Titanium dioxide (TiO2) has been utilized for decades in a variety of applications and is thought to be a safe and harmless substance. TiO2-based nanomaterials have emerged as promising candidates for various biomedical applications due to their unique properties, including biocompatibility, photocatalytic activity, and large surface area. These nanomaterials have been extensively studied for their potential use in drug delivery, tissue engineering, cancer therapy, and antibacterial applications. In this chapter, we will discuss the recent advances in the development of TiO2-based nanomaterials for biomedical applications and highlight their potential impact on healthcare. Furthermore, the study will also encompass the examination of composite nanostructures containing titanium dioxide, with a focus on their surface and bulk characteristics, to analyze the existing difficulties and potential opportunities.