The present work tackled the development and evaluation of inclusion complex of khellin (KH) and methyl-beta-cyclodextrin (MbetaCD). In addition, it tested its possible hypoglycemic and hypolipidemic effects. This study points for the first time that the complexation of Khellin with Methyl-betaCyclodextrin 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).