Delivery of the drug to the pulmonary region is rapidly growing and the lungs offer a diversity of advantages compared to oral drug delivery. The respiratory tract is an attractive target for delivery of drugs for both local and systemic effect. Chitosan is broadly used as a carrier for controlled drug delivery, owing to its considerable chemical and biological properties such as bioactivity, biocompatibility, and biodegradability. Absorption of systemically acting drugs administered through pulmonary route is performed to establish bioavailability and biodistribution. Chitosan-based aerosolized nanoparticles of itraconazole, administered through the pulmonary route demonstrated greater efficacy by virtue of their greater pulmonary deposition. Chitosan nanocarriers are an attractive drug delivery vehicle for treatment of both local and systemic lung diseases. Biodegradable polymeric nanoparticles especially chitosan nanoparticles may exhibit a sustained release effect. Chitosan nanoparticles loaded with isoniazid were prepared by an iontropic gelation method for controlled delivery of the drug to the pulmonary region.