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  

Prescription optimization of vinblastine hydrophilic group-modified cationic liposomes by central composite design-response surface method

作　　者：谭静净[1] 程岚[1] 李学涛[1] 

机构地区：[1]辽宁中医药大学药学院,辽宁大连116600

出　　处：《中草药》2012年第9期1742-1745,共4页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(1110172)

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。Objective To optimize the prescription of vinhlastine （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.

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 

分 类 号：R283.6[医药卫生—中药学]