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.

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