Development and Evaluation of Tumor-Targeting Curcumin-Loaded Magnetic Nanoparticles Based on PEG-PLGA and Transferrin for Anti-Lung Cancer Therapy

This study developed transferrin (Tf) -functionalized magnetic nanoparticles (Tf-MNP-PEG-PLGA-Cur) to enhance curcumin (Cur)’s therapeutic potential for lung cancer. Tf-MNP-PEG-PLGA-Cur was synthesized by chemically coupling Tf (tumor-targeting ligand) to the surface of MNP-PEG-PLGA-Cur. Its size and morphology were measured, in vitro drug release was evaluated via dialysis, oral bioavailability and tissue distribution were studied in rats and mice. Cytotoxicity to normal cells was tested by CCK-8, A549 cell uptake was observed by confocal laser microscopy, and in vitro anti-lung cancer activity was studied using MTT assay. In vivo, its distribution in tumor-bearing nude mice was detected by near-infrared imaging, followed by measuring tumor growth and histopathological observation. Tf-MNP-PEG-PLGA-Cur nanoparticles had a small size (137.39 ± 3.72   nm, PDI 0.224 ± 0.010) with a biphasic release pattern, longer half-life (P<0.05), and 186% relative oral bioavailability. It promoted Cur accumulation in tissues, especially liver and spleen. Both Tf-MNP-PEG-PLGA-Cur and Cur showed good cytocompatibility. Tf-MNP-PEG-PLGA-Cur enhanced curcumin's anti-lung cancer activity in vitro and in vivo, indicating good tumor-targeting. H&E staining showed it protected nude mice's vital organs and inhibited tumor growth. Tf-MNP-PEG-PLGA-Cur is a promising polymeric sustained-release curcumin preparation, improving oral bioavailability and anti-lung cancer activity.