Receptor-targeted, drug-loaded, functionalized graphene oxides for chemotherapy and photothermal therapy.
Receptor-targeted, drug-loaded, functionalized graphene oxides for chemotherapy and photothermal therapy.
复制标题
DOI：
10.2147/ijn.s105401
复制
发表时间：
2016
影响因子：
8
通讯作者：
Kim JO
中科院分区：
文献类型：
--
作者：
Thapa RK;Choi JY;Poudel BK;Choi HG;Yong CS;Kim JO
癌症是全球主要的死亡原因之一。尽管已经开发了不同的化学治疗剂来治疗癌症，但它们的使用可能受到低细胞摄取、耐药性和副作用的限制。因此，不断开发靶向药物递送系统以改善化疗剂的功效。本研究的主要目的是制备叶酸（FA）缀合的聚乙烯吡咯烷酮官能化氧化石墨烯（GO）（FA-GO）用于索拉非尼（SF）的靶向递送。使用改进的Hummer方法制备GO，随后改变以制备FA-GO和负载SF的FA-GO（FA-GO/SF）。使用紫外/可见光谱、傅里叶变换红外光谱、X-射线衍射、原子力显微镜、zeta电位测量和体外药物释放的测定进行GO衍生物的表征。还研究了FA-GO/SF的溶血毒性、体外细胞毒性、细胞摄取和凋亡作用。结果表明，成功地合成了GO，进一步转化为FA-GO提高了SF的稳定性和载药能力。此外，在酸性条件下增强的SF释放表明对癌症治疗可能有益。FA-GO/SF递送系统内FA的缀合使得能够将SF靶向递送至表达高水平FA受体的癌细胞，从而增加SF的细胞摄取和凋亡作用。此外，通过将GO暴露于近红外辐射实现的光热效应增强了FA-GO/SF的抗癌效果。总之，FA-GO/SF是一种潜在的癌症化疗药物靶向递送载体。
Cancer is one of the leading causes of death worldwide. Although different chemotherapeutic agents have been developed to treat cancers, their use can be limited by low cellular uptake, drug resistance, and side effects. Hence, targeted drug delivery systems are continually being developed in order to improve the efficacy of chemotherapeutic agents. The main aim of this study was to prepare folic acid (FA)-conjugated polyvinyl pyrrolidone-functionalized graphene oxides (GO) (FA-GO) for targeted delivery of sorafenib (SF). GO were prepared using a modified Hummer’s method and subsequently altered to prepare FA-GO and SF-loaded FA-GO (FA-GO/SF). Characterization of GO derivatives was done using ultraviolet/visible spectroscopy, Fourier transform infrared spectroscopy, X-ray diffraction, atomic force microscopy, zeta potential measurements, and determination of in vitro drug release. Hemolytic toxicity, in vitro cytotoxicity, cellular uptake, and apoptotic effects of FA-GO/SF were also investigated. The results revealed that GO was successfully synthesized and that further transformation to FA-GO improved the stability and SF drug-loading capacity. In addition, the enhanced SF release under acidic conditions suggested possible benefits for cancer treatment. Conjugation of FA within the FA-GO/SF delivery system enabled targeted delivery of SF to cancer cells expressing high levels of FA receptors, thus increasing the cellular uptake and apoptotic effects of SF. Furthermore, the photothermal effect achieved by exposure of GO to near-infrared irradiation enhanced the anticancer effects of FA-GO/SF. Taken together, FA-GO/SF is a potential carrier for targeted delivery of chemotherapeutic agents in cancer.