College of Chemistry and Chemical Engineering, Central South University, Changsha, Hunan 410083, PR China.
College of Chemistry and Chemical Engineering, Central South University, Changsha, Hunan 410083, PR China.
Mater Sci Eng C Mater Biol Appl. 2018 Aug 1;89:316-327. doi: 10.1016/j.msec.2018.04.031. Epub 2018 Apr 14.
A stimuli-responsive polypyrrole (PPy) nanotubes drug carrier system has been designed to deliver anticancer drugs to tumor cells in a targeted and controlled manner. The PPy nanotubes drug carrier was fabricated by a template method. The nanotubes surface was functionalized with cleavable acylhydrazone and disulfide bonds by attaching thiolated β-cyclodextrin (β-CD). The solubilizing poly(ethylene glycol) polymer (PEG), attached with an adamantane (Ad) entity at one end and a folate (FA) entity at the other end, was introduced onto the nanotubes surface via β-cyclodextrin-adamantane interaction. The synthesized FA-PEG-Ad-β-CD-PPy showed excellent biocompatibility and low cytotoxicity for two cell lines. Doxorubicin (Dox) loaded FA-PEG-Ad-β-CD-PPy nanotubes showed a triggered in vitro drug release behavior in the presence of acidic media and reducing agents. The folate-mediated endocytosis and intracellular release of Dox-loaded nanoparticles were confirmed by fluorescence microscopy and cell viability evaluations. In the in vitro study, Dox loaded within the nanoparticles showed enhanced selectivity for cancerous cells and reduced cytotoxicity for normal cells compared to free Dox. The PPy based targeted drug vehicle shows excellent promise for drug delivery.
设计了一种对刺激响应的聚吡咯（PPy）纳米管药物载体系统，以靶向和控制方式将抗癌药物递送到肿瘤细胞。通过模板法制备 PPy 纳米管药物载体。通过将巯基化的 β-环糊精（β-CD）连接到纳米管表面上，纳米管表面被功能化有可裂解的酰腙和二硫键。将一端连接有金刚烷（Ad）实体、另一端连接有叶酸（FA）实体的可溶性聚乙二醇（PEG）通过β-环糊精-金刚烷相互作用引入到纳米管表面。合成的 FA-PEG-Ad-β-CD-PPy 对两种细胞系表现出优异的生物相容性和低细胞毒性。在酸性介质和还原剂存在下，负载 FA-PEG-Ad-β-CD-PPy 纳米管的阿霉素（Dox）表现出触发的体外药物释放行为。通过荧光显微镜和细胞活力评估证实了载药纳米颗粒中阿霉素的叶酸介导的内吞作用和细胞内释放。在体外研究中，与游离 Dox 相比，载药于纳米颗粒中的 Dox 对癌细胞表现出增强的选择性和降低的细胞毒性。基于 PPy 的靶向药物载体在药物传递方面具有广阔的应用前景。
