CN1443529A - Liposome enveloping fruit acid, its preparation method and application - Google Patents
Liposome enveloping fruit acid, its preparation method and application Download PDFInfo
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- CN1443529A CN1443529A CN 03114221 CN03114221A CN1443529A CN 1443529 A CN1443529 A CN 1443529A CN 03114221 CN03114221 CN 03114221 CN 03114221 A CN03114221 A CN 03114221A CN 1443529 A CN1443529 A CN 1443529A
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- liposome
- fruit acid
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Abstract
The present invention relates to fruit acids and phospholipids of chemical field, in particular, it relates to a liposome for enclosing fruit acid, its preparation method and application in preparation of skin-protecting product. Its preparation method includes the following steps: (1) dissolving soya bean lecithin and cholesterol in a solvent, making reduced pressure evaporation to form a layer of lipoid film; (2). adding solvent to dissolve lipoid film and adding phosphate buffer solution containing fruit acid, uniformly mixing them to form stable single-phase system; and (3). reducing pressure, forming water suspension liquor and separating to obtain the liposome enclosing fruit acid. Said liposome enclosing fruit acid can be used as main component of skin-protecting product.
Description
Technical field
The present invention relates to the fruit acid and the phospholipid of chemical field, seal liposome and preparation method thereof the application in the preparation skin care item of fruit acid specifically.
Liposome is that phospholipid is dispersed in the multilamellar vesicle that forms in the water, and its each layer is bilayer, is separated by water between each layer.By the liposome that natural component is formed, the double-decker of its film is the same with the natural fine after birth in principle, so liposome is called artificial membrane again.
Liposome mainly is made of phospholipid and cholesterol.Phospholipid is prevalent in the protoplasm and biomembrane of animal and plant cells, is one of main component that constitutes cell membrane, and the homergy of biomembranous physiologically active and body is had important regulatory function.The mixture that phospholipid is made up of lecithin, cephalin, inositol, serinephosphatide, free fatty etc.Wherein phosphatidylcholine (PC) is the main phospholipid constituent of many cell membrane, the PC of natural origin is a kind of mixture, each PC has different length, the aliphatic chain of different saturation, the aliphatic chain of vegetalitas PC has the height unsaturation, and the aliphatic chain major part of animality PC is saturated.Though saturated aliphatic chain can strengthen the robustness and the impermeability of liposome membrane, can not lower even biochemical reaction that prevention is relevant with film.And be the film material with the soybean lecithin, have good flowability and permeability, the not only favourable surface barrier that penetrates, and help biochemical reaction between the trigger cell, so after the nineties, having turned to the soybean phospholipid is the raw material of preparation liposome.
Cholesterol is a kind of neutral lipid, and content is higher in all kinds of animal cell membranes.It is main in film to play a part to change phospholipid layer character with phospholipids incorporate, and it trends towards weakening being connected between the lipoid and protein in the film, and it plays a part the flowability of adjusting film as " buffer agent ".
Because these two kinds of compositions still do not form the basic substance of liposome bilayer, and itself also has a very important physical function,, unlike assisting (assisting as the miniature glue of nylon), synthetic little glue often in body, is difficult to get rid of easily by the body digest and decompose by their formed " artificial membranes ".
Liposome is as carrier, and its value is to mix various materials, and its mode of mixing is physical property fully, and water miscible material can be encapsulated in the water layer structure of liposome, and fat-soluble material and amphipathic material then are incorporated in the liposome bilayer.Liposome does not have any restriction to the chemical property of these encapsulated materials, therefore has only two class materials can not dope liposome, one: at water and all undissolvable material of organic facies; Its two: dissolubility is all very good in two media, and liposome does not all have barrier action to this material from the inner face to the outside.
The particle diameter of liposome that is used for cosmetics is generally between 100-300nm, by the also short and small particle diameter of its small ratio visible light and with the affinity of Skin Cell, lipoid bimolecular film and cell membrane interaction, bimolecular film and cell membrane fusion, active ingredient is released, absorb, perhaps complete liposome is entered into Cytoplasm then by cytophagy, is absorbed again.Because the phospholipid bimolecular film of liposome has identical basic structure with cell, both have very strong adhesion, make liposome and encapsulation object thereof be easy to enter in the cell simultaneously.Therefore than the operational efficiency height of common permeating method to skin.In addition, liposome can promote the absorption of skin to encapsulating substance.After liposome enters deep skin, what have enters in the cell, what have stops at intercellular substance, because centering on of phospholipid molecule tunic, encapsulation object can only infiltrate by liposome membrane lentamente in the liposome, thereby can slowly discharge the skin activity material of being sealed, the increase active substance is to the action time of skin.Simultaneously because the effect of sealing of liposome, the degraded that can prevent many active substances is with rotten, for example V
E, V
C,, SOD.
