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

Abstract

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.

Chloroquine and hydroxychloroquine for combating COVID-19: Investigating efficacy and hypothesizing new formulations using Bio/chemoinformatics tools

“…After performing an un-paired t-test using GraphPad Prism® v.5.0, the slightly significant ( P < 0.05) lower score of the binding energy (more negative values of ΔG) indicated better interaction of HCQ on the gelatin matrix. This could be attributed to its more hydrophilic nature demonstrated by its higher total polar surface area and more H-bond donors and acceptors that can interact with the gelatin carboxylic and amino groups [ 22 , 38 ] compared to the CQ counterparts. This higher interaction may result in a higher loading potential and more sustained release effect of HCQ, specifically, from the gelatin matrix.…”

Comparing cefotaxime and ceftriaxone in combating meningitis through nose-to-brain delivery using bio/chemoinformatics tools

“…Table 1 demonstrates the results of docking the investigated drugs; cefotaxime and ceftriaxone on the selected carriers. The higher score of ceftriaxone on the gelatin matrix could be attributed to its more hydrophilic nature demonstrated by its lower Log P (− 1.59), higher total polar surface area (506.48) and higher number of h-bond donors and acceptors (5 and 9, respectively) that can interact with the gelatin carboxylic and amino groups 38 , 39 compared to the cefotaxime counterparts. Table 2 depicts the SMILES (that were needed for docking experiments, electronic, constitutional and topological physico-chemical descriptors) of the two studied antibiotics.…”

Natural Biocidal Compounds of Plant Origin as Biodegradable Materials Modifiers

“…The presence of allicin elongates the release of the nutrients in the soil which is desired in perennial plants cultivation [ 331 ]. Gelatin nanoparticles loaded with allicin could be used in cancer therapy due to the anticancer activity of allicin [ 332 ]. The strong antibacterial activity of biocomposites [chitosan/polyvinyl alcohol (PVA)] doped with allicin has been noticed.…”