Lung cancer is the second most diagnosed cancer in both men and women worldwide. Considering the high mortality rate of lung cancer and inadequacy of conventional treatment methods such as surgical resection, chemotherapy and radiotherapy; new treatment strategies are an emerging area of interest. Nanoparticle-based drug and small interfering RNA delivery systems such as lipid, polymeric, inorganic, micellar and dendrimer nanoparticles are designed to enhance the bioavailability, stability and retention of anti-cancer drugs in the targeted regions of the lung. These nanoparticle-based delivery systems increase the active ingredient half-life and targeting efficiency while reducing the required dose of the drug. Hence, they have many advantages such as higher therapeutic efficacy and reducedside effects and adverse events. Combinations of active ingredients, anti-cancer agents and small interfering RNA can be formulated into nanoparticle-based delivery systems that can be administered by various routes including inhalation and intravenous. In this review, the development of lipidic and polymeric nanoparticle-based drug and small interfering RNA delivery systems used in the treatment of lung cancer is discussed.