ABSTRACT
This chapter provides an overview of pulmonary drug-targeting strategies that are
discussed from a number of different perspectives. An initial section on general
considerations discusses the structure of the pulmonary epithelial membrane and
considers the various factors affecting drug clearance and absorption through the
pulmonary epithelial membrane. There is a section on recent advances in the
design of drug molecules, which reviews recent research in the design of drug
molecules for pulmonary receptor targeting and addresses new areas of
pulmonary drug discovery and development. A section on structural factors
governing the uptake of drugs into the lung discusses the structural requirements
for the selective uptake and how these data may be used in drug targeting to the
respiratory tract. The use of prodrugs for lung targeting and extending drug
activity in the lung is addressed in the section on prodrug approaches. A section
on the potential utility of cell membrane-bound drug entities deals with
the possible usefulness of pulmonary cell membrane-bound enzymes or
receptors as targets for drugs covalently linked to respective substrates or
agonists and inhibitors or antagonists of these membrane-bound entities. The
section on conjugation of drugs focuses on drug conjugation with
macromolecules for selective targeting of the lung, which is followed by a
section on the use of bioadhesives in drug targeting to pulmonary tissues. A
section on the use of drug-monoclonal antibody conjugates for drug targeting to
the lung is followed by a concluding section on the future direction of research in
this exciting area of pulmonary drug targeting.