Due to a rapid development in biotechnologymore and more macromolecular
drugs such as therapeutic peptides, oligosaccharides and nucleic acids are
entering the pharmaceutical arena representing unprecedented challenges
from the drug delivery point of view. One of the likely greatest challenges is
their oral administration presenting a series of attractive advantages. These
advantages are in particular of high relevance for the treatment of pediatric
patients and include the avoidance of additional risks, pain and discomfort
associated with injections. Furthermore, oral formulations are less expensive
to produce, as they do not need to be manufactured under sterile conditions.
The oral administration is by far the most favored one. The majority (84%)
of 50 most-sold pharmaceutical products in US and Europe markets are given
orally. Although there have been major advances in delivering
macromolecular drugs in humans by other non-invasive routes, including
the pulmonary delivery of insulin, we did so far not succeed in the
development of oral delivery systems for these therapeutic agents. Apart
from a few exceptions such as ciclosporin, desmopressin, chondroitin
sulphate and bromelain macromolecular drugs cannot be administered
orally. The development of oral formulations for macromolecular drugs is
therefore highly on demand. Due to the scientific progress having been made
within the 1990s and this decade numerous novel oral delivery systems for
macromolecular drugs are meanwhile subject of clinical trials. This book
addresses the most critical issues for a successful oral delivery of
macromolecular drugs by a detailed characterisation of the ‘enemy’s
strength’.