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顺铂多囊泡脂质体的制备及顺铂在体外从脂质体中的释放

[Preparation of cisplatin multivesicular liposomes and release of cisplatin from the liposomes in vitro].

作者信息

Xiao Chao-ju, Qi Xian-rong, Aini Waer, Wei Shu-li

机构信息

Department of Pharmaceutics, School of Pharmaceutical Science, Peking University, Beijing 100083, China.

出版信息

Yao Xue Xue Bao. 2003 Feb;38(2):133-7.

PMID:12778750
Abstract

AIM

To prepare cisplatin multivesicular liposomes with high encapsulation efficiency and sustained-release character, and compare the release characteristics with conventional liposomes prepared by reverse-phase evaporation method.

METHODS

Cisplatin multivesicular liposomes were prepared using multiple emulsion method. The concentrations of cisplatin and lipids in the liposomes were measured by flameless atomic absorbance spectroscopy (FAAS) and phosphalipid enzyme reagent method, respectively. The encapsulation efficiency, size and release of the cisplatin from the liposomes were studied in vitro.

RESULTS

The mean diameter of cisplatin multivesicular liposomes was (16.6 +/- 1.0) micron. The encapsulation efficiency of cisplatin was more than 80%. The release profile in vitro fitted with a first-order equation. The releasing t1/2 of cisplatin multivesicular liposomes is 37.7 h, which is 8.4 that of conventional liposomes. Co-membrane stabilizer has remarkable stabilizing effect on the multivesicular liposomal membrane confirmed by differential scattering calorimetry (DSC).

CONCLUSION

The cisplatin multivesicular liposomes showed high encapsulation efficiency and sustained-release character.

摘要

目的

制备具有高包封率和缓释特性的顺铂多囊泡脂质体,并与采用逆相蒸发法制备的常规脂质体的释放特性进行比较。

方法

采用复乳法制备顺铂多囊泡脂质体。分别采用无火焰原子吸收光谱法(FAAS)和磷脂酶试剂法测定脂质体中顺铂和脂质的浓度。体外研究顺铂从脂质体中的包封率、粒径和释放情况。

结果

顺铂多囊泡脂质体的平均直径为(16.6±1.0)微米。顺铂的包封率超过80%。体外释放曲线符合一级方程。顺铂多囊泡脂质体的释放半衰期为37.7小时,是常规脂质体的8.4倍。差示散射量热法(DSC)证实共膜稳定剂对多囊泡脂质体膜具有显著的稳定作用。

结论

顺铂多囊泡脂质体具有高包封率和缓释特性。

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