HIGHLIGHTS • Multifunctional TiO 2 nanostructures hold promise for advancing a wide range of biomedical applications due to a feasible integration of distinct theranostic features. • Fabrication and post-fabrication strategies implemented to generate multifunctional TiO 2 nanostructures for a broad range of biomedical applications are briefly outlined. The opportunities and challenges of TiO 2 nanomaterials are highlighted in order to open the possibility of clinical translation. ABSTRACT Titanium dioxide (TiO 2 ) nanostructures exhibit a broad range of theranostic properties that make them attractive for biomedical applications. TiO 2 nanostructures promise to improve current theranostic strategies by leveraging the enhanced quantum confinement, thermal conversion, specific surface area, and surface activity. This review highlights certain important aspects of fabrication strategies, which are employed to generate multifunctional TiO 2 nanostructures, while outlining post-fabrication techniques with anemphasis on their suitability for nanomedicine. The biodistribution, toxicity, biocompatibility, cellular adhesion, and endocytosis of these nanostructures, when exposed to biological microenvironments, are examined in regard to their geometry, size, and surface chemistry. The final section focuses on recent biomedical applications of TiO 2 nanostructures, specifically evaluating therapeutic delivery, photodynamic and sonodynamic therapy, bioimaging, biosensing, tissue regeneration, as well as chronic wound healing.