DEVELOPMENT OF XYLAN MICROPARTICLES CONTAINING MESALAMINE FOR COLON DRUG RELEASE
Mesalazine; Biopolymer; Hemicellulose; Drug delivery systems; DDsolver.
Xylan is an important biopolymer that can be extracted from several agro-wastes in the world and has been receiving a great attention in the production of colon drug delivery systems. This polymer has the ability to pass through the digestive tract unchanged and its complex structure requires enzymes that are produced specifically by the human colonic microflora, which makes it an interesting raw material in the production of targeted drug delivery systems. In this work, xylan extracted from corn cobs was used to produce mesalamine-loaded xylan microparticles (XMP5-ASA) by cross-linking polymerization using a non-hazardous cross-linking agent. The microparticles were characterized by thermal analysis (DSC/TG), X-ray diffraction (XRD), Infrared spectroscopy (FTIR-ATR) and scanning electron microscopy (SEM). A comparative study of the in vitro drug release from XMP5-ASA and from gastro-resistant capsules filled with XMP5-ASA (XMPCAP5-ASA) or 5-ASA was also performed. NMR, FTIR-ATR, XRD and DSC/TG studies indicated molecularly dispersed drug in the microparticles with increment on drug stability. The release studies showed that XMPCAP5-ASA allowed more efficient drug retention in the simulated gastric fluid and a prolonged drug release lasting up to 24 h. XMPCAP5-ASA retained approximately 48 % of its drug content after 6 h on the drug release assay. Thus, the encapsulation of 5-ASA into xylan microparticles together with gastro-resistant capsules allowed a better release control of the drug during different simulated gastrointestinal medium.