Preparation method for improving liposome entrapment efficiency

A body encapsulation rate, lipid technology, applied in the field of medicine, can solve the problems of difficult to increase the encapsulation rate of lipid-water insoluble compounds, large toxic and side effects, etc., to improve solubility and bioavailability, eliminate side effects, and improve drug stability sexual effect

Active Publication Date: 2010-11-03
SHENYANG PHARMA UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above improvement scheme still has the problem that it is difficult to improve the encapsulation rate of some lipid-water insoluble compounds, or the addition of surfactants in the prescription has the problem of relatively large toxic and side effects.

Method used

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  • Preparation method for improving liposome entrapment efficiency
  • Preparation method for improving liposome entrapment efficiency
  • Preparation method for improving liposome entrapment efficiency

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0103] 7-Ethyl-10-Hydroxycamptothecin Liposomes

[0104] (1) Dissolve 30 grams of soybean lecithin (injection grade), 5 grams of cholesterol (injection grade), and 2 grams of α-tocopherol in 2000 ml of ethanol (analytical pure), vacuum rotary transfer organic solvent, and place in a vacuum constant temperature drying oven overnight The residual organic solvent was evaporated to prepare dry lipid film, and the above operations were all completed under sterile conditions.

[0105] (2) Dissolve 1.67 grams of 7-ethyl-10-hydroxycamptothecin and 100 grams of sucrose (injection grade) in 1000 ml of sodium carbonate-sodium bicarbonate buffered saline solution (pH=9.9) at a hydration temperature of 45°C Next, use the above-mentioned alkaline buffered saline solution to hydrate the lipid dry film, and after the hydration is complete, use a milk homogenizer to reduce the particle size to 100-200nm to obtain drug-containing liposomes. All the above operations were completed under sterile...

Embodiment 2

[0108] 10-Hydroxycamptothecin liposomes

[0109] (1) Dissolve 40 grams of sphingomyelin (injection grade), 10 grams of cholesterol (injection grade), and 4 grams of α-tocopherol in 6000 ml of ethanol (analytical pure), vacuum rotary transfer organic solvent, and place in a vacuum constant temperature drying oven The residual organic solvent was evaporated overnight to prepare a dry lipid film. The above operations were all completed under sterile conditions.

[0110](2) Dissolve 2 grams of 10-hydroxycamptothecin and 100 grams of trehalose (injection grade) in 3000 ml of potassium dihydrogen phosphate-sodium hydroxide buffer solution (pH=10.0), and use the above-mentioned Alkaline buffered saline solution hydrates the dry lipid film, and after the hydration is complete, use a homogenizer to reduce the particle size to 100-200nm to obtain drug-containing liposomes. All the above operations were completed under sterile conditions.

[0111] (3) Vacuum freeze-drying the drug-cont...

Embodiment 3

[0113] Tegafur Liposome

[0114] (1) Dissolve 50 grams of phosphatidylserine (injection grade), 30 grams of cholesterol (injection grade), and 6 grams of α-tocopherol in 8000 ml of ethanol (analytically pure), vacuum rotary transfer organic solvent, and place in a vacuum constant temperature drying oven The residual organic solvent was evaporated overnight to prepare a dry lipid film. The above operations were all completed under sterile conditions.

[0115] (2) Dissolve 1.67 g of tegafur and 300 g of glycine (injection grade) in 4000 ml of sodium carbonate-sodium bicarbonate buffered saline solution (pH=10.0), and use the above-mentioned alkaline buffered salt at a hydration temperature of 45°C The solution hydrates the lipid dry film, and after the hydration is complete, reduce the particle size to 100-200nm with a homogenizer to obtain the drug-containing liposome. All the above operations were done under sterile conditions.

[0116] (3) Vacuum freeze-drying of the drug-c...

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Abstract

The invention aims to provide a preparation method for improving liposome entrapment efficiency. The preparation method comprises the following steps: dissolving liposoluble components in an organic solvent, and dissolving water-soluble components in alkalescent or acidulous buffer salt; transferring the organic solvent, and adding buffer salt solution for hydration; and after vacuum freeze drying, redissolving the components in the alkalescent or acidulous buffer salt, and incubating to obtain a medicament-containing liposome. Acid compounds are easily dissolved in alkaline solution, and alkaline compounds are easily dissolved in acid solution; and in the method, the liposome is prepared by utilizing the characteristic of solubility change due to the acid-base difference, so that the entrapment efficiency of the compounds in the liposome is improved greatly, and a novel idea for preparing the liposome for indissoluble compounds is provided.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a preparation method for improving liposome encapsulation efficiency. Background technique [0002] The improvement of in vivo bioavailability of poorly soluble compounds has always been a research hotspot in pharmacy. However, many poorly soluble compounds are not only insoluble in water, but also insoluble in physiological tolerance and solvents commonly used in pharmacy, that is, lipid-water insolubility, which hinders the design and application of dosage forms. [0003] When the liposome is delivered to the tumor blood vessels, it can enter the tumor tissue through the capillary epithelial tissue gap, so as to achieve a certain tumor tissue targeting effect. The passive targeting of the liposome drug delivery system, because it changes the distribution of the drug in the body, can improve the curative effect and reduce toxicity at the same time, and it is a good carrier for in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127
Inventor 王淑君叶田田
Owner SHENYANG PHARMA UNIVERSITY
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