Abstract: Objective :To investigate the rabbit's blood drug level and pharmacokinetics (PK) pa-rameter of 10- hydroxycamptothec (HCPT) nanoparticle injection and to detected the tissue distributionperformance in mice. Methods :HCPT in plasma and tissues was quantitated by reversed-phase HPLCand L1V detector. EXCEL software was used in drawing the plasma concentration-time curves, and3p97 software was used in calculation of compartment model and PK parameters. HCPT nanoparticleinjection was administered to BALB/c mice by bolus injection at dose of lOmg kg‘body weight. Druglevels in various tissues was detected at post injection time of 15, 60 and 120 min. Results :a, the concentration- time profile for HCPT nanoparticle injection could be best described by three-compartmentmodel, and the PK parameter transformed following the dose ascend in a certain range; b, the highestconcentration of HCPT nanoparticle injection was obtained in liver, and the sequence of HCPT levels invarious tissues was: liver>kidney>spleen>stomach> lung>heart; c, HCPT nanoparticle injection was ob-viously accumulated in liver. Conclusions :HCPT nanoparticle injection can be distributed into organsmore extensively and can reflect great liver targeting capability.