Central nervous system leukemia (CNS-L) is a fatal complication with low remission, high relapse and high death rates in leukemia. Because the existence of blood brain barrier (BBB) hinders drug from going into CNS, therefore it is urgent that to develop a new drug delivery system by which drug can highly and effectively go through BBB. Searching home and abroad literatures from December 2012 to February 2014 found a scheme which may effectively treat the CNSL, that is, ultrasonic microbubbles loading Ara-C, which changes the cell membrane permeability and increases the intercellular space by cavitation effect so as to make the Ara-C through the BBB for therapy. This review focuses on the present status of CNSL treatment and the progress of treating CNSL with ultrasonic microbubbles loading drug.