八聚精氨酸修饰的载紫杉醇脂质体的制备工艺研究  

Preparation process of R8-modified paclitaxel-loaded liposomes

作　　者：尹愈佳[1] 王小双[2] 唐洁[1] 张莉[1] 谢亮[2] 刘瀚旻[2] 何勤[1] 

机构地区：[1]四川大学靶向药物与释药系统教育部重点实验室,四川成都610041 [2]四川大学华西第二医院妇儿疾病与出生缺陷教育部重点实验室,四川成都610041

出　　处：《华西药学杂志》2012年第6期630-633,共4页West China Journal of Pharmaceutical Sciences

摘　　要：目的研究八聚精氨酸(R8)修饰的载紫杉醇脂质体的制备工艺。方法采用有机相反应法,将R8修饰到脂质体表面,并以薄膜分散-探头超声法制备载紫杉醇脂质体,以细胞摄取、粒径、PDI、包封率为主要指标对磷脂/胆固醇、药脂比、水化液种类、R8密度、DSPE-PEG2000密度进行筛选,进一步优化处方。结果最优处方为磷脂-胆固醇2∶1、药脂比1∶40、水化液为PBS(pH6.5)、R8密度5%、DSPE-PEG2000密度3%,所制脂质体的粒径为156±2 nm,PDI=0.25,包封率为80.87%±8.9%。结论成功制备了八聚精氨酸(R8)修饰的载紫杉醇脂质体。OBJECTIVE To fabricate a novel liposomal formulation of paclitaxel modified with octaarginine（R8）.METHODS R8 was modified onto the surface of liposomes by organic-phase reaction.The liposomes were prepared by thin film-ultrasonic method.The formulation was optimized by means of single-factor experiments with cellular uptake,entrapment efficiency,particle size and PDI as the factors to determine phospholipids-cholesterol,the ratio of drug to lipid,the hydration solution,the density of R8 and the density of DSPE-PEG2000.RESULTS The optimal formulation was that phospholipids-cholesterol（2：1）,the ratio of drug to lipid was 1：40,the hydration solution was PBS（pH6.5）,the density of R8 was 5%,and the density of DSPE-PEG2000 was 3%.The particle diameter of liposomes was 156±2 nm,PDI was 0.25,and the entrapment efficiency was 80.87%±8.9%.CONCLUSION The R8-modified paclitaxel-loaded liposomes were successfully prepared.

关 键 词：八聚精氨酸 紫杉醇 血管平滑肌细胞 细胞摄取 

分 类 号：R94[医药卫生—药剂学]