Improvement of antithrombotic activity of red ginseng extract by nanoencapsulation using chitosan and antithrombotic cross-linkers: polyglutamic acid and fucoidan

Abstract

Background Red ginseng (RG) extract, especially ginsenoside Rg1 and Rb1 fractions has been reported to have antithrombotic activities. However, gastric instability and low intestinal permeability are considered to be obstacles to its oral administration. We hypothesized that stability, permeability, and activities of RG might be improved by encapsulation within nanoparticles (NPs) prepared with antithrombotic coating materials. Methods RG-loaded chitosan (CS) NPs (PF-NPs) were prepared by complex ionic gelation with the antithrombotic wall materials, polyglutamic acid (PGA), and fucoidan (Fu). The concentrations of PGA (mg/mL, X 1 ) and Fu (mg/mL, X 2 ) were optimized for the smallest particle size by response surface methodology. Antithrombotic activities of RG and PF-NPs were analyzed using ex vivo and in vivo antiplatelet activities, in vivo carrageenan-induced mouse tail, and arteriovenous shunt rat thrombosis models. Results In accordance with a quadratic regression model, the smallest PF-NPs (286 ± 36.6 nm) were fabricated at 0.628 mg/mL PGA and 0.081 mg/mL Fu. The inhibitory activities of RG on ex vivo and in vivo platelet aggregation and thrombosis in in vivo arteriovenous shunt significantly ( p < 0.05) increased to approximately 66.82%, 35.42%, and 38.95%, respectively, by encapsulation within PF-NPs. For an in vivo carrageenan-induced mouse tail thrombosis model, though RG had a weaker inhibitory effect, PF-NPs reduced thrombus significantly due to the presence of PGA and Fu. Conclusion PF-NPs contributed to improve the activities of RG not only by nanoencapsulation but also by antithrombotic coating materials. Therefore, PG-NPs can be suggested as an efficient delivery system for oral administration of RG.

Gegen Qinlian pills alleviate carrageenan-induced thrombosis in mice model by regulating the HMGB1/NF-κB/NLRP3 signaling

“…Carrageenan is a linear sulfur-containing macromolecular polysaccharide, that is widely used in the model of thrombosis. It can cause inflammation in local blood vessels, lead to the secretion of inflammatory factors, damage vascular endothelial cells, and cause thrombosis ( Kim et al., 2021 ). Therefore, in this study, we used the carrageenan-induced thrombus model to evaluate the effect of GQP on inflammation-induced thrombus.…”

Indole-3-carbinol ameliorated the isoproterenol-induced myocardial infarction via multimodal mechanisms in Wistar rats

“…The initial absorbance was measured at 570 nm on a microplate reader (BioTek, USA). Then, platelet aggregation was induced by adding 10 μM ADP and 5μg/ ml of collagen (Kim et al 2020, Shin et al 2020 then continuously incubated at 37 °C for 5 min with shaking. The change in absorbance values was recorded at 570 nm (n=6).…”

Antithrombotic effects of Protaetia brevitarsis seulensis larvae in a rat tail thrombosis model using κ‐carrageenan

“…Remarkably, 900 mg/kg of P. brevitarsis larvae effectively alleviated the histological changes induced by κ ‐carrageenan, and this effect was comparable with that of heparin. Heparin, a sulfated glycosaminoglycan, is extensive employed as an anticoagulant for thrombosis prevention owing to its notable antithrombotic properties (Kim et al 2021). However, its administration requires a parenteral route because of the limited absorption and low bioavailability in the gastrointestinal tract (Chen et al 2009).…”