Strategies to overcome the enzymatic barrier

Abstract

Enzymatic degradation of various hydrophilic macromolecules including peptide- or protein drugs by enzymes present in the gastrointestinal tract can be regarded as one main reason for their poor bioavailability after peroral administration. Within the current chapter, strategies to overcome the so-called enzymatic barrier are described. Besides formulations that can protect the drug from enzymatic digestion via, e.g., drug encapsulation and chemical modifications of the drug itself, an emphasis has been put forward on enzyme inhibitors. © Springer Science+Business Media, LLC 2009. All rights reserved.