Phosphorylcholine oligomer-grafted graphene oxide for tumor-targeting doxorubicin delivery
Phosphorylcholine oligomer-grafted graphene oxide for tumor-targeting doxorubicin delivery
复制标题
磷酸胆碱低聚物接枝氧化石墨烯用于肿瘤靶向阿霉素递送
DOI：
10.1039/c7ra08287h
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发表时间：
2017-01-01
期刊：
影响因子：
3.9
通讯作者：
Zhang, Tao
中科院分区：
文献类型：
--
作者：
Qin, Yu;Wang, Changyu;Zhang, Tao
设计并制备了一种新型的磷酸胆碱寡聚体接枝叶酸标记的氧化石墨烯（GO-PCn-FA），并通过傅里叶变换红外光谱、核磁共振、拉曼光谱、X射线衍射、X射线光电子能谱、扫描透射电子显微镜、透射电子显微镜和原子力显微镜对其进行了表征。GO-PCn-FA被证明是一种优良的水溶性和pH响应性药物载体，用于靶向递送阿霉素（DOX），载药量为21%。体外细胞毒性试验和流式细胞术分析显示，GO-PCn-FA的上级生物相容性相比，正常细胞，而DOX负载GO-PCn-FA发挥有效的根除肿瘤细胞，特别是那些与叶酸受体表达。体内试验表明，静脉给药后GO-PCn-FA主要沉积于肺实质，未见明显不良反应。总之，磷酸胆碱低聚物接枝的氧化石墨烯被开发用于具有最佳生物相容性的靶向药物递送。
A novel phosphorylcholine oligomer-grafted and folate moiety-labeled graphene oxide (GO-PCn-FA) was designed, prepared, and characterized by Fourier transform infrared spectra, nuclear magnetic resonance, Raman spectra, X-ray diffraction, X-ray photoelectron spectroscopy, scanning transmission electron microscopy, transmission electron microscopy, and atomic force microscopy. GO-PCn-FA proved to be an excellent water-soluble and pH-responsive drug carrier for the targeted delivery of doxorubicin (DOX) with a drug loading content of 21%. An in vitro cytotoxicity assay and flow cytometry analysis revealed the superior biocompatibility of GO-PCn-FA compared to normal cells, while DOX-loaded GO-PCn-FA exerted efficient eradication of tumor cells, especially of those with folate receptor expression. An in vivo test showed that GO-PCn-FA was deposited mainly in the pulmonary parenchyma after intravenous administration, and no obvious adverse effect was observed. In summary, phosphorylcholine oligomer-grafted graphene oxide was developed for targeted drug delivery with optimal biocompatibility.