CN103800207A - Glycolic acid lipid particle and preparation method thereof - Google Patents
Glycolic acid lipid particle and preparation method thereof Download PDFInfo
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- CN103800207A CN103800207A CN201410036625.3A CN201410036625A CN103800207A CN 103800207 A CN103800207 A CN 103800207A CN 201410036625 A CN201410036625 A CN 201410036625A CN 103800207 A CN103800207 A CN 103800207A
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Abstract
The invention discloses a glycolic acid lipid particle and a preparation method thereof. The glycolic acid lipid particle is prepared from the following raw materials in percentage by weight: glycolic acid 2-8%, an emulsifier 12-18%, a lipid material 25-45%, and deionized water as balance, wherein the emulsifier is at least two compounds selected from polyethylene glycol-30-dipolyhydroxystearate, polyglycerol-2-dipolyhydroxystearate, span, polyoxyethylene-21-stearate, tween and PEG-23-lauryl ether; the lipid material is selected from glyceryl monostearate, glyceryl monolaurate and glyceryl monocaprate. The glycolic acid lipid particle disclosed by the invention has the advantages of good stability, water solubility and low irritation, and can be used in preparation of glycolic acid cosmetics; the preparation method is simple and controllable, and has good repeatability.
Description
Technical field
The invention belongs to the carrier system technical field in cosmetics technology of preparing, relate to a kind of liposome take glycolic acid as active component and preparation method thereof.
Background technology
Glycolic acid has another name called glycolic, is Alpha-hydroxy acids material, is mainly gone out by extraction in Caulis Sacchari sinensis.Glycolic acid is the fruit acid of molecular weight minimum, and skin is had to splendid affinity, can reach remarkable moistening effect by deep enough skin.
Glycolic acid can come off by accelerated ageing horn cell, removes and piles up cutin, promotes epithelial cell metabolic speed, promotes skin to upgrade, and improves pigmentation or abnormal after hyperkeratosis, coarse obscure, black speck and inflammation, makes skin become smooth bright.Simultaneously glycolic acid can make pore around keratinization thromboembolism be easy to come off, and unimpeded follicular canal, effectively prevents that pore from stopping up, and then improves the symptom such as acne, corse sweat pore.
Improving aspect aging skin, glycolic acid be because stimulating hypertrophy and the rearrangement of intradermal hyaluronic acid, acid mucus polysaccharide, collagen protein and elastic fiber, makes skin-tightening and high resilience significantly reduces microgroove and wrinkle.Meanwhile, the increase of hyaluronic acid can promote skin self water holding capacity, can solve scaly dry skin problem.
Therefore in the market, glycolic acid is often applied to skin protection and changes in skin product, reaching moisturizing, skin care, promotion epidermal renewal effect, and effectively solves at short notice the problems such as skin aging, wrinkle, black speck, skin sore.But glycolic acid more directly penetrates to the skin compared with deep layer because of molecular weight, and even in skin corium, then directly affects basal layer cell metabolism, therefore tend to produce twinge and the sensation such as scorching hot while use.And glycolic acid addition is higher, corresponding zest is larger, and concurrent degree of inflammation is more serious.
At present, research worker adopts carrier technique one after another both at home and abroad, develops as carrier transportation systems such as W/O/W type multiple emulsion, liposome, microcapsules for water-soluble active ingredient.Active component is embedded in interior phase by W/O/W type multiple emulsion, has the advantages such as the active component stability of raising, slow-releasing, targeting, but multiple emulsion is thermodynamic unstable system because easily there is between formula ripening difficult to understand and interior foreign minister transmission etc.In conjunction with adopting solid lipid embedding active component thinking in solid lipid nanoparticle technology, replace the liquid fatty in traditional W/O/W type multiple emulsion with solid lipid, can effectively pin interior phase, stop that foreign minister infiltrates and avoids formula ripening difficult to understand, improve to a certain extent system stability, therefore the present invention therefore.Utilize the present invention to be conducive to avoid dissociate in a large number glycolic acid directly with contact skin and its zest that reduces, simultaneously because of carrier slow-releasing with controlled capability is conducive to control the release of glycolic acid and in epidermis concentration, ensure that glycolic acid brings into play effect.
Summary of the invention
The object of the invention is to provide a kind of stability high, good water solubility, bland glycolic acid liposome, the problems such as the zest height that in solution prior art, glycolic acid exists.And the glycolic acid liposome of preparation can conveniently make an addition in cosmetics.
