School of Mechanical and Aerospace Engineering, Nanyang Technological University, Singapore.
Small. 2011 Jun 6;7(11):1569-78. doi: 10.1002/smll.201100191. Epub 2011 Apr 28.
The covalent functionalization of graphene oxide (GO) with chitosan (CS) is successfully accomplished via a facile amidation process. The CS-grafted GO (GO-CS) sheets consist of about 64 wt.% CS, which imparts them with a good aqueous solubility and biocompatibility. Additionally, the physicochemical properties of GO-CS are studied. As a novel nanocarrier, GO-CS is applied to load a water-insoluble anticancer drug, camptothecin (CPT), via π-π stacking and hydrophobic interactions. It is demonstrated that GO-CS possesses a superior loading capacity for CPT, and the GO-CS-CPT complexes show remarkably high cytotoxicity in HepG2 and HeLa cell lines compared to the pure drug. At the same time, GO-CS is also able to condense plasmid DNA into stable, nanosized complexes, and the resulting GO-CS/pDNA nanoparticles exhibit reasonable transfection efficiency in HeLa cells at certain nitrogen/phosphate ratios. Therefore, the GO-CS nanocarrier is able to load and deliver both anticancer drugs and genes.
通过简单的酰胺化过程，成功地实现了氧化石墨烯（GO）与壳聚糖（CS）的共价功能化。接枝有 CS 的 GO（GO-CS）片层含有约 64wt%的 CS，这赋予了它们良好的水溶性和生物相容性。此外，还研究了 GO-CS 的物理化学性质。作为一种新型纳米载体，GO-CS 通过π-π堆积和疏水相互作用来负载水不溶性抗癌药物喜树碱（CPT）。实验表明，GO-CS 对 CPT 具有优异的负载能力，与纯药物相比，GO-CS-CPT 复合物在 HepG2 和 HeLa 细胞系中表现出显著更高的细胞毒性。同时，GO-CS 还能够将质粒 DNA 凝聚成稳定的纳米级复合物，所得的 GO-CS/pDNA 纳米颗粒在一定氮/磷比下在 HeLa 细胞中表现出合理的转染效率。因此，GO-CS 纳米载体能够负载和递送货载药物和基因。
