Titania nanostructures (TNSs) provide exceptional choice for developing innovative biomedical applications due to their unique and characteristic biocompatibility, and their ability to integrate functional moieties to modulate biological responses. In this review, we provided first-hand knowledge of all contemporary TNS-based biomedical research for future innovations and benefits to society and patient care. Starting with a brief discussion on the crystallographic phases of TNSs, we presented a detailed description of the commonly used fabrication and surface modification techniques, followed by a systematic and comprehensive summary of various biomedical evaluations with a special emphasis on drug-delivery, tissue engineering, biosensor, and anti-bacterial applications.