The present work tackled the development and evaluation of inclusion complex of khellin (KH) and methyl-β-cyclodextrin (MβCD). In addition it tested its possible hypoglycemic and hypolipidemic effects. This study points for the first time that the complexation of Khellin with Methyl-βCyclodextrin could notably improve the dissolution rate and hence the bioavailability of khellin. Moreover this study demonstrated that this compound has a hypoglycemic and hypolipidemic effect. Thus it can be a promising natural supportive treatment for type 2 diabetes mellitus (T2DM).