Quercetin delivery characteristics of chitosan nanoparticles prepared with different molecular weight polyanion cross-linkers

The aim of the study was to investigate the effects of cross-linkers on quercetin (QUE) absorption characteristics of QUE-loaded chitosan nanoparticles (CS-NPs). CS-NPs (461.2-482.7 nm) were prepared by ionic gelation at pH 3.5 using tripolyphosphate (367.9 Da), dextran sulfate (>15 kDa), arabic gum (AG, >250 kDa), or hyaluronic acid (HA, >1000 kDa). Mucoadhesion and cell permeation of QUE were significantly increased by positive charged CS-NPs due to interactions with negatively charged mucosal layer. Moreover, CS-AG and CS-HA NPs prepared with relatively higher MW cross-linkers exhibited significantly higher adhesion and permeation than the others. These results were verified by a cellular antioxidant activity assay; CS-AG (137.5 unit) and CS-HA NPs (126.5 unit) showed significantly higher activities after internalization into Caco-2 cells. Therefore, encapsulation within CS-NPs prepared using high MW cross-linkers such as AG and HA is found to be potentially valuable techniques for improving the QUE absorption.

Automated summary

The study revealed that chitosan nanoparticles prepared using high molecular weight cross-linkers such as arabic gum and hyaluronic acid significantly enhance the absorption of quercetin in cells. This technique has potential value in improving the absorption efficiency of quercetin.