Tuberculosis is a fatal disease caused by Mycobacterium tuberculosis with highest morbidity and mortality every year. The evolution of anti-TB drugs is promising in controlling and treating TB. Yet, the drug response varies depending on the bacterial load and host immunological profiles. The prolonged anti-TB treatment regimen and high pill burden leads to poor adherence to treatment and acquired drug resistance. In the clinical arena, sustainable nanotechnology improves the targeted strategies leading to enhance therapeutic recovery with minimum treatment duration and virtuous drug adherence. Determinants of nanosystems are the size, nature, formulation techniques, stable dosing patterns, bioavailability and toxicity. In the treatment of chronic illness, nanomedicines inclusive of biological macromolecules such as lipids, peptides, and nucleic acids occur to be a successive alternative to synthetic carriers. Most biological nanomaterials possess antimicrobial properties with other intrinsic characteristics. Recently, the pulmonary delivery of anti-TB drugs through polymeric nanocarrier systems is shown to be effective in achieving optimal drug levels in lungs for longer duration, enhanced tissue permeation and sustained systemic clearance. This thematic review provides a holistic insight into the nanodelivery systems pertinent to the therapeutic applications in pulmonary tuberculosis describing the choice of carriers, optimized process, metabolic action and excretion processes.