Gefitinib is anticancer drug which is sparingly soluble in water. This limits its dissolution and bioavailability. Binary inclusion complex of gefitinib with Epi-β-CD was prepared by freeze-drying method. Stoichiometric ratio of 1:1 M was established by continuous variation (Job's) plot. The stability constant of complex as determined by phase solubility study was found to be 15,871.3 M−1. Complex was characterized by FTIR, DSC, DTA and dissolution study. Results revealed that in complex the drug no longer exist in crystalline state and is converted into amorphous form; which shows higher dissolution efficiency as compared to crystalline drug. The solubilizing efficiency for freeze dried complex was found to be 175.57 and the relative drug crystallinity degree was 87.91% as estimated by thermal analysis. Complexation led to decrease in surface tension; from 54.8 dynes/cm (pure gefitinib) to 40.3 dynes/cm (FD complex) due to adsorption phenomenon. The results obtained in this study confirmed that complexation of gefitinib with Epi-β-CD is a prominent approach and suitable tool for tailoring the issue related to its delivery and can be explored for development of an effective delivery system.