Efficacy of resveratrol encapsulated microsponges delivered by pectin based matrix tablets in rats with acetic acid-induced ulcerative colitis

Abstract

<b>Objectives:</b> The objective of the present work to encapsulate the resveratrol (RES) inside the chitosan-based microsponges, employing the systematic optimization by 3³ Box-Behnken design for the colonic targeting.<b>Significance:</b> Enhanced therapeutic efficacy of RES-loaded microsponges and matrix tablets, <i>vis-a-vis</i> pureRES for ulcerative colitis.<b>Methods:</b> RES-loaded microsponges were prepared employing the systematic optimization by 3³ Box-Behnken design for the colonic targeting. The best-optimizedRES-loaded microsponge was compressed in the form of a tablet, employing pectin as a matrix-forming material. The encapsulation of RES inside microsponge was confirmed by XRD, DSC and FT-IR. Further, both RES-loaded microsponges and matrix tablets were evaluated for <i>in vitro</i> release kinetics and further evaluated for <i>in vivo</i> ulcerative colitis animal model.<b>Results:</b> Optimization experiments was obtained as the high value of <i>r</i>² (particle size = 0.9999; %EE = 0.9652; %CDR = 0.9469) inferred excellent goodness of fit. SEM revealed nearly spherical and porous nature of RES-loaded microsponges. The <i>in vitro</i> release kinetic showed zero-order release for RES-loaded microsponges and Korsmeyer-Peppas model for matrix tablets. The pharmacodynamic studies, in ulcerative colitis rat model, indicated better therapeutic efficacy of drug-loaded microsponges and matrix tablets, <i>vis-a-vis</i> pure RES. Thus, the present study advocates the potential of RES based microsponges delivered by pectin based matrix tablet, in the treatment of various colonic disorders.<b>Conclusion:</b> The present study proved that RES-loaded microsponges and matrix tablets based on chitosan and pectin can be the ideal delivery system for colonic delivery of RES.