Anticancer drugs embedded in or conjugated with nanocarriers have shown obvious therapeutic advantages over carrier-free drugs,yet they still face the problems like low drug loading capacity,possible systemic toxicity.Herein,we demonstrate a new concept which involves first preparation of pure drug into nanoparticles and then the functionalization of NPs with amphipathic surfactant through to achieve good biocompatiblity.As a proof of concept,10-HydroxyCamptothecin (HCPT) was chosen as a model anticancer drug to demonstrate the effectiveness of this strategy.Such modified NPs exhibit excellent dispersity and stability in physiological saline and high drug loading content and great in vitro anti-cancer activity.Significantly,HCPT NPs are readily conjugated with targeting agents to afford a targeted drug delivery system,which exhibits significantly enhanced drug efficacy and specific receptor-positive tumor cells with high selectivity.This strategy can be generally extended to other hydrophobic drugs to achieve biocompatible nanoparticles for efficient drug delivery.