Covalently Combining Carbon Nanotubes with Anticancer Agent: Preparation and Antitumor Activity

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• 作者：Wei Wu ; Rutian Li ; Xiaochen Bian ; Zhenshu Zhu ; Dan Ding ; Xiaolin Li ; Zhijun Jia ; Xiqun Jiang ; Yiqiao Hu
• 刊名：ACS Nano
• 出版年：2009
• 出版时间：September 22, 2009
• 年：2009
• 卷：3
• 期：9
• 页码：2740-2750
• 年卷期：0
• ISSN：1936-086X

文摘

A multiwalled carbon nanotube (MWNT)-based drug delivery system was developed by covalently combining carbon nanotubes with the antitumor agent 10-hydroxycamptothecin (HCPT) using hydrophilic diaminotriethylene glycol as the spacer between nanotube and drug moieties. The surface functionalizations of the nanotube were carried out by enrichment of carboxylic groups with optimized oxidization treatment, followed by covalently linking hydrophilic diaminotriethylene glycol via amidation reaction, and then HCPT was chemically attached to carbon nanotubes through a cleavable ester linkage. It is demonstrated that the obtained MWNT−HCPT conjugates are superior in antitumor activity both in vitro and in vivo to clinical HCPT formulation. In vivo single photon emission computed tomography (SPECT) imaging and ex vivo gamma scintillation counting analyses reveal that MWNT−HCPT conjugates have relatively long blood circulation and high drug accumulation in the tumor site. These properties together with the enhanced cell uptake and multivalent presentation of HCPT on a single nanotube benefit substantially the antitumor effects and would boost significantly the applications of carbon nanotubes in the biomedicine field.