The development of active targeting DDS nanoparticles is gaining attention in malignant tumor and other disease treatments that are seeking DDSs that do not produce side-effects. In the present work we have prepared two types of sugar-chain remodeled glycoprotein-lipo some conjugates. These liposomal particles had a mean diameter of 100 nm, and maintained stable properties for several months. The lectin-binding affinity of 3'-sialyl-Lewis X-type sugar-chain-bearing liposomes was specific toward E-Selectin, and the dissociation constant was estimated to be in the level of about 300 pM. The uptake of 3'-sialyl-Lewis X-type sugar-chain-bearing liposomal nanoparticles was predominant for solid tumor tissue. These results emphasize the importance of structural features of sugar-chain ligands on the membrane surface of liposomal nanoparticles. (C) 2004 Elsevier B.V. All rights reserved.