In recent years, the utilization of nanocarriers has significantly broadened across a diverse spectrum of biomedical applications. However, the clinical translation of these tiny carriers is limited and encounters hurdles, particularly in the intricate landscape of the tumor microenvironment. Lung cancer poses unique hurdles for nanocarrier design. Multiple physiological barriers hinder the efficient drug delivery to the lungs, such as the complex anatomy of the lung, the presence of mucus, immune responses, and rapid clearance mechanisms. Overcoming these obstacles necessitates a targeted approach that minimizes off-target effects while effectively penetrating nanoparticles/cargo into specific lung tissues or cells. Furthermore, understanding the cellular uptake mechanisms of these nano carriers is also essential. This knowledge aids in developing nanocarriers that efficiently enter cells and transfer their payload for the most effective therapeutic outcome. Hence, a thorough understanding of biological cues becomes crucial in designing multifunctional nanocarriers tailored for treating lung cancer. This review explores the essential biological cues critical for developing a flexible nanocarrier specifically intended to treat lung cancer. Additionally, it discusses advancements in nanotheranostics in lung cancer.