Abstract The formation of supramolecular host-guest inclusion complex of amitriptyline [AP] and - Cyclodextrin [-CD] have been studied in solution state. The stoichiometric ratio of the inclusion complexes between AP and -CD in solution state is confirmed by the absorption and fluorescence spectroscopic tehniques. The binding constant value has been calculated for the 1:1 complex by using Benesi-Hildebrand equation. An in-vitro cytotoxic performance also checked for pure AP and its inclusion complex with -CD and the inclusion complex clearly had shown that the no change after making AP towards inclusion complex with -CD.