Glycyrrhizic acid (GA) is one of the components of licorice roots (Glycyrrhiza glabra L.). GA is a triterpenoid saponin can be used as a medicinal plant with its antiallergic, antiviral, anti-inflammatory, anti-ulcer, hepatoprotective, anticancer, anti-oxidation activities and several other therapeutic properties. The aim of this study is to develop an anti-aging formulation for topical application containing GA. In this context, GA-loaded Poly (D,L-lactide-co-glycolide) (PLGA) nanoparticles (NPs) were prepared using the double emulsion method, and were characterized by various spectroscopic methods. The efficacy of GA-PLGA NPs was evaluated with in vitro and in silico methods. The encapsulation efficiency and loading capacity were calculated. The in vitro release study was conducted, and the GA release profile was determined. The genotoxic activity of GA and GA-PLGA NPs was evaluated by the Ames test using TA98 and TA100 mutant strains of Salmonella typhimurium. The cytotoxic potential of GA-PLGA NPs was evaluated on the HaCaT cell line using the MTT assay. According to the genotoxicity and cytotoxicity results, it was found that the GA-PLGA NP formulation did not exhibit genotoxic and cytotoxic effects. Moreover, the efficacy of GA in preventing UVB-induced photo-aging in HaCaT cells and the clarification of the molecular mechanism of GA binding to MMPs were revealed by molecular docking analysis. In addition, through molecular dynamics (MD) analysis, the binding interaction of GA with MMPs in a dynamic system, and protein-ligand stability were predicted as a result of 50 ns MD simulation studies considering various analysis parameters. Finally, it was evaluated that GA-PLGA nanoformulation might be used as an alternative anti-aging skin care product candidate via topical application.
Onopordum acanthium is a medicinal plant with many important properties, such as antibacterial, anticancer, and anti-hypotensive properties. Although various studies reported the biological activities of O. acanthium, there is no study on its nano-phyto-drug formulation. The aim of this study is to develop a candidate nano-drug based on phytotherapeutic constituents and evaluate its efficiency in vitro and in silico. In this context, poly (lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) of O. acanthium extract (OAE) were synthesized and characterized. It was determined that the average particle size of OAE-PLGA-NPs was 214.9 ± 6.77 nm, and the zeta potential was −8.03 ± 0.85 mV, and PdI value was 0.064 ± 0.013. The encapsulation efficiency of OAE-PLGA-NPs was calculated as 91%, and the loading capacity as 75.83%. The in vitro drug release study showed that OAE was released from the PLGA NPs with 99.39% over the 6 days. Furthermore, the mutagenic and cytotoxic activity of free OAE and OAE-PLGA-NPs were evaluated by the Ames test and MTT test, respectively. Although 0.75 and 0.37 mg/mL free OAE concentrations caused both frameshift mutation and base pair substitution (p < 0.05), the administered OAE–PLGA NP concentrations were not mutagenic. It was determined with the MTT analysis that the doses of 0.75 and 1.5 mg/mL of free OAE had a cytotoxic effect on the L929 fibroblast cell line (p < 0.05), and OAE-PLGA-NPs had no cytotoxic effect. Moreover, the interaction between the OAE and S. aureus was also investigated using the molecular docking analysis method. The molecular docking and molecular dynamics (MD) results were implemented to elucidate the S. aureus MurE inhibition potential of OAE. It was shown that quercetin in the OAE content interacted significantly with the substantial residues in the catalytic pocket of the S. aureus MurE enzyme, and quercetin performed four hydrogen bond interactions corresponding to a low binding energy of −6.77 kcal/mol with catalytic pocket binding residues, which are crucial for the inhibition mechanism of S. aureus MurE. Finally, the bacterial inhibition values of free OAE and OAE–PLGA NPs were determined against S. aureus using a microdilution method. The antibacterial results showed that the inhibition value of the OAE–PLGA NPs was 69%. In conclusion, from the in vitro and in silico results of the nano-sized OAE-PLGA NP formulation produced in this study, it was evaluated that the formulation may be recommended as a safe and effective nano-phyto-drug candidate against S. aureus.
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