Preparation method of liposome medicine with outer layer modified by hydrophilic polymer

A technology of hydrophilic polymers and hydrophilic polymers, applied in the field of preparation of drugs for the treatment of tumor diseases, can solve problems such as difficult control of yield, difficulty in industrialization, phospholipid hydrolysis, etc., to achieve sustained release and targeting, The effect of improving economic benefits and high encapsulation efficiency

Active Publication Date: 2011-05-04
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, we found in the process of preparing vinorelbine long-circulating liposomes that the addition of mPEG-DSPE will hinder the loading of vinorelbine. When the drug lipid ratio is high, mPEG-DSPE has a greater impact on vinorelbine Significantly, the encapsulation efficiency is less than 10%
The final product obtained by the above method is the ideal liposome model suitable for vinorelbine that we constructed before, but this method introduces chemical reactions in the preparation process of liposomes, which easily causes the hydrolysis of phospholipids and affects the liposomes. The stability of the body, and the yield is not easy to control, but also requires multi-step removal of impurities, it is difficult to achieve industrialization

Method used

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  • Preparation method of liposome medicine with outer layer modified by hydrophilic polymer
  • Preparation method of liposome medicine with outer layer modified by hydrophilic polymer
  • Preparation method of liposome medicine with outer layer modified by hydrophilic polymer

Examples

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Effect test

Embodiment 1

[0015] Embodiment 1 does not contain the preparation of the liposome of hydrophilic polymer

[0016] Mix phospholipids, such as hydrogenated soybean lecithin (or bispalmitate lecithin or bis myristate lecithin), with cholesterol at a weight ratio of 3:1, dissolve in 95% tert-butanol, and freeze-dry in a lyophilizer The organic solvent is removed to form a loose lipid phase mixture lyophilized powder, and the lyophilized powder is hydrated with a solution containing counter ions to form blank liposomes. The blank liposomes use high-pressure extrusion equipment or micro-fluidic equipment to reduce the particle size of liposomes, and then use column chromatography or dialysis means to remove counterions outside the liposomes with sucrose-histidine solution as the external phase. This creates an ion gradient inside and outside the lipid membrane. The aqueous drug solution is mixed with the liposome suspension, and incubated at 50-60° C. to obtain liposomes without hydrophilic pol...

Embodiment 2

[0017] The preparation of the liposome modified by embodiment 2 bilayer hydrophilic polymer

[0018] Mix phospholipids, such as hydrogenated soybean lecithin (or bispalmitate lecithin or bis myristate lecithin), cholesterol with a weight ratio of 3:1, and an appropriate amount of lipids derived from hydrophilic polymers, and dissolve them in In 95% tert-butanol, lyophilize in a lyophilizer to remove the organic solvent to form a loose lipid phase mixture lyophilized powder, and hydrate the lyophilized powder with a solution containing counter ions to form blank liposomes. The blank liposomes use high-pressure extrusion equipment or micro-fluidic equipment to reduce the particle size of liposomes, and then use column chromatography or dialysis means to remove counterions outside the liposomes with sucrose-histidine solution as the external phase. This creates an ion gradient inside and outside the lipid membrane. The drug aqueous solution is mixed with the liposome suspension,...

Embodiment 3

[0019] The preparation of the liposome modified by embodiment 3 outer layer hydrophilic polymer

[0020]Mix phospholipids, such as hydrogenated soybean lecithin (or bispalmitate lecithin or bis myristate lecithin), with cholesterol at a weight ratio of 3:1, dissolve in 95% tert-butanol, and freeze-dry in a lyophilizer The organic solvent is removed to form a loose lipid phase mixture lyophilized powder, and the lyophilized powder is hydrated with a solution containing counter ions to form blank liposomes. Blank liposomes use high-pressure extrusion equipment or micro-fluidic equipment to reduce the particle size of liposomes, and then use column chromatography or dialysis means to use sucrose histidine solution as the external phase to remove counterions outside the liposome, so that the liposomes An ion gradient is formed inside and outside the membrane. Mix the drug aqueous solution with the liposome suspension, and incubate at 50-60°C to obtain drug-containing liposomes, t...

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Abstract

The invention discloses a preparation method of a liposome medicine with the outer layer modified by a hydrophilic polymer. The method comprises the following steps of: preparing a liposome, and then inserting a lipid substance modified by a hydrophilic polymer outside two layers of the phospholipid. The method not only can achieve high encapsulation rate, but also can realize the slow release and target action of a long circulating liposome.

Description

technical field [0001] The invention relates to a preparation method of a liposome, in particular to a preparation method of a liposome whose outer layer is modified by a hydrophilic polymer, and an application thereof in preparing medicine for treating tumor diseases. Background technique [0002] Liposomes can be used as carriers for many drugs. As a carrier of antineoplastic drugs (especially chemotherapy drugs), it can reduce the distribution of drugs in normal tissues and increase the accumulation of drugs in tumor tissues, thereby improving the therapeutic index of drugs. [0003] Traditional liposomes are easily recognized and phagocytosed by the immune system in the body, so liposomes may have been cleared by the body before they reach the target area and cannot play their targeting role. Long-circulating liposomes, also known as stealth liposomes, can prevent the recognition and uptake of liposomes by macrophages, thereby prolonging the circulation time of liposome...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/28A61K47/34A61K47/32A61K45/00A61K31/475A61P35/00
Inventor 李春雷张莉王彩霞张兰王世霞李彦辉魏娜修宪梁敏李永丰
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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