大内径多壁碳纳米管基靶向缓释载药系统的制备及性能  

Preparation and performance of LID-MWCNT based sustained release targeted drug delivery system

作　　者：孟艾[1] 杨涛[1] 王娉婷[1] 王剑[2] 隋磊[1] 

机构地区：[1]天津医科大学口腔医院,300070 [2]四川大学华西口腔医院

出　　处：《天津医药》2015年第8期852-855,I0001,共5页Tianjin Medical Journal

基　　金：天津市应用基础及前沿技术研究计划项目(11JCYBJC10100);四川省科技支撑计划项目(2014SZ0201);教育部留学回国科研启动基金(2013-693-11-8)

摘　　要：目的制备大内径多壁碳纳米管(LID-MWCNT)基靶向抗肿瘤药物缓释系统,分析其功能特性并检测其对肿瘤细胞的增殖抑制作用。方法纯化、切割LID-MWCNT,制备碳管载体及同源封堵物超短LID-MWCNT(UST)。碳管表面负载靶向分子叶酸(FA)及荧光标记分子;管内负载抗肿瘤药物顺铂(CDDP),并以UST封堵药物通道。观察载药系统显微形态;测定载药率及药物释放曲线;观察载药系统对肿瘤细胞的靶向趋化状况及增殖抑制效应。结果成功制备大内径多壁碳纳米管基靶向抗肿瘤药物缓释系统(CDDP@UST-FA-LID-MWCNT),其载药率为70.97%。体外释放呈双相缓释模式,持续释放时间约18 h。载体系统具备了一定靶向趋化能力;较低载药浓度的CDDP@UST-FA-LID-MWCNT即对肿瘤细胞具有增殖抑制作用,且随着药物浓度的增加,抑制作用增强。结论载药系统CDDP@UST-FA-LID-MWCNT具有较高的载药率及良好的药物缓释效果,能够靶向作用于肿瘤细胞,具有较强的抗肿瘤作用。Objective To prepare a targeted antitumor drug delivery system using large-inner-diameter multi-walled carbon nanotubes （LID-MWCNTs） for sustained release and to study its performance. Methods LID-MWCNTs were purified and oxidized,then use nanocarriers and USTs as homologous blockers. Folic acid and fluorescent labels were conjugated onto the external surfaces of nanocarriers. CDDP （cisplatin） was encapsulated and ultrashort tubes （USTs） were employed to block the drug entry/exit paths. The microstructure of resulted drug delivery system （DDS） was observed, while drug loading efficiency and drug release profile in vitro were determined. The tumor-targeting property and cytotoxicity of DDS were also assessed. Results LID-MWCNT based sustained release targeted drug delivery system was established. Drug loading efficiency of CDDP@UST-FA-LID-MWCNTs was as high as 70.97%. A typical biphasic sustained release pattern was demonstrated, and the accumulating release time was 18 h. DDS exhibited a certain kind of tumor-targeting property, and inhibited proliferation of tumor cells in a dose-dependent manner. Conclusion CDDP@UST-FA-LID-MWCNT drug delivery system exhibited an improved drug loading efficiency and a sustained drug release profile. It could specifically target the tumor cells and had a significant antitumor effect.

关 键 词：纳米管 碳 顺铂 抗肿瘤药 药物载体 迟效制剂 多壁碳纳米管 靶向作用 释放模式 

分 类 号：R318.08[医药卫生—生物医学工程]