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Pulmonary delivery of drugs has grown to be a smart target and gained remarkable scientific and biomedical attention in the health care research area as the lung is capable of absorbing pharmaceuticals for local deposition as well as systemic delivery. In this respect, growing interest has been given to the potential of a pulmonary route as an attractive non-invasive route of administration for systemic and local delivery of therapeutics, on account of the high permeability, large absorptive surface area, and good blood supply in the lungs. The integration of therapeutics with polymeric nanoparticles offers further degrees of manipulation for drug delivery systems, providing sustained release and the facility to target specific cells as well as organs. On the other hand, nanoparticle delivery to the lungs has a lot of challenges counting formulation instability as a result of particle–particle interactions and poor delivery effectiveness attributable to exhalation of low-inertia nanoparticles. Hence, novel methods for formulating inhalable nano-particulate dry powders have been developed. These transporter particles show better handling and delivery while releasing nanoparticles upon deposition in the lungs. This chapter covers the anatomy of the respiratory system, significance of particulate-based pulmonary drug delivery, lung compatibility of formulation excipients/polymers, fundamental properties of powders used in drug delivery by inhalation, modes of pulmonary administration, mechanism of deposition and clearance of particles in lungs, factors affecting drug bioavailability via pulmonary route, devices for pulmonary delivery, nanoparticle-based lung therapy, and technical issues of nanoparticle applications.
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