The present invention provides an ultrasound-mediated drug delivery method for administering a compound to a targeted tissue, and the method at least comprises the following steps: First, an ultrasound apparatus is provided. The compound is then administered to the targeted tissue. A sonication is performed by the ultrasound apparatus to a blood vessel of the targeted tissue after the administration of the compound, and the sonication is capable of enhancing the permeability of the blood vessel to allow the administration of the compound to the targeted tissue. An ultrasound-mediated drug delivery system is also disclosed here.
