Oral delivery has distinct advantages over parenteral administration. These include ease of administration and improved patient compliance. Physiological barriers to oral drug delivery include low pH environment of the stomach, high enzymatic activity of the small intestine, and poor permeability of large molecular weight and hydrophilic compounds across the gastrointestinal epithelial layer. These barriers reduce stability and absorption of drug molecules to the systemic circulation. In order to overcome these barriers, nanopreparations have been investigated for their potential in oral delivery. In this chapter, selected nanoscale formulations investigated for oral drug delivery are discussed.Handbook of Nanobiomedical Research Downloaded from www.worldscientific.com by UNIVERSITY OF QUEENSLAND on 02/03/15. For personal use only.