Microbubble-assisted ultrasound has emerged as a promising method for the delivery of low molecular weight chemotherapeutic molecules, nucleic acids, therapeutic peptides and antibodies in-vitro and in-vivo. Its clinical applications are under investigations for local delivery drug in oncology and neurology. However, the biophysical mechanisms supporting the acousticallymediated membrane permeabilization are not fully established. This review describes the present state of the investigations concerning the acoustically-mediated stimuli (i.e., mechanical, chemical and thermal stimuli) as well as the molecular and cellular actors (i.e., membrane pores, endocytosis) involved in the reversible membrane permeabilization process. The different