Nanotechnology has enabled tremendous breakthroughs in the development of materials and, nowadays, is well established in various economic fields. Among the various nanomaterials, TiO2 nanoparticles (NPs) occupy a special position, as they are distinguished by their high availability, high photocatalytic activity, and favorable price, which make them useful in the production of paints, plastics, paper, cosmetics, food, furniture, etc. In textiles, TiO2 NPs are widely used in chemical finishing processes to impart various protective functional properties to the fibers for the production of high-tech textile products with high added value. Such applications contribute to the overall consumption of TiO2 NPs, which gives rise to reasonable considerations about the impact of TiO2 NPs on human health and the environment, and debates regarding whether the extent of the benefits gained from the use of TiO2 NPs justifies the potential risks. In this study, different TiO2 NP exposure modes are discussed, and their toxicity mechanisms—evaluated in various in vitro and in vivo studies—are briefly described, considering the molecular interactions with human health and the environment. In addition, in the conclusion of this study, the toxicity and biocompatibility of TiO2 NPs are discussed, along with relevant risk management strategies.