Enhancement of oral bioavailability of celastrol by chitosan microencapsulated porous starch carriers

Celastrol demonstrates significant potential in immunomodulatory applications; however, its low oral bioavailability presents a substantial obstacle to its clinical translation. Here, we combined porous starch with chitosan to develop an efficacious microencapsulation system aimed at enhancing the oral absorption of celastrol. Microcapsule carrier for celastrol was formulated Through the utilization of chitosan-coated porous starch particle technology and Subsequent evaluations of the morphology and release kinetics of microcapsules. The impact of microencapsulation on the enhanced absorption of celastrol was assessed through Caco-2 cell uptake experiments and in vivo pharmacokinetic studies. FT-IR analysis revealed the stable presence of celastrol in an amorphous state within the microcapsules, facilitated by hydrogen-bonding interactions between celastrol and porous starch. Simulated release experiments indicated that the chitosan coating improved the stability and extended the release of celastrol. Cell experiments, as well as in vivo distribution and pharmacokinetic investigations, demonstrated that the chitosan microencapsulation strategy significantly enhanced cellular uptake and in vivo absorption of celastrol, resulting in notably higher bioavailability compared to conventional formulations. This study successfully demonstrated the remarkable efficacy of chitosan microencapsulated porous starch carriers in enhancing the oral bioavailability of celastrol, revealing novel potential applications for these two food-grade materials in delivery systems.