Keep the smooth of skin, softness, resilient key component is a water, and what play a crucial role to preserving moisture in the skin is horny layer.Because constituting the main component of liposome bimolecular film is phospholipid, and the special class cellularity of liposome, be it than in the easier deep layer that infiltrates into skin of other materials, and well be distributed in the there, liposome has stronger affinity to the horny layer in skin and the hair simultaneously.Simultaneously liposome not only has moisture-keeping function to skin, can also moisture absorption to keep the moisture of skin.
Fruit acid be a class from Caulis Sacchari sinensis, Fructus Mali pumilae, the 'alpha '-hydroxy acids that extracts in the Fructus Citri Limoniae etc. has hydroxyacetic acid in them, L-lactic acid, tartaric acid, citric acid, in the malic acid etc. tens, wherein common with hydroxyacetic acid and L-lactic acid.Fruit acid is a natural organic acids, and it is simpler to have a molecular structure, and molecular weight is little, fabulous water solublity, and strong permeability can transdermal horny layer and by skin absorbs.Fruit acid is to reduce sticking of corneocyte to the mechanism of action of skin, quickens coming off of cell, promotes the renewal of epidermis cell simultaneously again.The desalination skin splash is opened Peppermint Extract, helps oily skin and acne skin treatments.AHAs can absorb moisture from atmosphere, thereby increases cuticular elasticity, handles dry skin.But the pH value of fruit acid is more little, and acidity is high more, and the skin of human body is had stimulation, influences the safe in utilization of fruit acid.
Summary of the invention
The object of the present invention is to provide a kind of preparation method that is used for the liposome of sealing fruit acid of skin protection, lipidic matrix is dissolved in the ethanol equal solvent, the aqueous solution that adds fruit acid then, fruit acid is encapsulated in the inner water, the fruit acid liposome that obtains both can increase the concentration of fruit acid at epidermis and deep skin, again can the sustained release fruit acid, reduce of the stimulation of high concentration fruit acid to skin.
The present invention also aims to provide the liposome of sealing fruit acid of described method preparation.
The present invention also aims to provide described application of sealing the liposome of fruit acid.
The preparation method that the present invention seals the liposome of fruit acid comprises the steps:
(1) soybean lecithin and cholesterol are dissolved in the solvent, and reduction vaporization is until forming one deck lipid membrane;
(2) add solvent and make the lipid film dissolving, add the phosphate-buffered buffer solution that contains fruit acid, mix homogeneously forms stable single_phase system;
(3) decompression until forming aqueous suspension, separates to such an extent that seal the liposome of fruit acid.
The consumption of described soybean lecithin and cholesterol is 1: the 0-1 mol ratio.
The composition and the percentage by weight thereof of described fruit acid are as follows:
Lactic acid 50-65
Glycolic 20-35
Citric acid 4-10
Malic acid 1-5
Tartaric acid 1-5
The solvent of soybean lecithin and cholesterol can be ethanol, chloroform, dichloromethane, propylene glycol or methanol.
The solvent of lipid film can use ether, diisopropyl ether.
The composition of phosphate buffered solution can be as follows:
Sodium chloride 137mmo/L,
Potassium chloride 12.6mmo/L,
Sodium hydrogen phosphate 6mmo/L,
Potassium dihydrogen phosphate 1.4mmo/L
Preparation liposome 1/10PBS.
The mixing in (2) step can be on the water-bath Ultrasound Instrument ultrasonic concussion 4-7min make to mixture and become stable single_phase system, this system should be placed not phase-splitting more than the 30min.
(1) step can be with mixture reduction vaporization on Rotary Evaporators, and vacuum is 0.005-0.01MPa, to forming gel.
It is to remove non-encapsulated fruit acid that (3) step separated, can be with prepared liposome liquid with the centrifugal 120min-180min of the above speed of 75000r/min, separate and remove the supernatant, lower floor is the fruit acid liposome, also can remove non-encapsulated fruit acid with the method for dialysis.
