Functionalized Graphene Oxide Nanoparticles for Cancer Cell-Specific Delivery of Antitumor Drug

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• 作者：Xubo Zhao ; Liangwei Yang ; Xiaorui Li ; Xu Jia ; Lei Liu ; Jin Zeng ; Jinshan Guo ; Peng Liu
• 刊名：Bioconjugate Chemistry
• 出版年：2015
• 出版时间：January 21, 2015
• 年：2015
• 卷：26
• 期：1
• 页码：128-136
• 全文大小：577K
• ISSN：1520-4812

文摘

The unique reduction-triggered functional graphene oxide nanoparticles (GON) with well-defined size and uniform distribution were designed as an innovative drug delivery platform for cancer treatment for the first time, via the redox radical polymerization of methacrylic acid from the polyethylene glycol (PEG) modified GON (GON-PEG), following by cross-linking with cystamine. Thermogravimetric analysis demonstrates that the typical PMAA₂-GON-PEG carriers contain about 16 wt % PEG segments and 33 wt % poly(methacrylic acid) (PMAA) brushes. PEG moieties are incorporated to make the drug delivery platforms stealthy during blood circulation. Notably, introducing the cross-linked PMAA brushes efficiently minimizes the premature release of doxorubicin (DOX) in the stimulated normal tissues, and accelerates DOX release in the stimulated tumor tissues through response to reduce agent. The carriers showed a 6-fold faster releasing rate at pH 5.0 in the presence of 10 mM glutathione (GSH) (stimulated tumor tissues) than at pH 7.4 with 10 渭M GSH (stimulated normal tissues). In vitro cytotoxicity test also showed that the cross-linked PMAA₂-GON-PEG (CPMAA₂-GON-PEG) carriers had remarkable cytocompatibility, and that the DOX-loaded CPMAA₂-GON-PEG had excellent killing capability to SiHa cells.