目的 制备羧基化多壁碳纳米管-紫杉醇复合物(PTX-MWCNTs-COOH),并考察其体外释药性能。方法 以紫杉醇(PTX)为药物,磷脂为表面活性剂,溶剂共混法制备PTX-MWCNTs-COOH,用激光粒径仪、透射电镜(TEM)、差示扫描量热仪(DSC)等对其进行表征,滤膜法-HPLC测定其载药量,微柱分离-HPLC测定其包封率,反向透析法研究PTX-MWCNTs-COOH在pH 7.4的PBS缓冲溶液(含1%聚山梨酯80)的体外释药行为。结果 药物成功加载到多壁碳纳米管上形成PTX-MWCNTs-COOH,其Zeta 电位为(-24.5±1.01) mV,载药量为(50.09±0.02)%,包封率为(76.80±0.02)%,在体外的释放效果良好。结论 制备的PTX-MWCNTs-COOH具有良好的理化性质,载药量与包封率较高,反向透析法能较好地用于研究PTX-MWCNTs-COOH的体外释药行为。
Abstract
OBJECTIVE To prepare and characterize PTX-MWCNTs-COOH complex and study its in vitro release properties. METHODS The PTX-MWCNTs-COOH complex was prepared by solvent blending method with paclitaxel as drug,phospholipid as surfactant. It was characterized by laser particle size analyzer,transmission electron microscope (TEM) and DSC analysis. The drug loading was determined by filtration membrane together HPLC method and the entrapment efficiency was determined by microcolumn separation together HPLC method. The in vitro release of the PTX-MWCNTs-COOH complex was studied in PBS buffer at pH 7.4(containing 1% Tween-80) with revers dialysis method. RESULTS The Zeta potential of PTX-MWCNTs-COOH complex was (-24.5±1.01) mV,the drug loading was(50.09±0.02)%,and the entrapment efficiency was (76.80±0.02)%. The cumulative release in vitro was perfect. CONCLUSION PTX-MWCNTs-COOH showed good physicochemical properties such as high drug loading and entrapment efficiency. The method of reverse dialysis can be used to study the release behavior of PTX-MWCNTs-COOH in vitro.
关键词
羧基化多壁碳纳米管 /
紫杉醇 /
磷脂 /
体外释放
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Key words
carboxylated multi-walled carbon nanotube /
paclitaxel /
phospholipid /
in vitro release
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中图分类号：
R944
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基金
国家自然科学基金项目资助(81303288);黑龙江省自然科学基金项目资助(H2015107)
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