Bioadhesion and enhanced bioavailability by wheat germ agglutinin-grafted lipid nanoparticles for oral delivery of poorly water-soluble drug bufalin.

Wheat germ agglutinin (WGA)-grafted lipid nanoparticles has been prepared and its in vitro association with Caco-2 cells has been studied previously. The purpose of this study was to further investigate the potential of WGA-grafted lipid nanoparticles for oral delivery of bufalin, a poorly water soluble drug, by evaluating its ex vivo bioadhesion with intestinal mucosal segments and in vivo bioavailability. A significant higher adhesion between WGA-grafted lipid nanoparticles and intestinal mucosa was found compared with that of WGA-free lipid nanoparticles (p<0.05). The in vivo pharmacodynamic studies were performed by oral administration of WGA-grafted lipid nanoparticles and suspensions to fasted rats. Compared with suspensions, WGA-grafted lipid nanoparticles showed much larger AUC and C(max), and a 2.7-fold improvement in oral bioavailability. These results illustrate the potential utility of WGA-grafted lipid nanoparticles for oral delivery of a poorly water-soluble drug such as bufalin.