Abstract: An optimum procedure was established for preparing mitoxantrone albumin microspheres (DHAQ-BSA-MS) with emulsion-heating solidification. The morphology, diameters, drug loading, release characteristics, stability and its distribution in vivo of the drug loaded albumin microspheres were studied. The results showed that the surface was regular, the average diameter was 0.99 μm, mean surface diameter was 1.24 μm and mean volume diameter was 1.44 μm, apprarent drug loading was 2.558±0.101 μg·mg^-1(n=5), effective drug loading was 1.503%±0.127%(n=5), embeding ratio was 92.82%±6.48% (n=5), and the release characteristics were in accord with "iphase kinetics equation": 1-Q=0.6428e^-0.2132t+0.3988e^-0.00150t(γ₁=-0.9951,γ₂=-0.9982);T_1/2α=3.250 h,T_1/2β=461,7 h. The stability of the drug loadeled albumin microspheres was good after three months storage at room temprebure. The results determined by HPLC showed that the drug accumulated about 77.6%±1.38% of the dose in the liver 20 minutes after intravenous injecton to mice. This indicates that DHAQ-BSA-MS showed remakable targeting for liver, and it seems to have important value for increasing the antihepatoma effect and decreasing the toxicity of mitoxantrone.