齐多夫定碳酸胆固醇酯脂质体的制备及性质考察
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张玲玲，邓意辉，赵 静，徐 速，吴红兵
(沈阳药科大学 药学院，辽宁 沈阳 110016)
摘 要：目的 用乙醇注入法制备齐多夫定碳酸胆固醇酯脂质体，并考察该脂质体的性质。方法 用不同磷脂和胆固醇半琥珀酸酯制备脂质体，通过正交设计实验得出最佳处方，并对该脂质体的平均粒径、Zeta电位和包封率等性质进行考察。结果 齐多夫定碳酸胆固醇酯脂质体最佳处方中药物-磷脂质量比为1:40、胆固醇半琥珀酸酯-磷脂质量比为1:30、磷脂类型为Epikuron 170。最佳处方的脂质体平均粒径为80.8 nm，Zeta电位为-36.9 mV。用微柱离心法和冷冻超速离心法测得该脂质体的平均包封率分别为94.3%和97.9%。结论 以乙醇注入法制备的齐多夫定碳酸胆固醇酯脂质体粒径较小、包封率高。
关键词：药剂学；脂质体制备；齐多夫定碳酸胆固醇酯；包封率；Zeta电位
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Preparation and characteristics investigation of cholesteryl carbonate zidovudine liposomes
ZHANG Ling-ling, DENG Yi-hui, ZHAO Jing , XU Su, WU Hong-bing
(School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China)
Abstract:Objective To prepare cholesteryl carbonate zidovudine (AZTC) liposomes with ethanol injection method and investigate its characteristics. Method AZTC liposomes were prepared with different phospholipids and cholesteryl succinate. The optimal formulation was obtained based on orthogonal design experiments. The mean diameter, Zeta potential and entrapment efficiency of the optimal preparation were measured. Results The optimal formulation of AZTC liposomes was drug-lipid 1:40, cholesteryl succinate-lipid 1:30, and the best lipid type was Epikuron 170. The mean diameter of the liposomes was 80.8 nm and Zeta potential was –36.9 mV. The mean entrapment efficiencies determined by minicolumn centrifugation method or ultracentrifugation method were 94.3% and 97.9% respectively. Conclusion AZTC liposomes prepared with ethanol injection method exhibite a small diameter with a high entrapment efficiency.
Key words: pharmaceutics; liposomes preparation; cholesteryl carbonate zidovudine; entrapment efficiency; Zeta potential
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