An oral form of insulin has been the elusive goal for many investigators si
nce the protein's initial discovery by Banting and Best in 1922. This paper
will attempt to answer why this is the case by describing the substantial
barriers to the development of oral insulin formulations. Following this de
scription, specific strategies to overcome the barriers to oral insulin adm
inistration will be discussed. Most notably, the use of permeation enhancer
s, protease inhibitors, enteric coatings and polymer microsphere formulatio
ns will be covered, including commentary on which methods hold more promise
towards the successful development of oral insulin. (C) 1999 Elsevier Scie
nce B.V. All rights reserved.