Oral delivery of chemotherapeutic agents still remains a challenging area as most of the chemotherapeutic agents are either not bioavailable or have very low bioavailabilty due to their poor solubility, stability and permeability. It has been found that the orally administered anticancer drugs would be eliminated either by metabolic enzymes like cytochrome P450 or by the efflux transporters like P-gp. Hence the present study is aimed to develop a dual loaded microparticulate system (Drug and P-gp herbal modulator) to enhance the bioavailability of the selected anticancer agent by P-gp modulation.