Tuberculosis (TB), an infectious disease caused by the bacillus Mycobacterium tuberculosis.According to world Health Organization (WHO) global TB report 2017, India accounts for about a quarter of the global TB burden.As per current therapy point of view, combination of antibiotics administered either by oral or parenteral route.The pulmonary route is noninvasive method of drug delivery, for both local and systemic delivery of an active pharmaceutical ingredient. Rifampicin (RIF) is one of the first line drug used in treatment of tuberculosis. The dose of RIF when orally given is 10mg/kg (maximum 600mg/day) daily. Since the minimum inhibitory concentration of RIF is only 0.005-0.2 mig/ml after a usual 600mg dose, there is a need to decrease the dose and thus decreasing the high dose related side effects such as skin rashes, immunological reactions, hepatotoxicity etc. Lung targeted drug delivery system is one of the approach to reduce dose related side effects of RIF. This overview enabled to conclude that Nanostructured Lipid Carrier could serve as viable option in targeting M. tb infected alveolar macrophages by pulmonary route.