Graphene, an allotrope of carbon, is a two dimensional one atom thick carbon sheet arranged in a honey comb lattice structure. Following its discovery, a lot of interesting work has been carried out to explore the use of graphene in both medical and non-medical fields. The graphene and their derivatives possess overwhelming properties such as amphiphilicity, surface functionality, fluorescence quenching ability, Surface Enhanced Raman scattering property (SERS), high mechanical strength, high thermal and electrical conductivity and so on. Biomedical application of graphene is a new fascinating area that is beyond imagination. Graphene and GO has been known to be used as a carrier for drug delivery, gene therapy, bioimaging, biosensors, antibacterial composites and scaffold for cell culture in tissue regeneration. The wide spread application of graphene concomitantly increases human and environmental exposure. Despite the increase in scientific interest and potential application, there is a great concern on the safety and toxicity of graphene materials which is not well established. The putative hazard arises from the exposure to graphene needs to be addressed before certifying its use for biomedical application. This chapter confers knowledge on different synthetic routes of graphene materials, biomedical applications and safety issues when living organisms are exposed.