Owing to its exceptional electronic, mechanical, thermal, as well as optoelectronic characteristics, graphene—a planar sheet with one-atom thickness and made of carbon atoms closely packed in quite a honeycomb crystal lattice—has already earned special consideration. The investigated characteristics or even applications of such a two-dimensional configuration of the structure of carbon have already created novel innovative opportunities in place of all of the future devices as well as nanosystems. These graphene systems have also been recognized as a potential drug-delivery carrier intended for target specific or even controlled drug delivery, which could be designed by utilizing various internal or external stimuli. This review predominantly focuses on graphene's synthesis and derivative, design of stimuli-responsive nanosystems, and applications in various fields. It is highlighted that with remarkable progress in graphene-related research, graphene's overall execution has a long road ahead to go.