Amelioration of experimental colitis by a site-specific novel plant polysaccharide (Opuntia ficusindica) based macroparticles contains probiotic biomass and mesalazine

Abstract

The availability of therapeutic substances at colonic regions is always challenging for researchers. In this work, we aimed to evaluate the colon-targeting ability of mesalazine and probiotic biomass using Opuntia ficusindica polysaccharide. The present work will explore the application of novel plant polysaccharides as a rate-controlling polymer for colon drug delivery. Opuntia ficusindica polysaccharide was extracted and evaluated for the in-vitro toxicity study on HT-29 cell lines. Drug-loaded macroparticles were prepared and compressed into the tablet. In-vitro drug release was determined in simulated gastric fluid. Disease models were developed in Sprague Dawley rats to determine the efficacy of prepared formulation in the presence of probiotic biomass. Colon targeting efficiency of 99mTc-pertechnetate labeled mesalazine was monitored in human volunteers. Investigation of the polysaccharide's in-vitro toxicity revealed that the polysaccharide was safe for colon applications. Drug release data increased (p < 0.05) in the presence of rat cecal material at 6 h. The study also revealed that drug release from the different batches was directly proportional to polysaccharide concentration. In-vivo animal study confirms the better prevention of the disease in the presence of probiotic mass and drug. Gamma scintigraphy further supports the minimal drug release from the radiolabeled formulation in the upper gastrointestinal tract (GIT), despite the fact that it started drug release after 360 min, which was then disseminated during the subsequent 720–960 min in the colon. The study shows that Opuntia ficusindica polysaccharide can be used to deliver mesalazine to the colon.