The quality of the liposome that obtains is composed as follows:
Soybean lecithin: cholesterol=1: 0-1 (mol ratio)
Fruit acid concentration: 5-10 (grams per milliliter)
The present invention is the main component of skin care item with the liposome of sealing fruit acid, accumulate in skin layer after can making the fruit acid transdermal penetration on the one hand, increase fruit acid epidermis and and the concentration of deep skin, utilize the slow-releasing of liposome on the other hand, reduce of the stimulation of the concentration of fruit acid to skin, both made full use of the skin care effect of fruit acid and liposome, avoided the stimulation of fruit acid again skin.
The specific embodiment
Embodiment 1
Get 10 gram lecithin, 1 gram cholesterol is dissolved in the 100mL chloroform, fully makes its dissolving.In 30 ℃ water-bath, in vacuum is under the 0.005Mpa, on Rotary Evaporators, makes it become a skim, adding concentration is the fruit acid phosphate buffered solution of 6g/mL, ultrasonic to mixture formation single_phase system on ultrasonic instrument, continuation reduction vaporization 5min is until forming aqueous suspension liquid, method with dialysis is removed non-encapsulated fruit acid, promptly obtain the fruit acid liposome, be used to prepare fruit acid liposome emollient cream, its percentage by weight prescription is as follows:
Stearic acid 2
Hexadecanol 1.2
Monoglyceride 1.5
PEG-2-hexadecanol ether 0.5
Propylene glycol 6
Isopropyl palmitate 2
Fruit acid liposome 15
BHT 0.05
Water surplus
Result of use: through 30 people in the forearm inboard or wrist 5cm*5cm skin carried out 60 days, the result shows no any stimulation or sensitization, it is moistening that skin keeps, bright in color
Embodiment 2
Get 10 gram lecithin and be dissolved in the 100mL propylene glycol, fully make its dissolving.In vacuum is under the 0.005MPa, on Rotary Evaporators, make it become a skim, adding concentration is 10g/L fruit acid phosphate buffered solution, ultrasonic to mixture formation single_phase system on ultrasonic instrument, continue reduction vaporization 5min, until, make it form aqueous suspension liquid, promptly obtain the fruit acid lipid, be used to prepare fruit acid liposome emollient cream, its percentage by weight prescription is as follows:
Fruit acid liposome 10
Propylene glycol 5
Cetyl Phosphate 0.5
Tocopherol acetate 10
Vitamin A palmitate 5
BHT 0.05
Carbopol?21 3
Water surplus
Result of use: through 30 people in the forearm inboard or wrist 5cm*5cm skin carried out 60 days, the result shows no any stimulation or sensitization, it is moistening that skin keeps, bright in color.
Embodiment 3
Get 20 gram lecithin, 10 gram cholesterol are dissolved in the 200mL methanol, fully make its dissolving.In 30 ℃ water-bath, in vacuum is under the 0.007MPa, on Rotary Evaporators, make it become a skim, adding concentration is 9g/L fruit acid phosphate buffered solution, ultrasonic to mixture formation single_phase system on ultrasonic instrument, continue reduction vaporization 5min, until, make it form aqueous suspension liquid, method with dialysis is removed and is the fruit acid of sealing, and promptly obtains the fruit acid liposome.Successively by the uneven polycarbonate membrane of size, the diameter of liposome is diminished this liposome, particle size distribution is even.Be used to prepare fruit acid liposome sunscreen, its percentage by weight prescription is as follows:
Fruit acid liposome 7
White mineral oil 5
IPP 10
Hexadecanol 0.5
Methyl hydroxybenzoate 0.1
SS 3
567 1.0
Glycerol 2
SSE-20 3.0
Water surplus
Result of use: through 30 people in the forearm inboard or wrist 5cm*5cm skin carry out at 60 days at sunshine, the result shows no any stimulation or sensitization, it is moistening that skin keeps, bright in color, the colour of skin does not have blackening.
Embodiment 4
Get 5 gram lecithin, 1.5 gram cholesterol are dissolved in the 60mL ethanol, fully make its dissolving.In vacuum is under the 0.008MPa, on Rotary Evaporators, makes it become a skim, adding concentration is the fruit acid phosphate buffered solution of 5g/L, ultrasonic to mixture formation single_phase system on ultrasonic instrument, continues reduction vaporization 5min, until, make it form aqueous suspension liquid.Be used to prepare the anti-emulsion of fruit acid liposome skin moistening, its percentage by weight prescription is as follows: lanoline 1.5 white mineral oils 6.0 fruit acid liposomees 4.0 hexadecanol 2.0 kojic acid derivative 0.5 methyl hydroxybenzoate 0.2SP-60 2.0 glycerol 2.0TW-60 2.0VE 0.5 water surplus
Result of use: through 30 people in the forearm inboard or wrist 5cm*5cm skin carry out at 60 days at sunshine, the result shows no any stimulation or sensitization, it is moistening that skin keeps, bright in color.
