Objective： To prepare amphotericin B-polybutylcyanoacrylate-loaded nanoparticle （AmB-PBCA-NP） and to assess their ability to pass the blood-brain barrier. Methods.- AmB-PBCA-NP was prepared by incubation, with the surface modified by polysorbate 80. High-performance liquid chromatography （HPLC） method was established using acetonitrile and water （40 ： 60, 4% of acetic acid） as mobile phase; detection was done at 405 nm. Mice were divided into 3 groups： AmB- injected, AmB-lipid-injected, and AmB-PBCA-NP-injected group. Brain-targeting ability of AmB-PBCA-NP was then evaluated by determination of AmB concentrations in mice brain and other specimens. Results： The mean diameter of the prepared AmB- PBCA-NP was 94.38 nm; the mean entrapment efficiency of the particles was 82% ; and the drug loading rate was 56.10%. It was found that AmB alone failed to pass the blood-brain barrier; only very low level of AmB was detected in AmB-lipid group 3 h after injection; moderate concentration of Amb was detected 30 min after injection of AmB-PBCA-NP and the concentration peaked at 133 ng/g 3 h after injection. Conclusion： AmB-PBCA-NP modified by polysorbate 80 can pass the blood-brain barrier