Chitosan-functionalized graphene oxide as a nanocarrier for drug and gene delivery

Abstract

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. The covalent functionalization of graphene oxide (GO) with chitosan (CS) is accomplished via a facile method. It is demonstrated that GO-CS possesses a superior loading capacity for camptothecin (CPT), and the GO-CS-CPT complexes show remarkably high cytotoxicity in cancer cells. In addition, GO-CS is able to transport plasmid DNA into HeLa cells with a reasonable transfection efficiency. © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.