[关键词]
[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=0.6162,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。
[Key word]
[Abstract]
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.
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[基金项目]
国家自然科学基金资助项目(30772790)