Dengning Xia,1, Jinsong Tao1, Yuan He1,2, Fude Cui3, Yong Gan1*
1. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; 2. Department of Pharmaceutics, School of Pharmaceutical Science, Chongqing Medical University, Chongqing 400016, China; 3. Department of Pharmaceutics, School of Pharmaceutical Science, Shenyang Pharmaceutical University, Shenyang 110016, China
A non-sheddable nanocage stabilizer was designed to anchor wheat germ agglutinin (WGA) to surface of itraconazole (ITZ) nanocrystals. The shedding WGA from crystal surface could be greatly reduced by the nanocage. Animal study indicated that the WGA nanocage stabilized nanocrystals (WGA-cage-NC) could largely accumulate on the epithelium surface. Surprisingly, we also found that the WGA-cage-NC could reach to lamina propria of intestinal villus via goblet cells. The WGA-cage-NC resulted in an oral bioavailability of 2.41-folds and 1.68-folds higher than that of ordinary nanocrystals (ONC) and WGA functionalized nanocrystals by physical absorption (WGA-NC), respectively.