Many people suffer and demise from chronic, recurrent, drug-resistant or biofilm-developing infections such as leishmaniasis, colitis and carcinogenesis throughout the globe annually. Despite the progress in medical treatment, drug resistance, adverse side effects, inadequate therapeutic index, poor bioavailability, insolubility and toxicity have hampered the disease curing process. Recently, nanotechnology-based metal nanoparticles have emerged as nanomedicine for the treatment of various diseases. Titanium dioxide nanoparticles (TiO2 NPs), owing to their unique photocatalytic characteristics, high chemical stability, excellent biocompatibility and low toxicity have attracted interest for disease-treatment. TiO2 NPs generally acts through metal ions liberation inducing oxidative and non-oxidative damages of the infected cells and micro-organisms. The attachments of pharmaceutics and ligands to TiO2 NPs may improve their targeted delivery to specific sites for sustained release of active ingredients with insignificant side-toxicity overcoming the biological barriers. The review focuses TiO2 NPs for the consideration as delivery system in combating diseases.