The invention discloses a bulleyaconitine A multivesicular liposome and a preparation method thereof. The bulleyaconitine A multivesicular liposome comprises medicament active components, namely bulleyaconitine A and blank multivesicular liposome which serve as carriers; the blank multivesicular liposome comprises the following components in part by mass: 1 part of lipid component and 0.1 to 50 parts of ion gradient regulator, wherein the lipid component comprises amphiphilic lipid and neutral lipid in a molar ratio of 5-36:1. In the preparation method, the blank multivesicular liposome whichis packaged with a gradient regulator is used, bulleyaconitine A permeates a phospholipid film and enters a water phase in the blank multivesicular liposome by a transmembrane gradient active loadingmethod to obtain the bulleyaconitine A multivesicular liposome. The bulleyaconitine A multivesicular liposome has the advantages of high utilization rate of raw materials, high loading concentration,excellent sustained release effect in in-vivo/in-vitro tests and better effect of resisting tumors.