Need for an oral replacement to parenteral delivery has led to renewed attentiveness in excipients like intestinal permeation enhancers which improve oral drug bioavailability. Delivery of a drug by oral route is predominantly restricted by pre-systemic degradation and poor penetration across the gut wall. The major challenge in the oral drug delivery is the development of novel dosage forms to endorse absorption of poorly permeable drugs across the intestinal epithelium. Fifty years ago research on oral absorption enhancers that increases gut permeability was first commenced yet clinical success yet to be achieved. Development has been troubled by lack of adequate reproducibility interest as well as perceived safety concerns. We reviewed some selected permeation enhancement techniques that are advantageous for increasing permeability of poorly permeable drugs.