: Though many active chemotherapeutics have been developed, they are not suitable for the treatment of brain diseases because of the blood-brain barrier(BBB), which limiting the therapeutic effect of the drug in clinical applications. The technique referred as ultrasound-targeted microbubble destruction (UTMD) can lead to non-invasive and reversible BBB disruption, thus improving the efficiency of drug delivery across biological barriers. This paper introduces the molecular structure and transport function of the blood-brain barrier, besides elaborates the influencing factors and related countermeasures which can realize the delivery of transporting the drugs into the brain, furthermore analyzes the deep mechanism and the safety of the disruption of blood-brain barrier in the pattern of ultrasound, finally, discusses the application of the ultrasound-mediated drugs delivery in clinical treatment.