Box-Behnken效应面法优化多西他赛长循环脂质体处方  

Formula optimization of Docetaxel long-circulation liposomes by Box-Behnken design and response surface method

作　　者：程怡[1] 吴琼[1] 余秋强[1] 赵菊香[1] 

机构地区：[1]广州中医药大学中药学院,广东广州510006

出　　处：《中草药》2012年第10期1946-1950,共5页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(30772790)

摘　　要：目的优化多西他赛长循环脂质体(DLCL)处方。方法采用薄膜蒸发法制备DLCL,分别以卵磷脂(PC)与多西他赛(DOC)质量比(X1)、PC与胆固醇(Chol)质量比(X2)、DSPE-PEG 2000与PC物质的量之比(X3)为考察对象,包封率(Y1)、载药量(Y2)、综合指标OD值为评价指标,采用Box-Behnken效应面法筛选DLCL的最佳处方。结果最优处方为X1=0.616 2,X2=1.0,X3=1.0;DLCL的包封率为(94.71±1.75)%,载药量为(5.37±0.43)%,标准偏差均小于10%;平均粒径139.6 nm,分布均匀,体外释放试验结果表明其具有明显的缓释效果。结论采用Box-Behnken效应面法优化DLCL处方是有效、可行的。Objective To optimize the formula of Docetaxel（DOC） long-circulation liposomes（DLCL）.Methods DLCL was prepared by the membrane-hydration method.The effects of phosphatidylcholine（PC）-DOC（X1）,PC-cholesterol（Chol）（X2）,and the amount of DSPE-PEG 2000（X3） were observed.The encapsulation efficiency（Y1）,drug loading amount（Y2）,and the general requirements（Y3） were evaluated and the formula was optimized by Box-Behnken design and response surface method.Results The optimal formula was as following： X1=0.616 2,X2=1.0,and X3= 1.0;The encapsulation efficiency was（94.71 ± 1.75）%,drug loading amount was（5.37 ± 0.43）%.The standard deviations were all below 10%.The average particle size was 139.6 nm.Moreover,in vitro release tests showed that the prepared DLCL had obvious sustained-release effects.Conclusion Using Box-Behnken design and response surface method to prepare DLCL is effective and feasible.

关 键 词：多西他赛 长循环脂质体 Box-Behnken 效应面法 体外释放 

分 类 号：R283.6[医药卫生—中药学]