Qun Wang,1,2,* Jian-Ying Huang,1,* Hua-Qiong Li,3 Zhong Chen,4 Allan Zi-Jian Zhao,3 Yi Wang,3 Ke-Qin Zhang,1 Hong-Tao Sun,2 Salem S Al-Deyab,5 Yue-Kun Lai1 1National Engineering Laboratory for Modern Silk, College of Textile and Clothing Engineering, Soochow University, Suzhou, 2College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou, People’s Republic of China; 3Wenzhou Institute of Biomaterials and Engineering, Chinese Academy of Sciences, Wenzhou, People’s Republic of China; 4School of Materials Science and Engineering, Nanyang Technological University, Singapore, Singapore; 5Department of Chemistry, College of Science, King Saud University, Riyadh, Saudi Arabia *These authors contributed equally to this work Abstract: Titania nanotube (TNT) arrays are recognized as promising materials for localized drug delivery implants because of their excellent properties and facile preparation process. This review highlights the concept of localized drug delivery systems based on TNTs, considering their outstanding biocompatibility in a series of ex vivo and in vivo studies. Considering the safety of TNT implants in the host body, studies of the biocompatibility present significant importance for the clinical application of TNT implants. Toward smart TNT platforms for sustainable drug delivery, several advanced approaches were presented in this review, including controlled release triggered by temperature, light, radiofrequency magnetism, and ultrasonic stimulation. Moreover, TNT implants used in medical therapy have been demonstrated by various examples including dentistry, orthopedic implants, cardiovascular stents, and so on. Finally, a future perspective of TNTs for clinical applications is provided. Keywords: TiO2 nanotubes, anodization, drug delivery, orthopedic implant