The concept of nanomaterials that can be designed and administered into the human body to improve health is of great interest. During the past years there has been an increasing amount of research on the uses of nanomaterials in diverse areas of biomedical research including biological sensing, labelling, imaging, cell separation and therapy. In this chapter, the first evaluation of titanate nanotubes (TiONts) as potential carriers of therapeutic molecules is presented. TiONts with controlled parameters have been developed from a hydrothermal synthesis and their biomedical applications have been explored over the last decade. These nanotubes are elaborated as stable suspensions of nanocarriers by surface chemistry engineering. They can be used as transfection agents for cardiomyocytes and we have shown that TiONts can increase the ionizing effect of radiation therapy in the case of glioblastoma. Furthermore, TiONts' biodistribution has been evaluated by SPECT/CT in male Swiss nude mice and TiONts are quickly cleared. More recently, we have demonstrated that TiONts-docetaxel (DTX) nanohybrids are versatile nanocarriers to limit the systemic toxicity of taxanes and to improve the selectivity of radiotherapy (RT). Our strategy is based on the intraprostatic injection of the TiONts-DTX nanohybrids both in place of brachytherapy and in combination with RT. This is achieved by taking advantage of the TiONts' morphology as well as their radiosensitization effect and by associating them with docetaxel molecules, also recognized for their radiosensitizing potential. We also grafted the surface of TiONts with gold nanoparticles, for a resulting combined radiosensitizing effect. The elaboration of nanohybrid materials, intended for drug delivery systems and based on TiONts coated with chitosan polymer has also been evaluated. Such nanotubes are combined with transresveratrol derivatives for their anti-oxidizing and antitumor effects. All the aspects of a potential toxicity are also considered.