Elucidation of siRNA complexation efficiency by graphene oxide and reduced graphene oxide

Abstract

Gene therapy has attracted tremendous attention as a promising method for the treatment of many diseases. Graphene oxide (GO), the oxidized form of graphene, is showing lot of potential in this field. Indeed, the polar GO oxygenated functional groups make this material highly hydrophilic, leading to a good dispersibility in water. Until now, the interaction of small interference RNA (siRNA) with graphene materials has not been elucidated. The main goal of this work was to develop a novel platform to complex siRNA molecules and to rationalize the supramolecular interactions between GO surface and the double strand RNA. Our study focused first on green and facile methods such as hydrothermal or vitamin C treatments to prepare graphene oxides at various percentage of oxygen. Epoxidation was also explored to reintroduce epoxide groups on reduced GO for further functionalization. Subsequently, we performed the covalent functionalization of GO with triethyleneglycoldiamine (TEG) and with low molecular weight polyethyleneimine (PEI) via the epoxy ring opening reaction. Finally, by gel electrophoresis, we were able to correlate the GO complexation ability with the graphene surface chemistry. In addition, ozonated GO functionalized with PEI showed a high complexing capacity for siRNA, proving to be a promising candidate for gene silencing.