The transport characteristics of peptide and proteins drugs across various epithelial membrane barriers are outlines. These include transport through the intestinal, buccal, nasal and pulmonary absorptive mucosae, as well as transdermal penetration. Because peptides and proteins are hydrophilic and high molecular weight compounds, they commonly show minor permeability across the mentioned biological membranes. In order to improve their transport properties and thereby their systemic bioavailability, several strategies can be undertaken, such as the synthesis of stabilized and lipophilic analogues, the application of absorption enhancers and protease inhibitors, and the design of suitable dosage forms (e.g., liposomes, biodegradable nanocapsules, bioadhesive microspheres).