[关键词]
[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。
[Key word]
[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 with good predictability. The prepared VLB hydrophilic group-modified cationic liposomes reach the design requirements.
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[基金项目]
国家自然科学基金资助项目（1110172）
