Graphene was first discovered as a sheet structure mechanically exfoliated from a block of graphite, but in recent years researchers have extended their investigations into this two‐dimensional carbon nanostructure. Various applications of graphene‐based materials have included electronics, photonics, optoelectronics, sensors, and drug / gene delivery systems. These single atom carbon layers have the potential to be formed in different morphologies e. g., quantum dots, nanosheets, and nanoparticles, which can be tailored to achieve new breakthrough innovations. Nowadays, the utilization of graphene‐based nanomaterials in medicine is a hot research topic. This review discusses the structure, properties, methods of synthesis, and surface modifications of graphene and graphene oxide divided into covalent and non‐covalent approaches.