胆甾醇基γ-聚谷氨酸负载阿霉素纳米胶束的制备与体内外释药性能评价  

Preparation of doxorubicin-loaded nanoparticles of cholesterol-bearingγ-polyglutamic acid and its drug-release in vivo and in vitro

作　　者：姚俊[1] 肖港 徐宁 曹新[1] 徐虹[2] 

机构地区：[1]南京医科大学基础医学院生物技术系,江苏南京211166 [2]南京工业大学食品与轻工学院材料化学工程国家重点实验室,江苏南京211800

出　　处：《生物加工过程》2017年第6期64-67,共4页Chinese Journal of Bioprocess Engineering

基　　金：国家自然科学基金青年基金(51403103);江苏省高等学校大学生实践创新训练计划(201710312065X)

摘　　要：笔者制备了胆甾醇基γ-聚谷氨酸负载阿霉素纳米胶束(DOX/NPs),并考察了该载药纳米胶束体系的形态与粒径、载药量、包封率以及体内外释药的特性。结果表明:DOX/NPs的最佳载药量为22.4%,包封率为90.2%,平均粒径为(312.3±7.2)nm,电镜下观察呈现明显的核壳结构。体外释药结果显示,DOX/NPs能延缓阿霉素的释放,并具有p H敏感的释药特性。小鼠体内释药结果表明:阿霉素经包埋后其消除半衰期(t1/2)、药时曲线下面积(AUC)、平均滞留时间(MRT)均明显大于游离阿霉素,达到了药物缓释的目的。We prepared adoxorubicin （DOX） loaded nanoparticles of cholesterol？bearing γ-polyglutamicacid （ DOX/ NPs） and studied the properties of DOX/ NPs, including drug loading, drug entrapmentefficiency,drug release in vitro and in vivo.The optimum loading was 22. 4% and entrapment efficiency was90. 2%.The mean size of DOX/ NPs was （312. 3±7. 2） nm with narrow distribution,and a typical core-shellstructure was observed via transmission electron microscope.A pH-sensitive sustainable drug-release wasdetected in vitro, and in vitro experiments confirmed the slow-releasing characteristic of DOX/ NPs.Compared with DOX · HCl injections,DOX/ NPs could significantly enhance the elimination half-life（t1/ 2）,area under concentration-time curveand mean residence time to achieve the slow-release of loaded DOX.

关 键 词：纳米胶束 Γ-聚谷氨酸 阿霉素 释药 药代动力学 

分 类 号：O636.9[理学—高分子化学] R944.15[理学—化学]