Claims (9)
1, a kind of preparation method of sealing the liposome of fruit acid is characterized in that comprising the steps:
(1) soybean lecithin and cholesterol are dissolved in the solvent, and reduction vaporization is until forming one deck lipid membrane;
(2) add solvent and make the lipid film dissolving, add the phosphate-buffered buffer solution that contains fruit acid, mix homogeneously forms stable single_phase system;
(3) decompression until forming aqueous suspension, separates to such an extent that seal the liposome of fruit acid; The consumption of described soybean lecithin and cholesterol is 1: the 0-1 mol ratio; The composition and the percentage by weight thereof of described fruit acid are as follows:
Lactic acid 50-65
Glycolic 20-35
Citric acid 4-10
Malic acid 1-5
Tartaric acid 1-5.
2, the preparation method of sealing the liposome of fruit acid according to claim 1, the solvent that it is characterized in that soybean lecithin and cholesterol is ethanol, chloroform, dichloromethane, propylene glycol or methanol.
3, the preparation method of sealing the liposome of fruit acid according to claim 1, the solvent that it is characterized in that lipid film is ether or diisopropyl ether.
4, the preparation method of sealing the liposome of fruit acid according to claim 1 is characterized in that the composed as follows of phosphate buffered solution:
Sodium chloride 137mmo/L,
Potassium chloride 12.6mmo/L,
Sodium hydrogen phosphate 6mmo/L,
Potassium dihydrogen phosphate 1.4mmo/L
Preparation liposome 1/10PBS.
5, the preparation method of sealing the liposome of fruit acid according to claim 1, the mixing that it is characterized in that for (2) step is that ultrasonic concussion 4-7min makes to mixture and becomes stable single_phase system on the water-bath Ultrasound Instrument, and this system should be placed not phase-splitting more than the 30min.
6, the preparation method of sealing the liposome of fruit acid according to claim 1 is characterized in that for (1) step with mixture reduction vaporization on Rotary Evaporators, and vacuum is 0.005-0.01MPa, to forming gel.
7, the preparation method of sealing the liposome of fruit acid according to claim 1, it is characterized in that it is to remove non-encapsulated fruit acid that (3) step separated, with prepared liposome liquid with the centrifugal 120min-180min of the above speed of 75000r/min, separate and remove the supernatant, lower floor is the fruit acid liposome, or removes non-encapsulated fruit acid with the method for dialysis.
8, the liposome of sealing fruit acid for preparing of the described method of claim 1.
9, the described application of liposome in the preparation skin care item of sealing fruit acid of claim 8.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03114221 CN1443529A (en) | 2003-04-15 | 2003-04-15 | Liposome enveloping fruit acid, its preparation method and application |
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| Application Number | Priority Date | Filing Date | Title |
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| CN 03114221 CN1443529A (en) | 2003-04-15 | 2003-04-15 | Liposome enveloping fruit acid, its preparation method and application |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109364011A (en) * | 2018-11-30 | 2019-02-22 | 佛山市奥姿美生物科技有限公司 | It is a kind of to be dissipated and preparation method thereof so that the coated of whitening spot-removing new eight is white |
| CN109691672A (en) * | 2017-10-24 | 2019-04-30 | 国家海洋局第三海洋研究所 | A kind of liposome and preparation method thereof for encapsulating free astaxanthin |
| CN114159332A (en) * | 2021-11-24 | 2022-03-11 | 北京理智之美科技有限公司 | Liposome composition and preparation method thereof |
-
2003
- 2003-04-15 CN CN 03114221 patent/CN1443529A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109691672A (en) * | 2017-10-24 | 2019-04-30 | 国家海洋局第三海洋研究所 | A kind of liposome and preparation method thereof for encapsulating free astaxanthin |
| CN109364011A (en) * | 2018-11-30 | 2019-02-22 | 佛山市奥姿美生物科技有限公司 | It is a kind of to be dissipated and preparation method thereof so that the coated of whitening spot-removing new eight is white |
| CN114159332A (en) * | 2021-11-24 | 2022-03-11 | 北京理智之美科技有限公司 | Liposome composition and preparation method thereof |
| CN114159332B (en) * | 2021-11-24 | 2023-11-10 | 北京理智之美科技有限公司 | Liposome composition and preparation method thereof |
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