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BACKGROUND Ultrasound microbubbles have conventionally been used for diagnostic purposes. In recent years, however, new types of microbubbles have emerged as important carriers for drug delivery. Moreover, studies have shown that ultrasound microbubbles can serve as valuable and noninvasive tools in cancer therapy; thus the use of ultrasound microbubbles to deliver chemotherapeutic drugs to malignant tissues is a promising possibility. METHODS In this review, we briefly describe the status of ultrasound microbubbles in clinical practice and then discuss the development of targeted microbubbles. Finally, we consider novel strategies for the use of microbubbles in cancer therapy. RESULTS Many different kinds of microbubbles are emerged. Novel strategies of ultrasound microbubble have been shown to be effective in cancer therapy. CONCLUSION Although many problems need to be solved in the future, the ultrasound drugs loaded microbubbles still have strong potential for the use in clinical cancer therapy.