Method for preparing alpha-lipoic acid liposome

A technology of lipoic acid and lipoic acid, which is applied in the directions of liposome delivery, food preparation, preparations for skin care, etc., can solve the problems of easy degradation, discounted effect, inability to play a normal physiological role, etc., and achieves uniform liposome, Reduced irritation, ease of hydration process

Inactive Publication Date: 2010-06-09
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current use of α-lipoic acid is not stable enough, it is easy to degrade in the human body, and cannot exert normal physiological functions. Therefore, the effect as a cosmetic or food is greatly reduced. If uniform and stable α-lipoic acid can be obtained, its market prospect very optimistic

Method used

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  • Method for preparing alpha-lipoic acid liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Take 5ml of α-lipoic acid dehydrated ethanol solution with a concentration of 1.6mg / mL, 0.15g of cholesterol, 0.5g of soybean lecithin and 5mL of chloroform as solvents, dissolve them in a rotary evaporator at an evaporation temperature of 35°C under vacuum Rotary evaporation at a temperature of 0.09MPa, the speed is 10 rpm, after the solvent evaporates completely to form a uniform film, add the auxiliary agent diethyl ether to dissolve, and then use 40mL of phosphate buffer solution with pH=7.4 to make it hydrated at 35°C. Then it was ultrasonically broken for 20 minutes, the power was 250w, the temperature of the water bath was 30°C, and then the product was obtained by rotary steaming for 5 minutes. After characterization by a laser particle size analyzer, the obtained product is uniformly dispersed, with an average particle size of about 120nm, an encapsulation rate of 59%, and no delamination after 20 days of constant temperature storage.

Embodiment 2

[0024] Weigh 0.5g of soybean lecithin, 0.15g of cholesterol and dissolve completely with 5mL of chloroform as solvent, then slowly pour 5mL of 1.6mg / mL α-lipoic acid absolute ethanol solution, stir well, place in a rotary evaporator to evaporate Rotary evaporation at a temperature of 40°C and a vacuum of 0.08Mpa at a speed of 10 revolutions / min. After the solvent evaporates completely to form a uniform film, add diethyl ether as an auxiliary agent to dissolve it, and then use 30mL of phosphate buffer solution with pH=7.4 in water at 40°C. Melt for 20min. Then it was ultrasonically crushed for 20 minutes, the power was 250w, and the temperature of the water bath was 30°C. Finally, vacuum rotary evaporation is carried out to obtain the product. After characterization by a laser particle size analyzer, the obtained product is uniformly dispersed, with an average particle size of about 110nm, an encapsulation rate of 51%, and no delamination after 20 days of constant temperature ...

Embodiment 3

[0026] Weigh 0.5g of soybean lecithin, 0.15g of cholesterol and dissolve completely with 5mL of chloroform as solvent, then slowly pour 5mL of 1.6mg / mL α-lipoic acid absolute ethanol solution, stir well, place in a rotary evaporator to evaporate Rotary evaporation at a temperature of 45°C and a vacuum of 0.07Mpa at a speed of 15 revolutions / min. After the solvent evaporates completely to form a uniform film, add diethyl ether as an auxiliary agent to dissolve it, and then use 30ml of phosphate buffer solution with pH=7.4 in water at 45°C. Ultrasonic crushing for 20 minutes after melting for 20 minutes, the power is 400w, and the temperature of the water bath is 30°C. Then carry out vacuum rotary evaporation to obtain the product. After characterization by a laser particle size analyzer, the obtained product is uniformly dispersed, with an average particle size of about 100nm, an encapsulation rate of 61%, and no delamination after 20 days of constant temperature storage.

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Abstract

The invention discloses a method for preparing an alpha-lipoic acid liposome, which comprises: dissolving soyabean lecithin and cholesterol in an organic solvent and adding the solution into solution of alpha-lipoic acid to form liposome solution, wherein the mass ratio of the soyabean lecithin to the cholesterol to the alpha-lipoic acid is 3.1-3.5:1:0.03-0.06; forming a thin film by water bath treatment, pressure reduction and distillation; and adding an ethylether assistant and forming the homogeneous liposome by hydration and crushing. The alpha-lipoic acid liposome preparation by the method is homogeneous, stable and high in entrapment rate and is favorable for industrial production.

Description

technical field [0001] The invention relates to the field of preparation of α-lipoic acid, in particular to a preparation method of α-lipoic acid liposome. Background technique [0002] Since liposomes were discovered by A.D.Bangham in 1965, liposomes have developed rapidly in the fields of biophysics, colloid science, chemistry, and cells. In particular, drug-loaded liposomes have attracted more and more attention because of their good cell affinity, targeting, sustained release and reduced drug toxicity. At present, there are many methods for preparing liposomes, commonly used are thin film method, reverse phase evaporation method, solvent injection method and double emulsion method, etc. These methods are generally called passive drug loading method; pH gradient method, ammonium sulfate gradient method, etc. Generally known as the active drug loading method. However, in the preparation process of some drug-loaded liposomes, problems such as the morphology and particle s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/385A61K8/49A61P1/16A61P3/04A61P39/06A61Q19/00A23L1/29A23L33/00
Inventor 何秋星王学文
Owner GUANGDONG PHARMA UNIV
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