Sonodyanmic Therapy (SDT) is a new type of cancer therapy and has attracted lots of research attention recently. In this article, we present how nano-formulation helped SL052 to form a water soluble sono/photo-sensitize nanoparticle (SL052-NPs) for cancer treatment. The nanostructure formation encapsulates SL052 and greatly improves the SL052 physicochemical properties without modifying its chemical structure. Nano-formulation also helps SL052 to achieve deep-site cancer delivery, image function for diagnosis, and ultrasound or photo controlled localized cancer therapy.