrogenated soybean phospholipid (manufactured by YMC), DK ester series such as DK ester S-L18A and S-160 (manufactured by Daiichi Kogyo Seiyaku Co., Ltd.), Amisoft HS-11P, etc. And Amisoft series (manufactured by Ajinomoto Co., Inc.). The blending amount of the film-forming substance is preferably from 0.01 to 5% by mass (hereinafter simply expressed as%), particularly preferably from 0.1 to 2%. If it is this range, the stickiness peculiar to surfactant will be reduced and the effect of a vesicle will be exhibited.

  On the other hand, the water-soluble polymer of the present invention is not particularly limited as long as it is generally used in cosmetics and external preparations for skin, and is naturally derived from plants, microorganisms, etc., or is synthetic or semi-synthetic. The xanthan gum, 1,3-1,6-β glucan, carrageenan, methylcellulose, hydroxyethylcellulose, carboxymethylcellulose, carboxyvinyl polymer, acrylic acid / alkyl methacrylate copolymer, poly, etc. Acrylic polymers such as acrylic amide, phospholipid polymers such as hyaluronic acid, collagen, polymethacryloyloxyethylphosphocholine, and the like are used. Among these, xanthan gum, 1,3-1,6-β glucan, hyaluronic acid, collagen, and phospholipid polymer are more preferable.

  Commercially available products of the water-soluble polymer include GRINSTED XANTHAN CLEAR80 (manufactured by DANISCO), CARBOPOL940, 1342 (manufactured by Goodrich Chemical), Sepigel 305 (manufactured by SEPPIC), LIPIDURE HM-600 (manufactured by NOF Corporation). Etc. The amount of the water-soluble polymer is preferably 0.001 to 1%.

  Further, the blend of the film-forming substance and the water-soluble polymer is preferably in the range of mass ratio of 1: 0.005 to 1: 1. If it is this range, the stability of a vesicle is fully maintained and there is little stickiness, and it is preferable.

  The active ingredient contained in the vesicle composition of the present invention is not particularly limited as long as it works effectively on the skin, such as whitening, moisturizing, anti-inflammatory, anti-aging, etc., but L-ascorbyl magnesium phosphate, Ascorbic acids such as glucoside, sodium ascorbate, whitening agents such as arbutin, vitamins, amino acids such as glycerin, 1,3-butylene glycol, glycine, serine, arginine, pyrrolidone carboxylic acid, lactic acid, citric acid, etc. Examples thereof include NMF components such as organic acids, urea and sugar, and moisturizing components.

  Furthermore, the vesicle composition of the present invention can contain water-soluble components such as water, lower alcohol, polyhydric alcohol and the like as an aqueous medium for vesicle formation as appropriate. In addition, for example, oil agents, surfactants, Powders (including pigments), colorants, antioxidants, ultraviolet absorbers, preservatives, fragrances and the like can be blended within a range that does not hinder the effects of the present invention.

  Of these optional ingredients, oils include animal oils, vegetable oils, synthetic oils, etc., hydrocarbons, fats and oils, regardless of their origin, solid oil, semi-solid oil, liquid oil, volatile oil, etc. Waxes, hardened oils, ester oils, fatty acids, higher alcohols, silicone oils, fluorine-based oils, lanolin derivatives, oily gelling agents and the like.

  The surfactant may be any surfactant generally used in cosmetics, and examples thereof include nonionic surfactants, anionic surfactants, cationic surfactants, and amphoteric surfactants.

  The vesicle composition of the present invention is prepared using the above components. At the time of vesicle preparation, a water-soluble polymer is present together with a vesicle film-forming substance, and these are subjected to high-pressure treatment, so that the polymer is contained in the vesicle. Make it inherent.

  Specifically, a mixed liquid containing a vesicle film-forming substance and a water-soluble polymer is introduced into a flow path in a chamber under pressure, and the mixed liquid is applied to a flat portion in the flow path under high pressure. It is made to collide or it is made to disperse | distribute by making this mixture collide in the said flow path under high pressure. By performing the high-pressure treatment in this manner, the stability of the vesicle composition itself and the stability of the vesicle composition-containing cosmetic using the vesicle composition can be enhanced.

