The present invention relates to an ultrasound contrast agent with drug-encapsulating nanoparticles and a method for preparing the same that increase drug delivery capabilities and drug penetration effects. According to the present investion, exposure to the foucused ultrasound triggers the cavitation of an ultrasound contrast agent, resulting in the local release of drug-encapsulating nanoparticles, which are conjugated onto the surface of the ultrasound contrast agent, and enhaced penetration of nanoparticles and drug delivery capbilities. Moreover, the present invention simultaneously and selectively diagnoses and treats cancers by conjugation cancer-targeting ligands on the surface of nanoparticles.