Novel gum acacia based macroparticles for colon delivery of Mesalazine: Development and gammascintigraphy study

摘要

Ulcerative colitis (UC) is an inflammatory bowel disease characterized by abdominal pain and the presence of blood in faeces. Mesalazine (MLZ) is a drug of choice that exerts topical anti-inflammatory response to inflamed mucosa. Conventional oral tablet of MLZ has certain limitations including drug loss and associated side effects. The colonic bacteria degradable polysaccharide based tablet would be an alternative with assurance of safe and effective treatment. This paper addresses the application of gum acacia (GA), for colon delivery of MLZ. The invitro cellular study confirms the safety of GA in HT-29 cells. Tablets prepared by compression of GA based macroparticles possess optimum values. The release profile of MLZ showed decrease in drug release by increasing concentration of GA. Results of in-vivo gamma scintigraphy study on human volunteers were in accordance with the in-vitro drug release study. Initially, no traces of the drug were found in stomach and tablet transit time through small intestine was observed 495 +/- 30 min. Colonic tablet reached at an ileocecal junction in 545 +/- 60 min and released the entire drug in colon fill 760 +/- 60 min course of study. The present study confirmed that GA based enteric coated tablet may be a promising carrier for colon-specific delivery of MLZ.