The invention discloses a high-efficiency, targeted drug-loaded nano-micelle and its preparation method and application. The preparation steps are: (1) dissolving the amphiphilic block copolymer in an organic solvent, and then adding a small-molecule anti-leukemia drug Hydrochloride, after fully dissolved and mixed, add triethylamine to remove hydrochloric acid to form a small molecule anti-leukemia drug, and then add it to PBS buffer to form nanomicelles with inner core encapsulated drug and outer shell hydrophilic; after dialysis, dry , to obtain drug-loaded nanomicelles; the polydopamine modification method is used to modify the specific antibody against the leukemia cell surface antigen to achieve targeting. The particle size of the drug-loaded nano-micelle prepared by the invention is 50-100nm, showing good monodispersity, high drug-loading capacity and encapsulation efficiency, simple targeting modification steps, and good targeting leukemia cell killing effect , while for normal cells, it has high biological safety and can achieve slow release, avoiding the disadvantages of long-term and multiple administrations.