蟾酥提取物长循环脂质体的制备及质量评价

目的研究蟾酥提取物长循环脂质体(chan su long-c ircu lation liposom e,CSLLP)的制备方法,并对其质量进行评价。方法考察不同方法制备CSLLP的包封率,最终确定选用乙醇注入法制备CSLLP,正交设计优化处方,用两亲性聚乙二醇2000-二硬脂酰磷脂乙醇胺(mPEG2000-DSPE)修饰脂质体膜,透射电镜观察形态,激光散射法测定粒径大小及分布,采用葡聚糖凝胶柱层析法和HPLC法测定CSLLP的包封率和渗漏率。结果乙醇注入法制备的CSLLP包封率最高,所得脂质体外观圆整而均匀,渗漏率小,稳定性好,平均粒径为69.8 nm,药物平均包封率为95.54%。结论用乙醇注入法可制备包封率高、稳定性好的CSLLP。

Preparation and evaluation of long-circulating liposomes of Venenum Bufonis extractive

Objective To prepare and characterize the long-circulating liposomes of extractive of Venenum Bufonis. Methods Compare the entrapment efficiency of each method including thin-film dispersion method , diethyl ether injection method and ethanol injection method ,the long-circulating liposomes were prepared by ethanol injection method at last. Amphipathic Polyethylene Glycol Distearoyl phosphatidylethanolamine (mPEG2000-DSPE) was added to modify the membrane of the liposomes.The entrapment efficiency and percolation rate were determined by Sephadex G-50 column chromatographic analysis antigenic and HPLC method. Results The average diameter of the Venenum Bufonis liposomes was 69.8 nm and the entrapment efficiency of the liposomes was 95.54% . Conclusions The preparation of Venenum Bufonis liposomes was easy and practicable,and pharmaceutical characterization showed that the Venenum Bufonis liposomes were stable.