Posted by 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 IC50 value of 5 μM. These results indicate that the 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.
Hay Marn Hnin, Theingi Tun, Chaisak Chansriniyom, Natsaranyatron Singharajkomron, Varisa Pongrakhananon, Thorsteinn Loftsson, and Phatsawee Jansook (2025) Cyclodextrin-Based Niosomal Delivery of Imatinib against A549 Nonsmall Cell Lung Cancer Cells. ACS Omega Article ASAP
https://doi.org/10.1021/acsomega.5c06264