Jiangsu Key Laboratory for Supramolecular Medical Materials and Applications, College of Life Sciences, Nanjing Normal University, Nanjing, People's Republic of China.
Nanotechnology. 2012 Feb 3;23(4):045104. doi: 10.1088/0957-4484/23/4/045104. Epub 2012 Jan 6.
To enhance the therapeutic potential of etoposide (ETO), we devised a targeted drug delivery system (TDDS) of epidermal growth factor-chitosan-carboxyl single-walled carbon nanotubes-ETO (EGF/CHI/SWNT-COOHs/ETO) using modified SWNTs (m-SWNTs) as the carrier, EGF-functionalized SWNTs (f-SWNTs) as the targeted moiety and ETO as the drug. After SWNT-COOHs were conjugated with CHI (CHI/SWNT-COOHs/ETO), they displayed high solubility and stable dispersion in aqueous solution. The drug loading capacity was approximately 25-27%. The m-SWNTs and f-SWNTs had only slight cytotoxicity. ETO was released from EGF/CHI/SWNT-COOHs/ETO at low pH and taken up by tumour cells via adenosine triphosphate (ATP)-dependent endocytosis. The cell death induced by EGF/CHI/SWNT-COOHs/ETO was as much as 2.7 times that due to ETO alone. In summary, these results demonstrated that our TDDS had a greater anticancer effect than free ETO in vitro.
为了提高依托泊苷（ETO）的治疗潜力，我们设计了一种表皮生长因子-壳聚糖-羧基单壁碳纳米管-依托泊苷（EGF/CHI/SWNT-COOHs/ETO）的靶向药物传递系统（TDDS），使用改性单壁碳纳米管（m-SWNTs）作为载体，表皮生长因子功能化的单壁碳纳米管（f-SWNTs）作为靶向部分，依托泊苷（ETO）作为药物。在 SWNT-COOHs 与 CHI（CHI/SWNT-COOHs/ETO）偶联后，它们在水溶液中表现出高溶解度和稳定的分散性。载药量约为 25-27%。m-SWNTs 和 f-SWNTs 的细胞毒性只有轻微的毒性。在低 pH 值下，依托泊苷（ETO）从 EGF/CHI/SWNT-COOHs/ETO 中释放出来，并通过三磷酸腺苷（ATP）依赖性内吞作用被肿瘤细胞摄取。EGF/CHI/SWNT-COOHs/ETO 诱导的细胞死亡比单独使用依托泊苷（ETO）高 2.7 倍。总之，这些结果表明，我们的 TDDS 在体外比游离依托泊苷（ETO）具有更强的抗癌作用。
