星点设计-效应面法优化隐丹参酮长循环脂质体的制备工艺  

Optimization of Cryptotanshinone Loaded Long-circulation Liposomes Preparation by Central Composite Design-Response Surface Methodology

作　　者：聂小玲 王婴[1] 李明[1] 夏丹敏 冼淑芬 黄斯熙 任笛 王岩[1] NIE Xiaoling;WANG Ying;LI Ming;XIA Danmin;XIAN Shufen;HUANG Sixi;REN Di;WANG Yan(Guangdong Pharmaceutical University,Guangzhou 510006 Guangdong,China)

机构地区：[1]广东药科大学,广东广州510006

出　　处：《中药新药与临床药理》2019年第9期1123-1128,共6页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：国家自然科学基金资助项目（81673608）;广东省科技计划项目（2015A020211034）;广州市科技计划项目（201707010155）

摘　　要：目的以包封率为指标,采用星点设计-效应面法(Central composite design-response surface methodology,CCD-RSM)优化隐丹参酮(CPT)长循环脂质体的制备工艺并进行质量评价。方法采用薄膜分散法制备CPT长循环脂质体,采用高速离心法检测包封率。采用单因素考察和星点设计-效应面法优化CPT长循环脂质体的制备工艺。运用粒径电位分析仪测定脂质体的平均粒径及Zeta电位,透射电镜观察脂质体的形态。结果通过单因素实验,确定膜材比(磷脂∶胆固醇)为2∶1,超声时间为30 min,星点设计-效应面法优化得到的最优处方为:载药温度48℃,水化介质pH值7.4,药脂比1∶17。在最佳制备工艺下,CPT长循环脂质体的包封率为89.16%。该脂质体为粒径均匀,结构完整的球形或类球形粒子,平均粒径和Zeta电位分别为117.8 nm、-47.7mV。结论采用星点设计-效应面法优选的CPT长循环脂质体制备工艺稳定可行,所得脂质体包封率高、粒径小,外观形态好。Objective To optimize the preparation and evaluate the quality of cryptotanshinone loaded longcirculating liposomes by central composite design-response surface methodology(CCD-RSM)using the encapsulation efficiency as the primary indicator.Methods Cryptotanshinone loaded long-circulating liposomes were prepared by film dispersion method.The entrapment efficiency was analyzed by high-speed centrifugation.The preparation process of cryptotanshinone loaded long-circulating liposomes was optimized by single factor experiments and CCDRSM.The particle size and Zeta potential of the liposomes were measured.The morphological examination of liposomes was performed using transmission electron microscopy.Results The best recipe was as follows:the ratio of soybean phospholipids and cholesterol is 2∶1,ultra-sonication time was 30 minutes,the incubation temperature was 48℃,p H value of hydration medium was 7.4,and drug/lipid ratio was 1∶17.With the optimal preparation condition,encapsulation efficiency of CPT long-circulating liposome was 89.16%.The resulting liposomes exhibited a spherical or ellipsoidal shape and were narrow in size distribution.Average particle size of liposomes was 117.8 nm and Zeta potential was-47.7 mV.Conclusion The optimized preparation is stable and feasible.The obtained liposomes have high encapsulation efficiency,small particle size,and good appearance.

关 键 词：隐丹参酮 长循环脂质体 星点设计-效应面法 制备工艺 

分 类 号：R283.6[医药卫生—中药学]