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表皮生长因子功能化单壁碳纳米管用于依托泊苷的靶向递药。

EGF-functionalized single-walled carbon nanotubes for targeting delivery of etoposide.

机构信息

Jiangsu Key Laboratory for Supramolecular Medical Materials and Applications, College of Life Sciences, Nanjing Normal University, Nanjing, People's Republic of China.

出版信息

Nanotechnology. 2012 Feb 3;23(4):045104. doi: 10.1088/0957-4484/23/4/045104. Epub 2012 Jan 6.

Abstract

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.

摘要

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。

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