Cyclodextrin-Based Niosomal Delivery of Imatinib against A549 Nonsmall Cell Lung Cancer Cells

High Resolution Image Download MS PowerPoint Slide Lung cancer remains a significant cause of cancer-related deaths globally. The effective cancer treatment aims to deliver drugs that specifically target cancer cells at the optimal dose. Imatinib (IMB), a selective kinase inhibitor, has demonstrated therapeutic efficacy against lung cancer. However, its use is often limited because of low solubility in water. This study investigated water-soluble IMB/cyclodextrin (CD) inclusion complex formation. IMB demonstrated a high affinity for γCD and HPγCD, as evidenced by phase-solubility studies, solid- and solution-state characterizations, and molecular docking study. IMB/CD complex-loaded niosomes in the presence and absence of D-alpha-tocopheryl polyethylene glycol succinate (TPGS) were fabricated using a thin-film hydration method. The prepared niosomal formulations showed nanoscale particle sizes (126–163 nm) with a low polydispersity index (<0.2), a negative zeta potential value (−3.65 to −13.67 mV), and % entrapment efficiency of 59–78%. The novel TPGS-based niosomes loaded with the IMB/CD complex significantly enhanced cellular uptake and induced apoptosis in A549 cells, exhibiting potent cytotoxicity with an IC 50 value of 5 μM. These results indicate that our developed IMB/CD complex-loaded niosomes could be promising for efficient IMB delivery to nonsmall cell lung cancer A549 cells and potentially contributing to future lung cancer therapy.