In past years with the advances of chemistry and material sciences, the development of nanotechnology brought generations of nanomaterials with specific biomedical properties. These include the nanoparticle-based drug delivery, nanosized drugs, and nanomaterials for tissue engineering. The present article focuses on the use of nanomaterials in controlled drug release. The applications of nanomaterials with nano-enabled drug release characteristics brought many benefits when compared to the traditional (bulk) materials. We discuss the current advances and propose some future directions for the technology development.