Galactosylated chitosan-polycaprolactone nanoparticles for hepatocyte-targeted delivery of curcumin

Galactosylated chitosan-polycaprolactone (Gal-CH-PCL) copolymers with a galactosylation degree of around 10% and varied PCL percentages less than 40 wt% were synthesized and used to produce nanoparticles for delivering curcumin. Some nanoparticles with encapsulation efficiency of 70% or higher and sizes changing from 100 to 250 nm were able to deliver curcumin in a controlled manner. PCL content in Gal-CH-PCLs was found to be a key factor for governing the release behavior of nanoparticles. Hepatocyte-targeted characteristic of nanoparticles was confirmed using human hepatocellular carcinoma (HepG2) cells. In comparison to free curcumin, curcumin-loaded Gal-CH-PCL nanoparticles well retained its anticancer activity. At an equivalent curcumin-dose of around 20 mu g/mL that was found to be relatively safe to human normal liver cells, the results obtained from flow-cytometry revealed that some optimized Gal-CH-PCL nanoparticles showed more than 6-fold increasing abilities to induce the apoptosis and necrosis of HepG2 cells during 72 h treatment compared to free curcumin. (C) 2013 Elsevier Ltd. All rights reserved.