In recent years, nanotechnology has led to significant scientific and technological advances in diverse fields, specifically within the field of medicine. Owing to the revolutionary implications in drug delivery, nanotechnology-based drug delivery systems have gained an increasing research interest in the current medical field. A variety of nanomaterials with unique physical, chemical and biological properties have been engineered to develop new drug delivery systems for the local, sustained and targeted delivery of drugs with improved therapeutic efficiency and less or no toxicity, representing a very promising approach for the effective management of diseases. The utility of nanotechnology, particularly in the field of orthopedics, is a topic of extensive research. Nanotechnology has a great potential to revolutionize treatment, diagnostics, and research in the field of orthopedics. Nanophase drug delivery has shown great promise in their ability to deliver drugs at nanoscale for a variety of orthopedic applications. In this review, we discuss recent advances in the field of nanostructured drug delivery systems for orthopedic applications.