The field of nanoscience has evolved into a wide variety of successes over the past two decades and the emphasis on nanotechnology is to revolve around various dynamic fields, such as sensor, biomedical, and many useful applications. Advances in related fields are certainly due to the ability to synthesize nanoparticles from a variety of materials, structures, and to convert samples into complex nanoarchitectures. The promises of nanomedicine are broad. Graphene (Gr), the first 2-dimensional material to stand alone, is a type of new nanomaterial that leads to the excitement of natural biological applications. Number of researches has been conducted on applicability of GBNs in the area of environment, biomedical, and healthcare sectors. As compared to other nanomaterials, extraordinary properties of graphene-based nanomaterials (GBNs) like high surface area, multilayers, multifunctional and excellent biocompatibility make them capable to play great roll of highly-tailored multifunctional delivery vehicles for drugs delivery, gene delivery, phototherapy and bioimaging. However, research communities performed plenty of research works on GBNs synthesis and biological acitivity evaluation, but  there is limited comprehensive reviews published so far biological applications. So, we have studied a large number of scientific reports and investigations, presented in this review describing recent progress and modern perspectives with respect to graphene and related nanomaterials for biological applications.