Sonodynamic therapy (SDT) which employs ultrasound-triggered sonosensitizers to generate reactive oxygen species (ROS) has been proved to be effective for treatment of cancers. However, it is still desirable for sonosensitizers to be delivered to tumors as effectively as possible. In this study, we prepared the hematoporphyrin monomethyl ether (HMME)-loaded liposome as the sonosensitizers for SDT and evaluated their effects on human MCF-7 breast cancer cells in vitro and in vivo. Liposomes prepared by thin film hydration technique were about 100 nm in size with positive zeta potential and exhibited spherical in shape. Following irradiation of ultrasound which generates intracellular ROS, the liposome facilitated the delivery of HMME to tumor cells. HMME-loaded liposomes showed low cytotoxicity under basal condition but significant sonodynamic effects under ultrasonic irradiation. Notably, HMME-loaded liposomes exhibited spatial distribution of HMME in tumor tissues of mice. The promoted delivery of HMME into the tumors by liposomes was shown by the greater tumor growth inhibition than free HMME after 20-day treatment. Taken together, these results show that HMME-loaded liposome functions as a promising sonosensitizer for SDT, implying the efficient antitumor effects of HMME-based SDT on breast tumor.