  The high-pressure treatment method is described in, for example, Japanese Patent Application Laid-Open No. 2000-26240, and the equipment used therefor has a general high-pressure homogenizer structure that performs dispersion and pulverization using high shearing force and impact force. Any ultrahigh pressure homogenizer can be used as long as the pressure can be adjusted and a pressure of 70 MPa or more can be applied.

  Examples of the ultra-high pressure homogenizer include a microfluidizer (manufactured by Mizuho Kogyo Co., Ltd.), an optimizer (manufactured by Sugino Machine Co., Ltd.) and the like.

  The pressure at the time of producing the vesicle composition of the present invention by the high-pressure treatment is about 70 to 300 MPa, preferably about 100 to 200 MPa, and the temperature and time are the type and size of equipment, the vesicle composition to be prepared, It can be set as appropriate depending on the amount of cosmetic.

  The vesicle composition thus obtained has the following excellent properties.

The vesicle composition of the present invention is stable even in an external environment where the stability of the vesicle is poor in the presence of an electrolyte or in a low viscosity of the outer phase of the vesicle due to the combination with a water-soluble polymer. It is possible to form a low-viscosity preparation such as a lotion with excellent stability, particularly in a low-viscosity region.
The vesicle composition obtained by the method of the present invention is not sticky and refreshed when applied, but the active ingredient is retained in the vesicle, so that its storage property (long-term stability), sustained release It has excellent properties and has a high permeation feeling and moisturizing feeling on the skin and a beauty effect on the skin.

  Therefore, active ingredients such as drugs and cosmetic ingredients are permeated and stored in the stratum corneum, and gradually released to maintain the effects of the active ingredients and to provide a higher effect on the skin and for external use on the skin. It can be advantageously used as an agent.

  EXAMPLES Next, although an Example is given and this invention is demonstrated in more detail, this invention is not restrict | limited at all by these Examples.

Example 1
A vesicle composition was prepared according to the formulation shown in Table 1 below and the following production method. About the obtained vesicle composition, stability, the retention property (retention rate) of the active ingredient, viscosity, non-stickiness, penetration feeling, and moisturizing feeling were evaluated by the following methods and criteria. The results are also shown in Table 1.

<Stability>
(Evaluation methods)
After preparing the sample, it was stored in a constant temperature bath at 40 ° C. for one month, and the presence and shape of vesicles were observed with a transmission electron microscope.
(Criteria)
A: The presence of vesicles was confirmed.
○: The presence of vesicles was confirmed, but some were slightly deformed.
Δ: It was confirmed that the vesicle was considerably deformed.
X: The presence of vesicles was not confirmed.

<Retention of active ingredients (retention rate)>
(Evaluation methods)
As the retention of the active ingredient, the amount of VC-PMG contained in the vesicle composition of L-ascorbyl magnesium phosphate (VC-PMG), which is the active ingredient in the sample of Example 1, was 1 at 40 ° C. Comparison was made after months of storage.
The amount of VC-PMG contained in the vesicle composition at the beginning of the preparation was expressed as the amount after storage at 40 ° C. for 1 month when the amount of VC-PMG was 100%, and was defined as the retention (retention rate) of the active ingredient.
(Criteria)
◎: Hold 80% or more ○: Hold 70% to less than 80% △: Hold 60 to less than 70% ×: Less than 60%

<Viscosity>
(Measuring method)
After sample preparation, the sample was placed in a constant temperature bath at 25 ° C. and measured with a B-type viscometer the next day.

<No stickiness>
(Evaluation methods)
Using a panel of 15 cosmetics, after washing the face, an appropriate amount of the sample was applied directly to the face, and the non-stickiness immediately after application was evaluated.
(Criteria)
◎: Decided that 12 or more people are not sticky ○: Decided that 8 to 11 or more people were not sticky △: Decided that 5 to 7 people were not sticky ×: 4 or less people judged to be non-sticky

<Permeation>
(Evaluation methods)
Using a panel of 15 cosmetics, after washing the face, an appropriate amount of the sample was applied directly to the face, and the feeling of penetration of the sample into the skin 30 minutes after application (penetration feeling) was evaluated.
(Criteria)
◎: Determined that 12 or more people felt a penetration feeling ○: Determined that 8 to 11 or more people felt a penetration feeling △: Determined that 5-7 persons felt a penetration feeling ×: Person determined to have felt a penetration feeling 4 or less

