Enhanced Allicin Cytotoxicity on HEPG-2 Cells Using Glycyrrhetinic Acid Surface-Decorated Gelatin Nanoparticles

The cytotoxic potential of allicin was evaluated on different cancer cell lines, particularly, hepatic (HepG-2), breast (MCF-7), lung (A-549), and prostatic (PC-3), where allicin scored an IC50 score of 19.26 mu M on HepG-2. In order to increase the cell uptake, optimized allicin-loaded gelatin nanoparticles (GNPs) were prepared where the optimum formulation was surface-conjugated to glycyrrhetinic acid. GNPs were optimized using a D-optimal design. The optimum formulation had a particle size of 370.7 +/- 6.78 nm and polydispersity index of 0.0363 +/- 0.009 and 39.13 +/- 2.38% of drug entrapment. The conjugation of the ligand, glycyrrhetinic acid with allicin-loaded GNPs, was confirmed utilizing H-1 NMR. Drug release profiles in the presence/absence of collagenase were obtained. Finally, a cytotoxicity study on HepG-2 was performed for the unconjugated and conjugated allicin-loaded GNPs scoring IC50 of 10.95 and 5.046 mu M, revealing two- and fourfold enhancements in allicin cytotoxicity, respectively. To our knowledge, the ligand-carrier pair, glycyrrhetinic acid-gelatin, was not explored before, and cancer therapy. the developed system poses a successful liver cancer therapy.