Fabrication, Characterization and in vitro Evaluation of Prednisolone Sustained Release Multiparticulate System for Colonic Targeting

Abstract

Background: Prednisolone (PRD) is orally prescribed for inflammatory bowel syndrome (IBS) as the upper GIT is the main site of absorption; therefore, long-term PRD dosing decreases therapeutic effectiveness through systemic side effects. Objective: This work focused on formulating sustained-release alginate beads as a multiparticulate system for colon targeting using prednisolone (PRD) to be filled in an HPMC capsule. Methods: PRD beads were prepared by the ionotropic gelation technique using sodium alginate as the primary polymer and inulin, guar gum, and pectin as secondary polymers. In addition to the impact of polymer type and quantity, other factors were investigated: The CaCl2 concentration and tween 80 addition Thirteen formulations were successfully prepared, and their properties, such as bead size, morphology, percentage of encapsulation efficiency, yield, DL, in vitro release study in GIT buffer media, IBS media, SEM, and FTIR, were assessed. Results: The study showed that the beads were close in size, and the size was not an obstacle for loading the beads in HPMC capsules. Further, yield%, EE%, and DL% increased according to the bead’s content increase. Conclusions: The optimum formula was F3 that coated HPMC capsules with Eudragit S-100, which gave sustained release profiles in GIT and IBS simulating media, and F13 that could last the release in different pH media, pH 1.2, 6.8, and 7.4.