Abstract: AimTo prepare the targete drug delivery systems(TDDS), albendazole polybutycyanocrylate nanoparticles (ABZ-PBCA-NP)， its pharmaceutical characters and tissue distributions were simultaneously investigated. MethodsAlbendazole nanoparticles were prepared with the emulsification-polymerization method and the drug-load mechanism of polybutycyanocrylate nanoparticles was studied with the equal-tempaerature adsorption principle. The dialyse dynamic of albendazole from ABZ-PBCA-NP was investigated in four formulations in vitro. The tissue distribution of albendazole in different drug vehicles was studied with isotope labelling experiment. ResultsABZ-PBCA-NP and ABZ-PVP-PBCA-NP fit to the Higuchi and bi-exponent function in vitro respectively. The drug loaded in nanoparticles was abide by the Langmuir adsorption equation. Targeting index of albendazole in liver and spleen in mice are 11.4 and 3.9 after ig ³H-ABZ-PBCA-NP. The bioavailability of albendazole nanoparticle and suspension are 76.0% and 36.9% respectively. Conclusion The absorptive capability of drug was enhance when 4% PVP was added into the nanoparticle, and its release time was lengthen. At the same time, the nanoparticles vehicles increase the albendazole bioavailability.