In order to solve these problems of the prior art, technical scheme provided by the invention is:
A kind of glycolic acid liposome, its supported active composition is glycolic acid, it is characterized in that described liposome counts by the mass percent of its raw material components:
Preferred technical scheme is: described glycolic acid lipid particles composition is counted by its percentage by weight:
Preferred technical scheme is: described glycolic acid lipid particles composition is counted by its percentage by weight:
Preferred technical scheme is: described glycolic acid lipid particles composition is counted by its percentage by weight:
Preferred technical scheme is: described the first emulsifying agent is selected from the one or more kinds of combination in any in Polyethylene Glycol-30-dimerization hydroxy stearic acid ester, Dehymuls PGPH Polyglycerin 12-hydroxystearate, sorbester p17.
Preferred technical scheme is: described the second emulsifying agent is selected from the one or more kinds of combination in any in the stearic alcohol ether of polyoxyethylene (21), Tween 80, polyoxyethylene (23) lauryl alcohol.
Preferred technical scheme is: described matrix material is selected from the one or more kinds of combination in any in glyceryl monostearate, glyceryl monolaurate, Capmul MCM C10.
Preferred technical scheme is: the particle size range of described glycolic acid liposome is at 300～500nm.
Another object of the present invention is to provide a kind of method of preparing described glycolic acid liposome, it is characterized in that said method comprising the steps of:
(1) take the first emulsifying agent and matrix material by formula proportion, the first emulsifying agent and matrix material heating are mixed, obtain liquid oil phase.
(2) take glycolic acid and deionized water by formula proportion, after mix homogeneously, obtain water.
(3) under preset temperature, water is added in oil phase, stir 5～10min, control mixing speed at 200～500r/min, obtain clear W/O emulsion, then W/O emulsion is cooled to room temperature;
(4) take the second emulsifying agent by formula proportion, under preset temperature, the second emulsifying agent is added in the W/O emulsion of step (3) gained, stir 10～30min, control rate, at 300～800r/min, is cooled to room temperature and can obtains described glycolic acid liposome.
Preferred technical scheme is: in described method, preset temperature is 60～75 ℃.
Another object of the present invention is to provide a kind of described glycolic acid liposome in the application of preparing aspect skin protection cosmetics.
The glycolic acid liposome that the present invention obtains, can be good at being scattered in water.Principle of the present invention is in conjunction with multiple emulsion and solid lipid nanoparticle technology of preparing, these two kinds of technology are applied to water-soluble active ingredient embedding, effectively solve traditional multiple emulsion thermodynamic instability and solid lipid nanoparticle and be difficult to occluded water soluble components problem.The liposome good stability that adopts two step emulsion process technologies of preparing to utilize solid lipid embedding glycolic acid to obtain, and can effectively reduce the zest of glycolic acid.
Glycolic acid liposome structure of the present invention is similar to traditional W/O/W type multiple emulsion, and difference is that the present invention adopts solid lipid but not liquid lipid, exist solidify after in be squeezed and deformation mutually.Glycolic acid liposome structure of the present invention and conventional solid lipid nanoparticle something in common are all to adopt solid lipid to realize embedding, difference is that conventional solid lipid nanoparticle is for load fat-soluble active ingredient, and glycolic acid liposome structure of the present invention has but realized the embedding of water-soluble components glycolic acid.Glycolic acid liposome of the present invention has that stability is high, active component does not leak, can occluded water soluble components, and the advantage such as interior phase particle diameter is stable.
With respect to the defect of prior art, advantage of the present invention is:
1, preparation process condition of the present invention is controlled, can be by regulating mixing speed and mixing time to prepare weight percent content at 2～8% glycolic acid liposome.
2, the glycolic acid liposome good stability that prepared by the present invention, room temperature ,-4 ℃ and 40 ℃ preserve 1 year above not stratified, dilute 10 times after under high speed centrifugation condition (10000r/min) centrifugal 10min there is not lamination.
3, the glycolic acid liposome pH that prepared by the present invention, 2～3, is positioned at glycolic acid performance optimal efficacy pH scope.
4, the present invention can effectively reduce the stimulation of glycolic acid, can be applicable to cosmetic industry, is added in cosmetic formulations, gives full play to glycolic acid effect, to reach the effect of long-time cosmetology.
5, preparation process of the present invention is simple and convenient, and repeatability is high.
Accompanying drawing explanation
Below in conjunction with drawings and Examples, the invention will be further described:
Fig. 1 is the preparation method flow chart of glycolic acid liposome of the present invention;
Fig. 2 is the structural representation of microparticulate after water; Wherein (a) is that traditional W/O/W type multiple emulsion, (b) are conventional solid lipid nanoparticle (b); (c) the glycolic acid liposome obtaining for the present invention.
