Drug delivery emerged as a discipline to solve problems associated with the majority of the current drugs, such as poor water solubility, poor physical stability, poor absorption and side effects. Large pharmaceutical companies are investing in drug delivery technologies to find better ways to administer existing drugs rather than designing new products. The secret to a successful drug delivery system, one that allows controlled release over a prolonged period of time, is in the carrier. An ideal drug carrier must be biocompatible, biodegradable, water friendly, selective, easy to prepare, stable, cheap, and finally, ultra-small. Therefore, the interdisciplinary field of nanotechnology and nanomaterials is playing a big role in drug delivery by providing new tools to develop ideal nanocarriers and find appropriate solutions for medical problems. In this review, we briefly recapitulate the history of nanomaterials in drug delivery, explore their unique properties, and report an example of the design and development of polymerbased nanomaterials. We also revisit the most challenging applications of drug delivery for cancer treatment, cell and tissue transplantations and stem cell therapies. Overall, nanotechnology-based drug delivery systems administered by different routes can be considered promising tools to improve patient compliance and achieve better therapeutic outcomes in critical illnesses.