In vitro characterization, and in vivo studies of crosslinked lactosaminated carboxymethyl chitosan nanoparticles

The liver targeting and controlled release nanoparticles based on carboxymethyl chitosan derivatives were prepared: firstly, novel thiolated lactosaminated carboxymethyl chitosan (LAC-CMC) was synthesized, its chemical structure was characterized by H-1 NMR spectroscopy. Then, glycyrrhizic acid was chosen as model drug and encapsulated within thiolated LAC-CMC nanoparticles through ionic gelification. The crosslinked glycyrrhizic acid-loaded nanoparticles dissociated to release drug in the presence of glutathione (GSH) at a concentration comparable to the intracellular environment, featuring the potential ability of this system for intracellular delivery. Crosslinked nanoparticles modify the tissue distribution profile of the glycyrrhizic acid solution, the kidney excretion rate is reduced and the drug accumulation in the liver is increased. According to these results, the nanoparticles have the potential to be used as drug delivery system with hepatic targeting and controlled release properties. (C) 2010 Elsevier Ltd. All rights reserved.