Box-Behnken响应面法优化哈西奈德脂质体的制备工艺  

Optimization of the preparation process of Hasinide liposomes by the Box-Behnken response surface methodology

作　　者：林肖霞[1] 蔡延渠[2] 高建滨[1] 蔡艳桃 苏少琴 LIN Xiaoxia;CAI Yanqu;GAO Jianbin;CAI Yantao;SU Shaoqin(Foshan Nanhai District Maternal and Child Health Hospital,Foshan 528200,China;The Center for Drug Research and Development,Guangdong Pharmaceutical University,Guangzhou 510006,China)

机构地区：[1]佛山市南海区妇幼保健院,广东佛山528200 [2]广东药科大学新药研发中心,广东广州510006

出　　处：《广东药科大学学报》2019年第2期169-173,185,共6页Journal of Guangdong Pharmaceutical University

摘　　要：目的采用Box-Behnken响应面法优化哈西奈德脂质体制备工艺。方法考察哈西奈德∶磷脂(质量比)、胆固醇∶磷脂(质量比)、VE∶磷脂(质量比)、乙醇用量等因素对哈西奈德脂质体包封率的影响;采用Box-Behnken响应面法优化哈西奈德脂质体制备工艺;并对脂质体的形态、粒径及透皮性能进行评价。结果哈西奈德脂质体优化工艺为:哈西奈德∶磷脂(质量比)为2.1∶10;胆固醇∶磷脂(质量比)为1.9∶10;VE∶磷脂(质量比)为0.4∶10;乙醇用量为4.66 mL,预测包封率达81.95%,实际包封率为79.25%,偏差较小,预测性良好。在最优化制备工艺条件下,哈西奈德脂质体的粒径为(148.2±10.3)nm、Zeta电位为41.67 mV,2、4、6、8、10、12 h的累积透过量和累积渗透率均显著高于哈西奈德溶液组(P<0.01)。结论 Box-Behnken响应面法可以准确快速地优化哈西奈德脂质体的制备工艺,哈西奈德脂质体具有良好的透皮性能。Objective To optimize the preparation process of the Hasinide liposomes by the Box-Behnken response surface methodology.Methods The effects of Hassinide ∶ phospholipid ratio,cholesterol ∶ phospholipid ratio,VE ∶ phospholipid ratio,ethanol dosage on encapsulation efficiency of Hassinide liposomes were investigated. Box-Behnken response surface methodology was used to optimize the preparation of Hassinide liposomes.The morphology,particle size and transdermal properties of liposomes were evaluated.Results The optimum technology of Hassinide liposomes was as follows:Hassinide ∶phospholipid ratio was 2.1∶10;cholesterol∶ phospholipid ratio was 1.9∶10;VE∶phospholipid ratio was 0.4∶ 10;ethanol dosage was 4.66 mL,the predicted encapsulation rate was 81.95%,the actual encapsu-lation rate was 79.25%,the deviation was small,and the predictability was good.Under the optimum preparation conditions,the particle size of Hassinide liposomes was (148.2+10.3) nm and Zeta potential was 41.67 mV.The cumulative transdermal amounts at 2,4,6,8,10 and 12 h and cumulative permeability of Hassinide liposomes were significantly higher than those of Hassinide solution group ( P <0.01).Conclusions Box-Behnken response surface methodology can accurately and rapidly optimize the preparation process of Hassinide liposomes.The Hasinide liposomes have good transdermal properties.

关 键 词：哈西奈德 脂质体 经皮吸收 响应面法 

分 类 号：R946.1[医药卫生—药剂学]