盐酸托泊替康脂质体包封率影响因素的考查  

Investigation on the Factors Affecting Entrapment Efficiency of Topotecan Hydrochloride Liposomes

作　　者：郭田田 解晓冬 张潞艳 石亮 张辉 GUO Tian-tian;XIE Xiao-dong;ZHANG Lu-yan;SHI Liang;ZHANG Hui(Shanxi Zhendong Pharmaceutical Co.Ltd.,Changzhi 047100,China)

机构地区：[1]山西振东制药股份有限公司,山西长治047100

出　　处：《安徽化工》2023年第3期101-104,共4页Anhui Chemical Industry

摘　　要：利用脂质体为药物载体,制备抗癌药盐酸托泊替康脂质体,并进一步探究影响盐酸托泊替康脂质体包封率的因素,筛选得到较优的制备工艺。以HSPC、DSPE-MPEG和Chol为包封材料,采用主动载药法—硫酸铵梯度法进行脂质体的制备,研究空白脂质体的pH、硫酸铵浓度、药磷比和孵育时间对盐酸托泊替康脂质体包封率的影响。空白脂质体的pH和孵育时间对包封率无显著影响,硫酸铵浓度为0.35 mol·L^(-1),API/P=3.5,空白脂质体pH=5.0,包封率>95%。硫酸铵浓度和药磷比为影响盐酸托泊替康脂质体包封率的最主要因素,两者可进一步提高盐酸托泊替康脂质体的包封率。To further explore the factors that affect the encapsulation efficiency of liposomal TPT hydrochloride,and to screen for a satisfactory results.By the method of ammonium sulfate gradient,HSPC,DSPE-MPEG and Chol were used as encapsulation materials.In order to investigate the effects of pH,ammonium sulfate concentration,drug-to-phosphorus ratio and incubation time of blank liposomes on the encapsulation efficiency of the product.The results showed that the pH of the blank liposome and incubation time had no significant effect on the encapsulation efficiency.The ammonium sulfate concentration was 0.35 mol·L^(-1),API/P=3.5,the blank liposome pH=5.0,the encapsulation efficiency was over 95%.The concentration of ammonium sulfate and the ratio of drug to phosphorus are the most important factors affecting the encapsulation efficiency and they have a significant effect on the encapsulation efficiency of TPT hydrochloride liposomes.

关 键 词：盐酸托泊替康 脂质体 硫酸铵梯度法 包封率 

分 类 号：R943[医药卫生—药剂学]