Novel pH-sensitive gellan gum–ε-polylysine hydrogel microspheres for sulforaphene delivery

Abstract

BACKGROUND: This study aimed to improve the stability and utilization of sulforaphene (SFE) and to enhance the intestinal stability and pH-sensitive release of SFE in the gastrointestinal tract. To achieve this objective, calcium chloride (CaCl2) was used as a crosslinking agent to fabricate novel SFE-loaded gellan gum (GG)-ε-polylysine (ε-PL) pH-sensitive hydrogel microspheres by using the ionic crosslinking technique. RESULTS: The molecular docking results of GG, ε-PL, and SFE were good and occurred in the natural state. The loading efficiency (LE) of all samples was above 70%. According to the structural characterization results, GG and ε-PL successfully embedded SFE in a three-dimensional network structure through electrostatic interaction. The swelling characteristics and in vitro release results revealed that the microspheres were pH-sensitive, and SFE was mainly retained inside the hydrogel microsphere in the stomach, and subsequently released in the intestine. The result of cytotoxicity assay showed that the hydrogel microspheres were non-toxic and had an inhibitory effect on human colon cancer Caco-2 cells. CONCLUSION: Thus, the hydrogel microspheres could improve SFE stability and utilization and achieve the intestinal targeted delivery of SFE. © 2024 Society of Chemical Industry.