Motivated by the accomplishment of carbon nanotubes (CNTs), graphene and graphene oxide (GO) has been widely investigated in the previous studies as an innovative medication nanocarrier for the loading of a variety of therapeutics as well as anti-cancer medications, poor dissolvable medications, antibiotics, antibodies, peptides, DNA, RNA and genes. Graphene provides the ultra-high drug-loading efficiency due to the wide surface area. Graphene and graphene oxide have been widely investigated for biomedical applications due to their exceptional qualities: twodimensional planar structure, wide surface area, chemical and mechanical constancy, sublime conductivity and excellent biocompatibility. Due to these unique qualities, GO applications provide advanced drug transports frameworks and transports of a broad range of therapeutics. In this review, we discussed the latest advances and improvements in the uses of graphene and GO for drug transport and nanomedicine. Initially, we have described what is graphene and graphene oxide. After that, we discussed the qualities of GO as a drug carrier, utilization of GO in drug transport applications, targeted drug transport, transport of anticancer medications, chemical control medicine releasee, co-transport of different medications, comparison of GO with CNTs, nano-graphene for drug transport and at last, we have discussed the graphene toxicity. Finally, we draw a conclusion of current expansion and the potential outlook for the future.