Development of Polysaccharide based Colon Targeted Drug Delivery System: Design and Evaluation of Assam Bora rice Starch based Matrix Tablet

Mohammad      Zaki Ahmad; Sohail      Akhter; Iqbal      Ahmad; Mahfoozur      Rahman; Mohammad      Anwar; Gourav      K. Jain; Farhan      J. Ahmad; Roop      Krishen Khar

doi:10.2174/156720111796642327

Abstract

The aim of this study was to develop a novel colon targeted matrix tablet containing Metronidazole (MTZ) as model drug. Matrix tablets were prepared using Assam Bora rice starch, which is essentially a natural polymer, by wet granulation technique. The granules prepared were subjected to evaluation for angle of repose, bulk density, compressibility index, Hausners ratio, total porosity, and drug content. The developed tablets were also analysed for thickness, diameter, weight variation tests, tablet crushing strength, friability, and in vitro release studies. The granules displayed satisfactory flow properties, compressibility, Hausnerapos;s ratio and drug content. Almost all the tablet formulations showed acceptable pharmacotechnical properties and complied with the in-house developed specifications for the tested parameters. Drug release study confirmed to the initial fast release in the acidic environment of surface adhered drug followed by slow release in alkaline media subsequently leading to fast and major drug release in the caecal content. Furthermore, the release of drug was unaffected by the hostile environment of GIT which can be ascribed to microbial degradation, promptly followed by enzymatic degradation. Curve fitting proved that the drug release from the tablets followed the Higuchi model. In vitro bacterial inhibition studies illustrated that the released drugs were able to diffuse through agar medium, inhibiting MTZ sensitive Bacteroides fragilis. The selected MTZ matrix tablets (F1-F6) had zones of inhibition paralleling those of the marketed formulation.

Keywords: Colon targeted drug delivery, Assam Bora rice starch, polysaccharide, matrix tablet, 5-fluorouracil, Colon specific drug delivery, HPMC, eudragit L 100, colon targeting, colon, direct compression coating, time-dependent drug delivery, pH responsive polymer, oral drug delivery and compression-coated tablets, metronidazole