The specific embodiment
Below in conjunction with specific embodiment, such scheme is described further.Should be understood that these embodiment are not limited to limit the scope of the invention for the present invention is described.The implementation condition adopting in embodiment can be done further adjustment according to the condition of concrete producer, and not marked implementation condition is generally the condition in normal experiment.
The preparation of embodiment 1 glycolic acid liposome
In the present embodiment, the composition of raw materials of glycolic acid liposome is:
Concrete preparation method is as follows:
1, take 28 grams of Polyethylene Glycol-30-dimerization hydroxy stearic acid esters, 24 grams of capric acid list glyceride, 12 grams of glyceryl monostearate heating obtain oil phase after mixing.
2, take 8 grams of glycolic acid, 8 grams of deionized waters, after stirring, obtain water
3, water is slowly joined in oil phase, at 65 ℃, stir 10min, control rate, at 300r/min, obtains clear emulsion, and is cooled to room temperature.
4, take 20 grams of polyoxyethylene (23) lauryl alcohol, added in the solid-state system of step (3) gained, at 65 ℃, stir 30min, control rate is at 500r/min.Then be cooled to room temperature and obtain glycolic acid liposome.
5, the glycolic acid liposome of gained being recorded to its particle diameter by photon correlation spectroscopy (PCS) is 320.12nm.
The preparation of embodiment 2 glycolic acid liposomes
In the present embodiment, the composition of raw materials of glycolic acid liposome is:
Concrete preparation method is as follows:
1, take 20 grams of Dehymuls PGPH Polyglycerin 12-hydroxystearates, 20 grams of single capric acid glyceride, 10 grams of glyceryl monostearate heating obtain oil phase after mixing.
2, take 4 grams of glycolic acid, 26 grams of deionized waters, after stirring, obtain water
3, water is slowly joined in oil phase, at 65 ℃, stir 10min, control rate, at 300r/min, obtains clear emulsion, and is cooled to room temperature.
4, take the stearic alcohol ether of 20 grams of polyoxyethylene (21), added in the solid-state system of step (3) gained, at 65 ℃, stir 30min, control rate is at 500r/min.Then be cooled to room temperature and obtain glycolic acid liposome.
5, the glycolic acid liposome of gained being recorded to its particle diameter by photon correlation spectroscopy (PCS) is 358.71nm.
The preparation of embodiment 3 glycolic acid liposomes
In the present embodiment, the composition of raw materials of glycolic acid liposome is:
Concrete preparation method is as follows:
1, take 28 grams of sorbester p17s, 24 grams of glyceryl monolaurates, 12 grams of glyceryl monostearate heating obtain oil phase after mixing.
2, take 2 grams of glycolic acid, 22 grams of deionized waters, after stirring, obtain water
3, water is slowly joined in oil phase, at 65 ℃, stir 10min, control rate, at 300r/min, obtains clear emulsion, and is cooled to room temperature.
4, take 12 grams of Tween 80s, added in the solid-state system of step (3) gained, at 65 ℃, stir 30min, control rate is at 500r/min.Then be cooled to room temperature and obtain glycolic acid liposome.
5, the glycolic acid liposome of gained being recorded to its particle diameter by photon correlation spectroscopy (PCS) is 482.39nm.
Structural change comparative result after being illustrated in figure 2 glycolic acid liposome that traditional W/O/W type multiple emulsion, conventional solid lipid nanoparticle and the present invention obtain and being dispersed in water; Wherein (a) is glycolic acid W/O/W type multiple emulsion; (b) be glycolic acid solid lipid nanoparticle; (c) be glycolic acid liposome.
As can be seen from Figure 2, glycolic acid liposome structure of the present invention, exists structural difference with traditional W/O/W type multiple emulsion, solid lipid nanoparticle; Glycolic acid liposome structure of the present invention is similar to traditional W/O/W type multiple emulsion, and difference is that the present invention adopts solid lipid but not liquid lipid, exist solidify after in be squeezed and deformation mutually.Glycolic acid liposome structure of the present invention and conventional solid lipid nanoparticle something in common are all to adopt solid lipid to realize embedding, difference is that conventional solid lipid nanoparticle is for load fat-soluble active ingredient, and glycolic acid liposome structure of the present invention has but realized the embedding of water-soluble components glycolic acid.Such glycolic acid liposome structure has the concomitant advantage of W/O/W type multiple emulsion and solid lipid nanoparticle, and has abandoned corresponding defect.
