Due to nanomaterials? potential benefits for diagnosis and treatment, they are widely used in medical applications and personal care products. Interaction of nanomaterials, which are very small in size, with tissue, cell and microenvironment, can reveal harmful effects that cannot be created with chemically identical and larger counterparts in biological organisms. In this review, a challenge for future medicine, nanotoxicity of nanomaterials is discussed. A detailed review of related literature was performed and evaluated as per medical applications of nanomaterials their toxicity. Most authors state ?the only valid technology will be nanotechnology in the next era?; however, there is no consensus on the impact of this technology on humankind, environment and ecological balance. Studies dealing with the toxic effect of nanomaterials on human health have also varied with developing technology. Nanotoxicology studies such as in-vivo-like on 3D human organs, cells, advanced genetic studies, and -omic approaches begin to replace conventional methods. Nanotoxicity and adverse effects of nanomaterials in exposed producers, industry workers, and patients make nanomaterials a double-edged sword for future medicine. In order to control and tackle related risks, regulation and legislations should be implemented, and researchers have to conduct joint multidisciplinary studies in various fields of medical sciences, nanotechnology, nanomedicine, and biomedical engineering.