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pH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-polyglutamic acid ( DOX/NPs ) and studied the properties of DOX/NPs, including drug loading, drug entrapment efficiency,drug release in vitro and in vivo.The optimum loading was 22. 4% and entrapment efficiency was 90. 2%.The mean size of DOX/NPs was (312. 3±7. 2) nm with narrow distribution,and a typical core-shell structure was observed via transmission electron microscope. A pH-sensitive sustainable drug-release was detected 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.
展开▼
