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 IC 50 score of 19.26 μM 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 1 H 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 IC 50 of 10.95 and 5.046 μM, revealing two- and fourfold enhancements in allicin cytotoxicity, respectively. To our knowledge, the ligand–carrier pair, glycyrrhetinic acid–gelatin, was not explored before, and the developed system poses a successful liver cancer therapy.

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Objectives The aim of this work was to study the effect of the physically adsorbed Poloxamer 188 coating polymer on the cytotoxic activity of allicin-loaded gelatin nanoparticles. Methods The double desolvation method was utilised to prepare the nanoparticles which were characterised for particle size (PS), polydispersity index (PDI) and zeta potential and visualised using transmission electron microscopy. The coating density of the used polymer was determined using 1H-nuclear magnetic resonance (1H-NMR); 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay was used to evaluate the cytotoxicity on HepG-2 cell lines. Key findings The particles were spherical possessing a PS of 714 ± 25.21 nm and a PDI of 0.663 ± 0.143. These results together with the 1H-NMR results analysis confirmed the efficient coating of Poloxamer 188. The coating of particles rendered them more cytotoxic, scoring an IC50 of 6.736 µm (2-folds lower than the uncoated counter parts and 4-folds lesser than the allicin solution), and apt for cancer-targeting. Moreover, the prepared nanoparticles were stable to gamma-sterilisation and to a storage of 12 months. Conclusions Augmented cytotoxicity on HepG-2 cell lines was obtained using the physical adsorption of an abundant and relatively cheap material, Poloxamer 188, on allicin-loaded gelatin nanoparticles.