A galactosamine-mediated drug delivery carrier for targeted liver cancer therapy

In order to minimize the side effect of cancer chemotherapy, a novel galactosamine-mediated drug delivery carrier, galactosamine-conjugated albumin nanoparticles (GAL-AN), was developed for targeted liver cancer therapy. The albumin nanoparticles (AN) and doxorubicin-loaded AN (DOX-AN) were prepared by the desolvation of albumin in the presence of glutaraldehyde crosslinker. Morphological study indicated the spherical structure of these synthesized particles with an average diameter of around 200 nm. The functional ligand of galactosamine (GAL) was introduced onto the surfaces of AN and DOX-AN via carbodiimide chemistry to obtain GAL-AN and GAL-DOX-AN. Cellular uptake and kinetic studies showed that GAL-AN is able to be selectively incorporated into the HepG2 cells rather than AoSMC cells due to the existence of asialoglycoprotein receptors on HepG2 cell surface. The cytotoxicity, measured by MIT test, indicated that AN and GAL-AN are non-toxic and GAL-DOX-AN is more effective in HepG2 cell killing than that of DOX-AN. As such, our results implied that GAL-AN and GAL-DOX-AN have specific interaction with HepG2 cells via the recognition of GAL and asialoglycoprotein receptor, which renders GAL-AN a promising anticancer drug delivery carrier for liver cancer therapy. (C) 2011 Elsevier Ltd. All rights reserved