Abstract: The liver targeting and sustained release hydroxycamptothecin polybutylcyanoacrylate nanoparticles(HCPT-PBCA-NP) which were wrapped up with ployvinylpyrrolidone(PVP) were prepared by adsorption-enwrapping method. The morphology, size and size distribution, drug loading, release characteristics in vitro , distribution and pharmacokinetic parameters in animals of the PVP-HCPT-PBCA-NP were studied. The results showed that the average diameter was 81.2 nm, drug loading was 1.22%. The release characteristics in vitro was in accord with Higuchi equation: Q =0.0615+0.0940t. 64.5% of the HCPT were concentrated in liver 15 min after iv PVP-HCPT-PBCA-NP. The plasma drug concentration time curve of the HCPT in 5 rabbits was fitted to a two compartment open model. The Vc was 3.548 L; T_1/2 was 146.99 h; CL was 0.178 L·h^-1. The method of preparation presented in this paper seems to have important reference value for the preparation of PBCA-NP of the insoluble drugs both in water and in oil.