A new drug delivery modality was developed based on drug encapsulation in polymeric micelles followed by a controlled release at the tumor site triggered by ultrasound focused on the tumor. Ultrasound not only released drug from micelles but also enhanced the local uptake of both free and encapsulated drug by tumor cells, thus providing effective drug targeting. The significant success of in vitro studies of this new drug delivery technique warranted extending studies to animal experiments. Here the results of the in vitro studies of the above technique are summarized and the first in vivo experiments using colon cancer model in rats are reported. The in vivo results showed that application of low-frequency ultrasound (20 and 70 kHz) significantly reduced the tumor size when compared with non-insonated controls; this result indicated in vivo drug targeting to tumors by ultrasound.