The purpose of this study was to examine whether Vitamin E-TPGS had a function in promoting the secretion of chylomicrons in enterocytes. Therefore, we simulated the human intestinal epithelial cells by Caco-2 cell model to study the effect of Vitamin E-TPGS on the chylomicron secretion in vitro. Meanwhile, chylomicron flow blocking rat model and mesenteric lymph cannulated rat model were used for the studies in vivo to evaluate the effect and probucol was chosen as the model drug. The results of cell experiments indicated that Vitamin E-TPGS at low concentration had a strong enhancement on the secretion of chylomicrons. The results of animal experiments indicated that Vitamin E-TPGS could significantly enhance the lymphatic transport of probucol by the same role consistently with the results obtained from cell experiments. However, the role would reach the plateau and saturate after a concentration dependent increase. These studies first demonstrate the function of Vitamin E-TPGS in the intestinal lymphatic transport of lipophilic drugs, which can significantly promote the secretion of chylomicrons by the intestinal epithelial cells.