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The present work explored the possibility of formulating oral insulin delivery system by combing the advantage of microemulsion and phospholipid complex Insulin phospholipid complex (IPC) was prepared by an anhydrous co-solvent lyophilization method.The parameters affecting formulation were characterized.The preparation has unimodal particle size distribution with a mean diameter of 27.3±0.2nm.The results of bioactivity evaluation indicated that insulin was able to withstand the preparation procedure.Insulin was protected from enzymes by incorporation into oil phase.The IPC-microemulsion was effective in enhancing insulin transport across caco-2 cell monolayers.The IPC-microemulsion especially the IPC-W/O microemulsion was effective in reducing blood glucose level in diabetic animal models.Phospholipid complex based microemulsion appear to be an interesting candidate for oral delivery of insulin.