中心组合设计-效应面法优化长春碱亲水基修饰阳离子脂质体的处方.pdf

·1742 · 中草药 Chinese Traditional and Herbal Drugs 第 43 卷 第 9 期 2012 年 9 月 中心组合设计-效应面法优化长春碱亲水基修饰阳离子脂质体的处方 谭静净，程 岚，李学涛* 辽宁中医药大学药学院，辽宁 大连 116600 摘 要：目的 采用中心组合设计-效应面法优化长春碱亲水基修饰阳离子脂质体的最佳处方。方法 以主动载药-pH 梯度 法制备亲水基修饰阳离子脂质体，以包封率、Zeta 电位为指标，考察长春碱与二棕榈酰磷脂酰胆碱（DPPC ）质量比、DPPC 与 3β-[N-(N ′, N ′-二甲基胺乙基)胺基甲酰胺基] 胆固醇（DC-Chol ）物质的量之比、二硬脂酰磷脂酰乙醇胺-聚乙二醇 （DSPE-PEG 2000 ）的质量分数3 个因素对考察指标的影响，并对各个因素进行二项式拟合，通过响应面分析选取最佳处方。 结果 优化出的长春碱亲水基修饰阳离子脂质体的处方为长春碱与 DPPC 质量比为 0.06、DPPC 与 DC-Chol 物质的量之比为 1.00、DSPE-PEG 2000 的质量分数为7% 。结论 中心组合设计-效应面法应用简便、预测性好，制备的长春碱亲水基修饰阳 离子脂质体符合设计要求。 关键词：中心组合设计；效应面法；长春碱；阳离子脂质体；主动载药-pH 梯度法 中图分类号：R283.6 文献标志码：A 文章编号：0253 - 2670(2012)09 - 1742 - 04 Prescription optimization of vinblastine hydrophilic group-modified cationic liposomes by central composite design-response surface method TAN Jing-jing, CHENG Lan, LI Xue-tao School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian 116600, China Abstract: Objective To optimize the prescription of vinblastine (VLB) hydrophilic group-modified cationic liposomes by using central composite design-response surface method. Methods The hydrophilic group-modified cationic liposomes were prepared by active loading-pH gradient method. Taking encapsulation efficiency (EE) and Zeta potential as indexes, the effects of weight ratio of VLB/DPPC, the mole ratio of DPPC/DC-Chol, and the concentration of DSPE-PEG 2000 on them were investigated. Binomial fitting of each factor was observed and response surface analysis was used to select the optimal prescription. Results The weight ratio of VLB/DPPC in optimized prescription of VLB hydrophilic group-modified cationic liposomes was 0.06, the mole ratio of DPPC/DC-Chol was 1.00, and the concentration of DSPE-PEG 2000 was 7%. Conclusion Central composite design-response surface method is convenient to use wit