This review discusses a novel nanocarrier-based targeted therapy for lung cancer, emphasizing its potential to improve treatment outcomes. Lung cancer has a low survival rate due to late diagnosis, poor prognosis, and tumor heterogeneity, which hinder effective treatment. The study explores the role of nanocarriers in enhancing drug delivery to the tumor microenvironment (TME) by targeting specific pathways and modulating the tumor environment. Biofunctionalized nanocarriers can stimulate cellular uptake, immune escape, and vascular changes to penetrate the TME. Inorganic metal compounds can scavenge reactive oxygen species (ROS) through photothermal effects, while nanocarriers conjugated with stroma, hypoxia, pH, and immunity-modulating agents can regulate the extracellular matrix, cancer-associated fibroblasts, and immune cells. Biomimetic conjugation or surface modification of nanocarriers can enhance active targeting by bypassing the TME. A nanocarrier system with biofunctionalized inorganic metal compounds and organic drug-loaded complexes is convenient for NSCLC treatment. The review also discusses challenges in lung cancer treatment, including drug resistance, tumor heterogeneity, and biological barriers. Strategies to overcome these include vascular remodulation, stromal regulation, hypoxia manipulation, pH modulation, immunity modulation, active targeting, and tumor environment-responsive drug delivery. These strategies aim to enhance drug delivery to the TME, improve targeting efficacy, and reduce systemic toxicity. Nanocarriers, such as lipid-based nanocarriers (solid lipid nanoparticles, liposomes), can deliver drugs to the targeted site with improved bioavailability and therapeutic efficacy. The review highlights the potential of nanocarriers in overcoming the limitations of conventional therapies and improving the treatment of lung cancer.This review discusses a novel nanocarrier-based targeted therapy for lung cancer, emphasizing its potential to improve treatment outcomes. Lung cancer has a low survival rate due to late diagnosis, poor prognosis, and tumor heterogeneity, which hinder effective treatment. The study explores the role of nanocarriers in enhancing drug delivery to the tumor microenvironment (TME) by targeting specific pathways and modulating the tumor environment. Biofunctionalized nanocarriers can stimulate cellular uptake, immune escape, and vascular changes to penetrate the TME. Inorganic metal compounds can scavenge reactive oxygen species (ROS) through photothermal effects, while nanocarriers conjugated with stroma, hypoxia, pH, and immunity-modulating agents can regulate the extracellular matrix, cancer-associated fibroblasts, and immune cells. Biomimetic conjugation or surface modification of nanocarriers can enhance active targeting by bypassing the TME. A nanocarrier system with biofunctionalized inorganic metal compounds and organic drug-loaded complexes is convenient for NSCLC treatment. The review also discusses challenges in lung cancer treatment, including drug resistance, tumor heterogeneity, and biological barriers. Strategies to overcome these include vascular remodulation, stromal regulation, hypoxia manipulation, pH modulation, immunity modulation, active targeting, and tumor environment-responsive drug delivery. These strategies aim to enhance drug delivery to the TME, improve targeting efficacy, and reduce systemic toxicity. Nanocarriers, such as lipid-based nanocarriers (solid lipid nanoparticles, liposomes), can deliver drugs to the targeted site with improved bioavailability and therapeutic efficacy. The review highlights the potential of nanocarriers in overcoming the limitations of conventional therapies and improving the treatment of lung cancer.