Sonodynamic therapy (SDT) is a newly developed anticancer treatment where ultrasound is used to trigger the cytotoxic effect of chemical compounds, known as sonosensitizers. Although SDT is similar to photodynamic therapy (PDT), SDT activates the chemical compounds through energy transfer using ultrasound rather than light. Moreover, SDT can focus the ultrasound energy onto malignant sites situated deeply within tissues, thus overcoming the main drawback linked to the use of PDT. Several physical and chemical mechanisms underlying ultrasound bioeffects and anticancer SDT take advantage of the non-thermal effect of acoustic cavitation generated by selected pulsed or continuous ultrasound. As the physical-chemical structure of the sonosentizer is essential for the success of SDT, we believe that the different aspects related to nanotechnology in medicine might well be able to improve the triggering effect ultrasound has on sonosensitizing agents. Therefore, the aim of this review is to focus on how nanotechnology might improve this innovative anticancer therapeutic approach.