Drug-delivery devices are fundamentally important in improving the pharmacological profiles of therapeutic molecules. Nanocontrolled-release systems are attracting a lot of attention currently owing to their large surface area and their ability to target delivery to specific sites in the human body. In addition, they can penetrate the cell membrane for gene, nucleic acid and bioactive peptide/protein delivery. Representative applications of nanodrug-delivery systems include controlled-release wound dressings, controlled-release scaffolds for tissue regeneration and implantable biodegradable nanomaterial-based medical devices integrated with drug-delivery functions. We review the present status and future perspectives of various types of nanocontrolled-release systems. Although many of the well-established degradable and nondegradable controlled-release vehicles are being investigated for their processing into nanocarriers, several new emerging nanomaterials are being studied for their controlled-release properties. The release of multiple bioactive agents, each with its own kinetic profile, is becoming possible. In addition, integration of the nanocontrolled-release systems with other desirable functions to create new, cross-discipline applications can also be realized.