International regulatory initiatives toward regulation of nanomaterials indicate an adaptive and flexible approach to identify and study its interaction with biological systems and its impact over the quality, safety, and efficacy of the product. Current focus remains on identification of critical physicochemical or biological parameters and endpoints, development of new techniques of manufacturing, harmonized testing methodologies, and standards for health, safety, and toxicity-related issues with regard to nanomedicines. Possibilities of better treatment approaches and huge market potential became the driving force for national initiatives that pumped adequate funds to motivate research and strategy development in the field of nanomedicines. New approaches carry uncertainties and risks. Regulatory agencies have performed commendable progress in terms of risk assessment and their management in terms of occupational safety, environmental protection, and health-related approaches. Science-based regulatory policies, harmonized good practices, guidance documents, and standards shall definitely unveil the potential of nanomedicines for the betterment of our healthcare system.