Tamoxifen is an anticancer drug which has very low oral bioavailability. It has been reported in the literature that the various P-gp and CYP3A4 enzyme inhibitors were co administered with drug to enhance their oral bioavailability. In the present report, the effect on the bioavailability of tamoxifen when co-administerd with herbal bioenhancers such as curcumin and piperine has been studied in experimental animals. The various pharmacokinetic parameters from different blood samples were determined using HPLC. It has been found that the co administration of selected bioenhancers significantly enhanced the oral bioavailability of tamoxifen.