功能性支链的合成及靶向性CPPs修饰纳米脂质体的初步理化性质评价  

The study on synthesis process of functional branch and the preliminary evaluation on physicochemical properties of targeting CPPs-modified nanoliposomes

作　　者：时念秋[1,2] 郝乘仪[1] 冯波[1] 张秀荣[1] 李正强[2] 齐宪荣[3] 

机构地区：[1]吉林医药学院,吉林吉林132013 [2]吉林大学生命科学学院,吉林长春130012 [3]北京大学药学院,北京100191

出　　处：《吉林医药学院学报》2016年第3期161-166,共6页Journal of Jilin Medical University

基　　金：吉林市科技发展计划资助项目(201464053);中国博士后科学基金面上项目(2015M571374);吉林省科技发展计划项目(20140311110YY);吉林省教育厅资助项目(2015401)

摘　　要：目的旨在合成功能性支链,并制备靶向细胞穿透肽(CPPs)修饰脂质体及对其体外理化性质进行初步表征。方法主要通过马来酰基团与巯基的特异反应合成多肽修饰的PEG-DSPE功能性支链,再通过薄膜分散法制备了靶向性CPPs修饰的载阿霉素多功能纳米脂质体,并利用激光粒度仪及荧光分光光度法对功能性脂质体的平均粒径、表面电位、包封率、多分散系数及体外释药等理化性质进行研究。结果在脱氧充氮的条件下,利用Michael加成反应可以成功地合成功能性支链,并通过硫酸铵梯度法顺利地构建了靶向CPPs修饰的纳米脂质体,及初步考察出其体外纳米载体理化性质。结论本研究为脂质体构建所需功能性支链的合成工艺参数提供有价值的参考,为下一步系统研究其生物学性质提供前期基础。Objective To synthesize the functional branch and prepare the targeting CPPs-modified liposomes which physicochemical properties are also characterized preliminary in vitro.Methods Polypeptides-modified PEG-DSPE functional branch was synthesized by specific reaction between maleimide and thiol group.Thin-membrane dispersed method was applied to construct targeting CPPs-modified nanoliposomes.In vitro physicochemical properties including mean particles size,surface potential,encapsulation efficiency,polydispersity indexs and in vitro release were studied by laser particle size analyzer and ultraviolet fluorescence spectrophotometry.Results Under the condition of deaer-ation by nitrogen stripping,functional branch could be successful synthesized through Michael addition reaction.Targe-ting CPPs-modified nanoliposomes may be prepared favorably by ammonium sulfate gradient strategy and their physico-chemical properties in vitro were studied.Conclusion This research provide valuable reference for the synthesis strategy applied in functional branch of liposomes and give an early foundation for next biological properties research.

关 键 词：功能性支链 合成 MICHAEL加成反应 纳米脂质体 

分 类 号：R943[医药卫生—药剂学]