Ticagrelor-loaded lipid nanocapsules as a promising nebulizable system for lung cancer: in-vitro characterization, 131I radiolabeling and in-vivo biodistribution

Abstract

This study investigates the encapsulation of Ticagrelor (Tic) within lipid nanocapsules (LNCs) as a potential nebulizable drug delivery system for the treatment of lung cancer. The prepared LNCs were evaluated through in-vitro characterization, including dynamic light scattering (DLS) and surface morphology. Additionally, an in-vivo biodistribution study was conducted after radiolabeling the selected Tic-LNCs with iodine-131 (¹³¹I) to assess their distribution and deposition within various body organs. Results indicated that the Tic-LNCs had a particle size ranging from 137.5 ± 0.4 nm to 340.15 ± 17.3 nm. The in-vitro cytotoxicity using the MTT assay showed that Tic-LNCs exerted a substantial inhibitory effect against A549 lung cancer cells, with IC₅₀ values of Tic and Tic-LNCs being 21.72 ± 1.22 μg/mL and 3.42 ± 0.103 μg/mL, respectively. The in-vivo biodistribution study revealed that the ¹³¹I-Tic-LNCs demonstrated significantly better lung uptake compared to the parent drug solution. The lung-to-blood ratio for the Tic-LNCs reached a maximum of 2.67 within 4 h after administration. In conclusion, the nebulizable Tic-LNCs nanosystem holds promise as a targeted pulmonary drug delivery system for the treatment of lung cancer.