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.