<Moisturizing feeling>
(Evaluation methods)
Using a panel of 15 cosmetics, after washing the face, an appropriate amount of the sample was applied directly to the face, and the skin 30 minutes after application was moist and moisturized (moisturizing feeling) was evaluated.
(Criteria)
A: Determined that 12 or more persons felt a moisturizing feeling. ○: Determined that 8 to 11 persons felt a moisturizing feeling. △: Determined that 5 to 7 persons felt a moisturizing feeling. X: 4 persons determined to have felt a moisturizing feeling. Below

(Production method)
In the production methods A to C, component B is prepared by previously dispersing with a homogenizer * 1.
Manufacturing method
1. Disperse A with a homogenizer * 1 (75 ° C. for 2 minutes).
Add B to 2.1 and disperse with a homogenizer (75 ° C. for 2 minutes).
Add C to 3.2 and disperse with a homogenizer (75 ° C., 3 minutes).
Slowly cool 4.3 to 40 ° C.
Disperse 5.4 with a high-pressure emulsifier microfluidizer * 2.

Production method B (mixed after preparation of water-soluble polymer vesicles):
1. Disperse A with a homogenizer (75 ° C. for 2 minutes).
Add C to 2.1 and disperse with a homogenizer (75 ° C. for 3 minutes).
Slowly cool 3.2 to 40 ° C.
Disperse 4.3 with a high-pressure emulsifier microfluidizer.
Add B to 5.4 and disperse with a homogenizer (75 ° C. for 2 minutes).

Manufacturing method C (prepared with normal emulsification equipment):
1. Disperse A with a homogenizer (75 ° C. for 2 minutes).
Add B to 2.1 and disperse with a homogenizer (75 ° C. for 2 minutes).
Add C to 3.2 and disperse with a homogenizer (75 ° C. for 3 minutes).
Slowly cool 4.3 to 40 ° C.
Disperse 5.4 with a homogenizer.
* 1 and 2 are both manufactured by Mizuho Kogyo Co., Ltd.

  As is apparent from Table 1, the vesicle composition of the present invention has a high vesicle stability and good retention of L-ascorbyl phosphate, which is an active ingredient, despite its very low viscosity. It was. In addition, there was no stickiness and the skin permeation and moisturization were also excellent.

Example 2
A vesicle composition was prepared according to the formulation shown in Table 2 below and the following production method. About the obtained vesicle composition, it carried out similarly to Example 1, and evaluated the stability of the vesicle, the storage property (retention rate) of an active ingredient, a viscosity, non-stickiness, a penetrating feeling, and a moisturizing feeling. The results are also shown in Table 2.

(Production method)
In Production Methods 2 to F, Component B is prepared by dispersing with a homogenizer * 1 in advance.
Production method II:
1. Disperse A with a homogenizer * 1 (75 ° C. for 2 minutes).
Add B to 2.1 and disperse with a high-pressure emulsifier Optimizer * 3 (75 ° C. for 2 minutes).
Add C to 3.2 and disperse with a homogenizer (75 ° C., 3 minutes).
Slowly cool 4.3 to 40 ° C.
Disperse 5.4 with a homogenizer.

Manufacturing method E (water-soluble polymer blended after vesicle preparation):
1. Disperse A with a homogenizer (75 ° C. for 2 minutes).
Add C to 2.1 and disperse with a homogenizer (75 ° C. for 3 minutes).
Slowly cool 3.2 to 40 ° C.
Disperse 4.3 with a high pressure emulsifier optimizer.
Add B to 5.4 and disperse with a homogenizer (75 ° C. for 2 minutes).

Manufacturing method (prepared with a normal emulsifier):
1. Disperse A with a homogenizer (75 ° C. for 2 minutes).
Add B to 2.1 and disperse with a homogenizer (75 ° C. for 2 minutes).
Add C to 3.2 and disperse with a homogenizer (75 ° C. for 3 minutes).
Slowly cool 4.3 to 40 ° C.
Disperse 5.4 with a homogenizer.
* 3 Made by Sugino Machine

  As is apparent from Table 2, the vesicle composition of the present invention has high vesicle stability and good storage properties (retention rate) of L-ascorbyl magnesium phosphate, which is an active ingredient, despite its low viscosity. Met. In addition, there was no stickiness and the skin permeation and moisturization were also excellent.