Particularly, glycolic acid liposome of the present invention has multiple emulsion similar structures, but difference be adopt be solid lipid, multiple emulsion is liquid fatty.The present invention is in fact a kind of new structure, is on the basis of multiple emulsion, uses for reference solid lipid nanoparticle, utilizes solid lipid high-melting-point characteristic, is all comparatively stable as long as storing temperature is no more than lipid fusing point system; In addition, the unstable transmission being also between interior foreign minister of multiple emulsion, interior phase can transfer to foreign minister by liquid fat, causes active component to reveal; Foreign minister also can enter interior phase by liquid fat, causes interior phase particle diameter to increase, and oil layer attenuation is even broken and system is unstable; And adopt solid lipid this transmission capable of blocking, ensure the stability of system.Also it should be noted that solid lipid nanoparticle is directly dissolved in active component in oils and fats and carries out in the preparation, what that is to say its realization is the embedding to liposoluble constituent, and glycolic acid is water-soluble components, therefore solid lipid nanoparticle can not be used for glycolic acid embedding.
Above-mentioned example is only explanation technical conceive of the present invention and feature, and its object is to allow person skilled in the art can understand content of the present invention and implement according to this, can not limit the scope of the invention with this.All equivalent transformations that spirit is done according to the present invention or modification, within all should being encompassed in protection scope of the present invention.
Claims (8)
1. a glycolic acid liposome, its supported active composition is glycolic acid, it is characterized in that described liposome counts by the mass percent of its raw material components:
2. glycolic acid liposome according to claim 1, is characterized in that described the first emulsifying agent is selected from the one or more kinds of combination in any in Polyethylene Glycol-30-dimerization hydroxy stearic acid ester, Dehymuls PGPH Polyglycerin 12-hydroxystearate, sorbester p17.
3. glycolic acid liposome according to claim 1, is characterized in that described the second emulsifying agent is selected from the one or more kinds of combination in any in the stearic alcohol ether of polyoxyethylene (21), Tween 80, polyoxyethylene (23) lauryl alcohol.
4. glycolic acid liposome according to claim 1, is characterized in that described matrix material is selected from the one or more kinds of combination in any in glyceryl monostearate, glyceryl monolaurate, Capmul MCM C10.
5. glycolic acid liposome according to claim 1, is characterized in that the particle size range of described glycolic acid liposome is at 300～500nm.
6. a method of preparing the glycolic acid liposome described in claim 1～5 any one, is characterized in that said method comprising the steps of:
(1) take the first emulsifying agent and matrix material by formula proportion, the first emulsifying agent and matrix material heating are mixed, obtain liquid oil phase.
(2) take glycolic acid and deionized water by formula proportion, after mix homogeneously, obtain water.
(3) under preset temperature, water is added in oil phase, stir 5～10min, control mixing speed at 200～500r/min, obtain clear W/O emulsion, then W/O emulsion is cooled to room temperature;
(4) take the second emulsifying agent by formula proportion, under preset temperature, the second emulsifying agent is added in the W/O emulsion of step (3) gained, stir 10～30min, control rate, at 300～800r/min, is cooled to room temperature and can obtains described glycolic acid liposome.
7. according to the method for claim 6, it is characterized in that in described method, preset temperature is 60～75 ℃.
8. the glycolic acid liposome described in claim 1～5 any one is in the application of preparing aspect skin protection cosmetics.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101486794B1 (en) * | 2014-07-24 | 2015-01-28 | 박희준 | Cosmetic effective in relaxation of striae distensae containing nano liposome glycolic acid |
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| US6096327A (en) * | 1998-11-05 | 2000-08-01 | Protease Sciences Inc. | Cosmetic compositions containing human type serine protease inhibitors for revitalizing the skin |
| CN102688151A (en) * | 2012-06-05 | 2012-09-26 | 东南大学 | Tanshinone microemulsion and preparation method thereof |
| CN102871936A (en) * | 2012-11-05 | 2013-01-16 | 上海相宜本草化妆品股份有限公司 | Nano-carrier loaded with rhodiola rosea extract and preparation method and application thereof |
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Patent Citations (3)
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| US6096327A (en) * | 1998-11-05 | 2000-08-01 | Protease Sciences Inc. | Cosmetic compositions containing human type serine protease inhibitors for revitalizing the skin |
| CN102688151A (en) * | 2012-06-05 | 2012-09-26 | 东南大学 | Tanshinone microemulsion and preparation method thereof |
| CN102871936A (en) * | 2012-11-05 | 2013-01-16 | 上海相宜本草化妆品股份有限公司 | Nano-carrier loaded with rhodiola rosea extract and preparation method and application thereof |
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| P. PERUGINI，ET AL: "Study on glycolic acid delivery by liposomes and microspheres", 《INTERNATIONAL JOURNAL OF PHARMACEUTICS》 * |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| KR101486794B1 (en) * | 2014-07-24 | 2015-01-28 | 박희준 | Cosmetic effective in relaxation of striae distensae containing nano liposome glycolic acid |
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