目的 采用叔丁醇-水共溶剂体系冻干法制备多西紫杉醇脂质体。 方法 单因素考察法优化叔丁醇-水共溶剂体系冻干法制备多西紫杉醇脂质体制剂的处方工艺,考察叔丁醇-水比例、糖脂比、药脂比、温度等因素对脂质体包封率和粒径的影响。结果 最佳处方工艺为:叔丁醇-水比50∶50,糖脂比为5∶1,药脂比为1∶10,温度60 ℃,脂质体平均包封率为(88.45±1.63)%,平均粒径263 nm,脂质体体外持续释药48 h。结论 优化的处方工艺可用于多西紫杉醇脂质体的制备。
Abstract
OBJECTIVE To prepare docetaxel liposomes by freeze-drying of tert-butyl alcohol (TBA)/water cosolvent system and evaluate the in vitro and in vivo properties. METHODS The formulation was optimized by single factor screening experiments. The effects of TBA/water ratio, lipid/drug ratio, sucrose/lipid ratio and mixing temperature on encapsulation efficiency were investigated. The in vitro release profiles were also investigated with docetaxel injection(Duopafei) as control. RESULTS The formulated liposomes had a mean size of 263 nm with entrapment efficiency of (88.45±1.63)% at TBA/water ratio 50∶50, lipid/ drug ratio 10∶1, sucrose/lipid ratio 5∶1 and mixing temperature 60 ℃. In vitro drug release from liposomes lasted for 48 h. CONCLUSION Freeze-drying of TBA/water cosolvent system method may be feasible to prepare docetaxel liposomes.
关键词
多西紫杉醇 /
脂质体 /
叔丁醇 /
冷冻干燥
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Key words
docetaxel /
liposome /
tert-butyl alcohol /
freeze-drying
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中图分类号：
R944
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参考文献
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脚注
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基金
山东省高等学校科技计划资助项目(J13LM01)
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