Intestinal mucosa permeability following oral delivery of wheat germ agglutinin non-sheddable nanocage stabilized nanocrystals

Category

Overcoming Barriers in the GI Tract

Year

2014

Authors

Dengning Xia,, Jinsong Tao, Yuan He Fude Cui, Yong Gan

Institutions

Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; Department of Pharmaceutics, School of Pharmaceutical Science, Chongqing Medical University, Chongqing 400016, China; Department of Pharmaceutics, School of Pharmaceutical Science, Shenyang Pharmaceutical University, Shenyang 110016, China

Summary

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.