Example 3
A vesicle composition-containing cosmetic was prepared according to the formulation shown in Table 3 below and the following production method. About the obtained vesicle composition-containing cosmetic, stability and retention of active ingredients (retention rate) were the same as in Example 1 except that the storage temperature was changed from 40 ° C. to 50 ° C. in the stability evaluation method. Viscosity, non-stickiness, penetrating feeling and moisturizing feeling were evaluated. The results are also shown in Table 3.

(Production method)
In the production method, the component B is prepared by dispersing in advance using a homogenizer * 1.
Manufacturing method:
1. Disperse A with a homogenizer * 1 (75 ° C. for 2 minutes).
Add B to 2.1 and disperse with a homogenizer (75 ° C. for 2 minutes).
Add C to 3.2 and disperse with a homogenizer (75 ° C. for 3 minutes).
Slowly cool 4.3 to 40 ° C.
Disperse 5.4 with a high-pressure emulsifier microfluidizer * 2 to prepare a vesicle composition.
Add D to H to 6.5 and disperse with a homogenizer.

Manufacturing method h (water-soluble polymer blended after vesicle preparation):
1. Disperse A with a homogenizer (75 ° C. for 2 minutes).
Add C to 2.1 and disperse with a homogenizer (75 ° C. for 3 minutes).
Slowly cool 3.2 to 40 ° C.
Disperse 4.3 with a high-pressure emulsifier microfluidizer.
Add B to 5.4 and disperse with a homogenizer. (75 ° C. for 2 minutes).
Add D to H to 6.5 and disperse with a homogenizer.

Manufacturing method (prepared with normal emulsification equipment):
1. Disperse A with a homogenizer (75 ° C. for 2 minutes).
Add B to 2.1 and disperse with a homogenizer. (75 ° C. for 2 minutes).
Add C to 3.2 and disperse with a homogenizer. (75 ° C. for 3 minutes).
Slowly cool 4.3 to 40 ° C.
Disperse 5.4 with a homogenizer.
Add D to H to 6.5 and disperse with a homogenizer.

  As is apparent from Table 3, the vesicle composition-containing cosmetic of the present invention had high stability and good retention of L-ascorbyl magnesium phosphate, which is an active ingredient, despite its low viscosity. . Moreover, it was a good cosmetic product with a refreshing feel without stickiness and excellent skin permeation and moisturizing feeling.

  Since the vesicle composition of the present invention is excellent in stability even in the presence of an electrolyte or in an environment where the viscosity of the vesicle outer phase is low, the active ingredient is not sticky and refreshing when applied. Since it is held inside, it has excellent storage properties (long-term stability) and sustained release properties.

Therefore, active ingredients such as drugs and cosmetic ingredients can penetrate and store in the stratum corneum, and can be gradually released, so that the effect of active ingredients is maintained and the aim is to bring higher effects on the skin. It can be advantageously used as a cosmetic or an external preparation for skin.
more than

Claims (8)

  A vesicle composition comprising one or more vesicle film-forming substances selected from phospholipids, sucrose fatty acid esters, and acylamino acid metal salts, and a water-soluble polymer, which is water-soluble during vesicle formation. A vesicle composition obtained by the presence of a functional polymer and high-pressure treatment.   The vesicle composition according to claim 1, wherein the water-soluble polymer is selected from xanthan gum, 1,3-1,6-β glucan, acrylic polymer, hyaluronic acid, collagen, and phospholipid polymer.   The vesicle composition according to claim 1 or 2, wherein the amount of the vesicle film-forming substance is 0.01 to 5% by mass.   The vesicle composition according to any one of claims 1 to 3, wherein the amount of the water-soluble polymer is 0.001 to 1% by mass.   The vesicle composition according to any one of claims 1 to 4, wherein the vesicle film-forming substance and the water-soluble polymer are mixed in a mass ratio of 1: 0.005 to 1: 1. .   The vesicle composition according to any one of claims 1 to 5, wherein the high-pressure treatment is performed at a pressure of 70 to 300 MPa.   A vesicle composition-containing cosmetic comprising the vesicle composition according to any one of claims 1 to 6.   A vesicle composition characterized by subjecting one or more vesicle film-forming substances selected from phospholipids, sucrose fatty acid esters and acylamino acid metal salts to water-soluble polymers and high-pressure treatment in an aqueous medium. Production method.