Preparation of MSZ Hydrogel and Its Treatment of Colitis

Abstract

In order to control the release of mesalazine (MSZ) in the gastrointestinal tract to achieve better pharmacological effects in the colon, in this study, MSZ was added to hydroxypropyl-β-cyclodextrin (HP-β-CD) to form a water-soluble HP-β-CD/MSZ inclusion complex. Then, the inclusion compound was loaded into the structure of the bilayer polyelectrolyte complex microsphere formed by alginate (Alg), chitosan (Cs), and kappa carrageenan (κ-Car) as the hydrogel carrier, and the hydrogel beads with colon-specific release MSZ after oral administration were formed. The formed hydrogel beads have different swelling capabilities in different pH media and have the greatest swelling degree under pH 7.4. The encapsulation efficiency and drug loading of hydrogel beads can reach up to 83.23 and 18.31%, respectively, and the size of hydrogel beads can be reduced to less than 1 mm after drying, so that the size of oral administration can be reached. In vivo experiments also showed that the formed hydrogel beads had a better therapeutic effect on colitis than free drugs, and the microspheres were biodegradable, so the double-layer pH-sensitive microspheres could be effectively used in colon-targeting drug delivery.

Application of chitosan/alginate nanoparticle in oral drug delivery systems: prospects and challenges

“…5-ASA, also known as mesalamine, is the treatment of choice for mild to moderate cases of UC. In our previous study, 5-ASA was encapsulated in microspheres prepared by CANPs-based hydrogels (Wu et al., 2021 ). This hydrogel microsphere had different swelling abilities in different pH media, which had colon-targeting and strong retention ability in colitis mice, and the microsphere was biodegradable, achieving a therapeutic effect superior to free drugs.…”