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。