Lung cancer, the second leading cause of cancer-related deaths, accounts for a substantial portion, representing 18.4% of all cancer fatalities. Despite advances in treatment modalities such as chemotherapy, surgery, and immunotherapy, significant challenges persist, including chemoresistance, non-specific targeting, and adverse effects. Consequently, there is an urgent need for innovative therapeutic approaches to overcome these limitations. Natural compounds, particularly phytoconstituents, have emerged as promising candidates due to their potent anticancer properties and relatively low incidence of adverse effects compared to conventional treatments. However, inherent challenges such as poor solubility, rapid metabolism, and enzymatic degradation hinder their clinical utility. To address these obstacles, researchers have increasingly turned to nanotechnology-based drug delivery systems (DDS). Nanocarriers offer several advantages, including enhanced drug stability, prolonged circulation time, and targeted delivery to tumor sites, thereby minimizing off-target effects. By encapsulating phytoconstituents within nanocarriers, researchers aim to optimize their bioavailability and therapeutic efficacy while reducing systemic toxicity. Moreover, the integration of nanotechnology with phytoconstituents allows for a nuanced understanding of the intricate molecular pathways involved in lung cancer pathogenesis. This integrated approach holds promise for modulating key cellular processes implicated in tumor growth and progression. Additionally, by leveraging the synergistic effects of phytoconstituents and nanocarriers, researchers seek to develop tailored therapeutic strategies that maximize efficacy while minimizing adverse effects. In conclusion, the integration of phytoconstituents with nanocarriers represents a promising avenue for advancing lung cancer treatment. This synergistic approach has the potential to revolutionize current therapeutic paradigms by offering targeted, efficient, and minimally toxic interventions. Continued research in this field holds the promise of improving patient outcomes and addressing unmet clinical needs in lung cancer management.