Nowadays, carbon-based nanostructure materials are regarded as promising carriers for
drug delivery to improve the effective treatment of diseases. The formation of covalent and noncovalent
molecular bonds can be used for surface modification of nano-carriers in order to manipulate
their toxicity, water solubility, and cellular internalization. Graphene and its derivatives have
shown important potential in drug delivery systems. Among different graphene derivatives, Graphene
Oxide (GO) is the most extensively used derivative. GO sheets have possessed certain oxygen
functional groups including carboxylic acid groups at the edges, epoxy and hydroxyl groups on the
basal planes. The oxygen groups on the surface of GO sheets enhance their capabilities for functionalization
with chemical and bioactive molecules. In this review, we highlight the recent researches
about the effect of reactive sites on the surface of GO and its derivatives in drug delivery systems.
Therefore, the application of GO and its derivatives have been discussed as a delivery system in cancer
treatment, gene therapy, and combination therapy, followed by discussions on their related issues.
Finally, the review will provide a future perspective to the applications of GO-based materials as part
of drug delivery systems, and may open up new viewpoints to motivate broader interests across these