Gefitinib-Loaded Polymeric Nanoparticles for Non Small Cell Lung Cancer (NSCLC): Advantages, Targeted Delivery and Therapeutic Potential

Abstract

Non-small cell lung cancer (NSCLC) is one of the leading causes of cancer-related deaths worldwide and accounts for nearly 85% of all lung cancer cases. Gefitinib, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, is widely used in the treatment of NSCLC, especially in patients with EGFR mutations. However, conventional gefitinib therapy faces several limitations such as poor water solubility, low bioavailability, non-specific drug distribution, systemic side effects, and development of drug resistance. To overcome these drawbacks, polymeric nanoparticles have emerged as a promising drug delivery system. Gefitinib-loaded polymeric nanoparticles improve drug solubility, enhance bioavailability, provide sustained and controlled drug release, and enable targeted delivery to tumor tissues through passive and active targeting mechanisms. Various biodegradable polymers such as PLGA, chitosan, PEG, and PCL are commonly used in nanoparticle formulation due to their biocompatibility and controlled release properties. Different preparation methods including emulsion solvent evaporation, ionic gelation, nanoprecipitation, and microfluidic techniques are employed to develop stable nanoparticles with high drug encapsulation efficiency. These nanoformulations demonstrate improved cellular uptake, enhanced anticancer activity, reduced systemic toxicity, and potential to overcome gefitinib resistance in NSCLC treatment. Therefore, gefitinib-loaded polymeric nanoparticles represent a promising and advanced therapeutic approach for improving the effectiveness and safety of NSCLC therapy.