Box-Behnken效应面法优化青藤碱肝靶向脂质体的制备工艺  

Optimization of Sinomenine Hepatic Targeted Liposomes Preparation by Box-Behnken Design-Response Surface Methodology

作　　者：周围 陈意苹 何永鹏 王淑香 黄文翔 李卓杰 孙雪芬 Zhou Wei;Chen Yiping;He Yonpeng;Wang Shuxiang;Huang Wenxiang;Li Zhuojie;Sun Xuefen(Institute of Chemical Engineering,Guangdong Academy of Sciences,Guangzhou 510630;Supervision Department of Drug Safety,Station for Supervision and Inspection of Drug and Instrument,Joint Logistics Support Center of Guilin,Guangzhou 510500;School of Traditional Chinese Medicine,Guangdong Pharmaceutical University,Guangzhou 510006,China)

机构地区：[1]广东省科学院化工研究所,广东广州510630 [2]桂林联勤保障中心药品仪器监督检验站药品安全监督科,广东广州510500 [3]广东药科大学中药学院,广东广州510006

出　　处：《广东化工》2020年第19期1-5,共5页Guangdong Chemical Industry

摘　　要：目的:以包封率为指标,采用Box-Behnken效应面法优化青藤碱肝靶向脂质体(GC-SIN-LP)的制备工艺并进行质量评价。方法:采用薄膜分散法制备(GC-SIN-LP),采用葡聚糖凝胶法测包封率。根据单因素考察结果,采用Box-Behnken效应面法优化(GC-SIN-LP)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:确定(GC-SIN-LP)的最优制备工艺参数:磷脂与胆固醇质量比为3.86∶1,温度为30.84℃,磷脂浓度为8.26 mg·mL-1;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204.6 nm、-0.926 mV。结论:该法具有工艺稳定、制法简便、重复性好等特点,适于(GC-SIN-LP)的制备。Objective:To optimize prescription and evaluate the quality of sinomenine hepatic targeted liposomes(GC-SIN-LP)by Box-Behnken design-response surface methodology(BBD-RSM),therefore to use the encapsulation efficiency as the primary indicator.Methods:GC-SIN-LP were prepared by film dispersion method.The entrapment efficiency was analyzed by sephadex column chromatography.The preparation process of GC-SIN-LP was optimized by BBD-RSM bacic on single factor experiments.The particle size and Zeta potential of the liposomes were measured.The morphological examination of liposomes was performed using transmission electron microscopy.Results:The optimum preparation process of GC-SIN-LP was determined as follows:the ratio of lipid to cholesterol was 3.86∶1,the temperature was 30.84℃,the concentrations of phospholipids was 8.26 mg·mL-1;The resulting liposomes exhibited a spherical or ellipsoidal shape and was narrow in size distribution.Average particle size of liposomes was 204.6 nm and Zeta potential was-0.926 mV.Conclusion:The method has the advantages of stable technology,simple preparation method and good repeatability,so it is suitable for the preparation of GC-SIN-LP.

关 键 词：青藤碱 靶向脂质体 薄膜分散法 BOX-BEHNKEN效应面法 制备工艺 

分 类 号：TQ[化学工程]