There has been an increasing interest in pulmonary drug delivery and lung tissue regeneration to treat lung disorders in the past two decades. This route of administration is advantageous for both systemic as well as local drug delivery due to the large surface area available in the lung for drug absorption, higher permeability to solutes, and the noninvasive nature of treatment. Inhalational drug delivery is also highly beneficial for the diagnosis and treatment of lung diseases such as pulmonary arterial hypertension, cystic fibrosis, asthma, and lung cancer. Statistics show that lung cancer alone is responsible for nearly 1.3 million deaths worldwide every year, necessitating the need for alternative treatment methods, which can cure the disease while reducing discomfort to the patient. This chapter attempts to summarize the different types of nanoparticles (NPs) currently available for pulmonary drug delivery, the various targeting mechanisms for drug delivery and uptake, the applications of these NPs, and the current challenges faced in inhalational drug delivery. Further, the lung half-life of the NPs and their clearance rate from the lung following administration will also be discussed.