白头翁皂苷B4长循环脂质体的处方优化与评价  

Formula optimization and evaluation of pulchinenoside B4-loaded long-circulation liposomes

作　　者：刘骏 罗莹 张婧 李翔[2] LIU Jun;LUO Ying;ZHANG Jing;LI Xiang(Jiangxi University of Chinese MedicineKey Laboratory of Modern Preparation of Chinese Medicines,Ministry of Education,Nanchang 330006,China;Jiangxi University of Chinese Medicine National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine,Nanchang 330006,China)

机构地区：[1]江西中医药大学现代中药制剂教育部重点实验室,南昌330006 [2]江西中医药大学中药固体制剂制造技术国家工程研究中心,南昌330006

出　　处：《中国新药杂志》2021年第16期1524-1529,共6页Chinese Journal of New Drugs

基　　金：国家自然科学基金资助项目(81760639,81603054);江西省自然科学基金资助项目(20171BAB215066,20202ACBL216015,20202BABL206157);江西省教育厅科研资助项目(GJJ190666,GJJ190663);江西省青年井冈学者;江西省新世纪百千万人才;江西中医药大学“1050”青年人才

摘　　要：目的:采用星点设计-效应面法优化白头翁皂苷B4长循环脂质体(long-circulation pulchinenoside B4-loaded liposomes, PB4-L)的处方并进行评价。方法:采用乙醇注入法制备脂质体,采用超滤离心法测定制剂包封率。采用4因素3水平星点设计-效应面法优化PB4-L的最佳处方;采用激光粒径仪和透射电镜对制剂的粒径、Zeta电位和形态特征进行表征,并对脂质体的稳定性进行评价。结果:星点设计-效应面法得到PB4-L最优处方如下:磷脂含量为2.4%,磷脂与胆固醇质量比为3∶1,脂药比为2∶1,DSPE-PEG2000含量为2.4%,在最佳制备工艺下,PB4-L的包封率为76.9%,平均粒径为(408.7±1.1) nm,聚合物分散性指数(PDI)为(0.16±0.08),Zeta电位为(-45.2±0.2) mV,透射电镜照片显示脂质体外观圆整,分散性较好;制剂在10%胎牛血清(FBS)培养基中稳定性良好。结论:采用星点设计-效应面法优化的PB4-L制备工艺可行,所得脂质体包封率高、粒径分布均匀,具有良好的体外血清稳定性。Objective:To optimize the formula of long-circulation liposomes loaded with pulchinenoside B4(PB4-L) by central composite design-response surface method and characterize the liposomes. Methods: PB4-L were prepared by ethanol injection and the encapsulation efficiency was determined by ultrafiltration centrifugation. The formula of PB4-L was optimized by the four-factor, three-level central composite design-response surface method. The particle size, zeta potential and morphology of PB4-L were characterized by laser particle zeta-sizer and transmission electron microscope. The stability of the liposomes was evaluated. Results: The optimal formula of PB4-L was as follows: the phospholipid content was 2.4%, the weight ratio of phospholipids to cholesterol was 3∶1, the weight ratio of lipids to drug was 2∶1, and the DSPE-PEG2000 content was 2.4%. The encapsulation efficiency of PB4-L was 76.9%, with a mean particle size of(408.7±1.1) nm, polymer dispersity index(PDI) of 0.16, and zeta potential of(-45.2±0.2) mV. The morphology study of PB4-L showed that the liposomes were round-shaped with good dispersity. PB4-L was stable in 10% FBS-containing medium. Conclusion: The formula of PB4-L was optimized by central composite design-response surface method. The liposomes were characterized by a high encapsulation efficiency, a uniform particle size distribution and a good serum stability in vitro.

关 键 词：脂质体 白头翁皂苷B4 星点设计-效应面法 稳定性 

分 类 号：K943.42[历史地理—人文地理学] R979.1[医药卫生—药品]