The purpose of this study was to present novel intravenous itraconazole-loaded nanoparticles (ITZ-NPs) using human serum albumin (HSA) as drug carrier materials. The ITZ-NPs were prepared by nanoparticle albumin bound technology involving a series of homogenization and lyophilization procedures. The ITZ-NPs powder could be easily reconstituted and provide stable solutions at a wide range of concentrations at 25 degrees C for 24h. In safety test, the ITZ-NPs caused mild hemolysis below the concentration of 10mg/mL and were well tolerated at the dose of 160 mg/kg in mice, indicating better biocompatibility than cyclodextrin formulation of itraconazole (ITZ-CD). The pharmacokinetic parameters of itraconazole and its major metabolite, hydroxyl-itraconazole, of ITZ-NPs had no differences from those of ITZ-CD in mice. For the ITZ-NPs group, the distributions of itraconazole in the lung, liver and spleen were higher than those for ITZ-CD group. It was of significance that ITZ-NPs increased the drug distribution in lung which was always the portal to fungal infection. These results indicate that the ITZ-NPs can be a potential intravenous formulation of itraconazole.