天津医药

天津医药 ›› 2015, Vol. 43 ›› Issue (8): 852-855.doi: 10.11958/j.issn.0253-9896.2015.08.006

• 细胞与分子生物学 • 上一篇    下一篇

大内径多壁碳纳米管基靶向缓释载药系统的制备及性能

孟艾，杨涛，王娉婷，王剑，隋磊   

  1. 1天津医科大学口腔医院（邮编300070）；2四川大学华西口腔医院
  • 收稿日期:2014-10-15 修回日期:2015-03-01 出版日期:2015-08-15 发布日期:2015-08-15
  • 通讯作者: 隋磊 E-mail:suilei@tmu.edu.cn
  • 作者简介:孟艾（1989），女，硕士，主要从事材料方面研究
  • 基金资助:
    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）

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

MENG Ai, YANG Tao, WANG Pingting, WANG Jian, SUI Lei   

  1. 1 Department of Prosthodontics, Hospital of Stomatology, Tianjin Medical University, Tianjin 300070, China; 2 Department of Prosthodontics, West China Hospital of Stomatology, Sichuan University
  • Received:2014-10-15 Revised:2015-03-01 Published:2015-08-15 Online:2015-08-15
  • Contact: Lei SUI E-mail:suilei@tmu.edu.cn

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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。

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

Abstract: 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 puri⁃ fied and oxidized，then use nanocarriers and USTs as homologous blockers. Folic acid and fluorescent labels were conjugat⁃ ed 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 load⁃ ing 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 dem⁃ onstrated, and the accumulating release time was 18 h. DDS exhibited a certain kind of tumor-targeting property, and inhibit⁃ ed 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 tu⁃ mor cells and had a significant antitumor effect.

Key words: nanotubes, carbon, cisplatin, antineoplastic agents, drug carriers, delayed-action preparations, multiwalled carbon nanotubes, property, release profile