Abstract

Background: Gefitinib (GEF) is a tyrosine kinase inhibitor that has proven good efficacy against Non-small cell Lung Carcinoma (NSCLC). It has low solubility and dissolution rate and low oral bioavailability. This work aimed to improve efficacy by loading on ZSM-5 silica nanoparticles and testing the prepared delivery system on A-549 lung cancer cells. Methods: ZSM-5 was synthesized in the laboratory and different methods of loading GEF on the nanoparticles were used, then the system was characterized by X-ray diffraction, Fourier Transport Infra-Red (FTIR), and drug release and dissolution. Results and conclusion: GEF-loaded nanoparticles (NPs) showed prolonged release of GEF over 12 hours with an improved biological efficacy expressed by the decrease in IC50 compared to free GEF (P < 0.001) using 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay. Also, there was a significant decrease in migration and colony formation ability of the GEF-loaded NPs on A-549 lung cancer cells. In conclusion, loading GEF onto ZSM-5 NPs resulted in a lower IC50 and improved biological action toward A-549 cells.

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