Optimised nano-formulation on the bioavailability of hydrophobic polyphenol, curcumin, in freely-moving rats

This study has optimised the poly lactic-co-glycolic acid (PLGA) nano-formulation of curcumin to prolong its retention time in the body and improve bioavailability. High-pressure emulsification-solvent-evaporation was designed to obtain curcumin-loaded PLGA nanoparticles (C-NPs) prepared with 2% of PVA containing 20% sucrose as aqueous phase and dichloromethane as oil phase. The size and entrapment efficiency of C-NPs was 158 +/- 10 nm and 46.6 +/- 13.5%, respectively. The stable storage time of C-NPs was one month at 4 degrees C. When curcumin was formulated, a significant increase of curcumin exposure in rat plasma was revealed from the intravenous study (AUC/Dose raised 55%) and the oral study (AUC/Dose increased 21-fold). The oral bioavailability of curcumin at C-NPs was 22-fold higher than conventional curcumin. Excretion results support oral study that absorption of curcumin was significantly increased by nano-formulation. These findings demonstrate that PLGA nano-formulation could potentially be applied to increase bioavailability of hydrophobic polyphenols. (C) 2011 Elsevier Ltd. All rights reserved.