Soluble starch nanoparticles loaded with Gefitinib for treating lung cancer: Optimization and cytotoxicity assessment

Lung Cancer (LC) represents a catastrophically huge problem and it is a worldwide issue that has to be resolved. There is a declining confidence in classic Cancer treatments as they lack selectivity, spur widespread harm, and exacerbate the suffering of LC patients. The poor solubility and extensive cell damage of Gefitinib limit its use in treating LC. Conversely, soluble starch nanoparticles could offer a significant advancement in LC treatment. Therefore, we have designed Gefitinib-loaded soluble starch NPs (Gefitinib-StNPs) to deliver Gefitinib to A549 LC cells, aiming to maximize therapeutic efficacy and minimize cell damage. The nano-formulation was characterized by utilizing TEM, SEM, XRD, DSC, and FT-IR. The optimized Gefitinib-StNPs displayed a particle size of (145 ± 2.3 nm), an entrapment of (85.2 ± 1.7 %), and a release of (73.9 ± 1.85 %) after 1 h. Gefitinib-StNPs revealed an IC₅₀ of (9.18 ± 0.72) μg/mL compared to unloaded Gefitinib, which possessed an IC₅₀ of (23.16 ± 0.26 μg/mL). Gefitinib-StNPs experienced higher cellular uptake than unloaded Gefitinib. Additionally, the intracellular concentration of Gefitinib-StNPs stood at (3.25 ± 0.09 μg/mL), while the concentration of unloaded Gefitinib was (1.33 ± 0.02 μg/mL). Gefitinib-StNPs outmatched unloaded Gefitinib in terms of Apoptosis with %apoptosis (63.51 ± 0.58 %) and (23.1 ± 0.92 %), respectively. These outcomes confirm that Gefitinib-StNPs could be a useful tool to fight LC.

Flow cytometry; Full factorial design; Gefitinib; Lung cancer; MTT assay; Nanoparticles; Nanotechnology; Soluble starch nanoparticles.