Nowadays, respiratory diseases have become the major cause of health care burded and death worldwide. According to the WHO, pulmonary disease holds the third position for mortality and supplement the development of antimicrobial resistance among immune-compromised patience are increasing the complication in health. Approximately, 65 million people are suffering from chronic obstructive pulmonary disease, 334 million are suffering from asthma, 10 million are suffering from tuberculosis, and 2.3 million are suffering from lung cancer. Different conventional methods have been used to treat these diseases, but certain limitations of conventional therapy limit their efficacy and efficiency. Hence, this leads to the exploitation of new therapeutic approaches as conventional approaches are not that much effective. Among the available alternatives, the targeted nanodrug delivery system (NDDS) has gained significant attention concerning their ability, activity, and tolerability to control these pulmonary diseases. Additionally, NDDS has associated advantages like a controlled deposition, controlled release of drugs and appropriate size for systemic and local treatment. This chapter plans to highlight the efficacy and physiological aspects of the targeted drug delivery, mechanism of pulmonary drug administration. Moreover, it will also discuss the different nanocarriers for drug delivery. As a better insight into the challenges and complications associated with developing the pulmonary disease will propose new opportunities to pharmacists to minimize the medical and technical gaps.