Xylan from Pineapple Stem Waste: a Potential Biopolymer for Colonic Targeting of Anti-inflammatory Agent Mesalamine
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Research Article Xylan from Pineapple Stem Waste: a Potential Biopolymer for Colonic Targeting of Anti-inflammatory Agent Mesalamine Atsarina Larasati Anindya,1 Risa Dwi Oktaviani,2 Benita Rachel Praevina,2 Sophi Damayanti,2 Neng Fisheri Kurniati,2 Catur Riani,2 and Heni Rachmawati2,3
Received 30 May 2018; accepted 3 October 2018 Abstract.
We have successfully conjugated mesalamine (5-aminosalicylic acid, 5-ASA) with xylan, a biopolymer isolated from pineapple stem waste, to form xylan-5-ASA conjugate. The biopolymer was used to provide colon-targeting properties for 5-ASA, a golden standard anti-inflammatory agent commonly used for ulcerative colitis treatment. A series of data from FTIR spectroscopy, UV-Vis spectrophotometry, and HPLC confirmed the xylan-5-ASA conjugate formation. To ensure successful colon targeting properties, in vitro and in vivo drug release studies after oral administration of xylan-5-ASA conjugate to Wistar rats were performed. Xylan-5-ASA conjugate was able to retain 5-ASA release in the upper gastrointestinal tract fluid simulation but rapidly released 5-ASA in the rat colon fluid simulation. In vivo release profile shows a very low peak plasma concentration, reached at 6 h after xylan-5-ASA conjugate administration. The delayed release and the lower bioavailability of 5-ASA from xylan-5-ASA conjugate administration compared to free 5ASA administration confirmed the successful local colon delivery of 5-ASA using xylan-5ASA conjugate. The administration of xylan-5-ASA conjugate also exhibited greater efficacy in recovering 2,4,6-trinitrobenzene sulfonic acid-induced colon ulcer compared to free 5-ASA administration. Taken together, xylan isolated from pineapple stem waste is promising to obtain colon targeting property for 5-ASA.
KEY WORDS: xylan; 5-ASA; colon targeting; colonic drug delivery; ulcerative colitis.
INTRODUCTION Pineapple stem waste is often either discarded as a bio-waste or burnt into a low-value material causing environmental concern, in spite of containing important constituents such as holocellulose and hemicellulose, both of which are the main components of plant cell walls (1). Xylan is the most abundant hemicellulose found in plant cell walls and some algae. The molecule has a linear backbone structure consisting of 1,4-β-D-xylopyranose, and depending on its origin, may contain branches of L-arabinofuranosyl, acetyl, D-glucuronosyl and/or 4-O-methylglucuronosyl residue (1,2). Apart from xylan, the pineapple stem also contains bromelain, a protease enzyme which is often extracted and leaving
Electronic supplementary material The online version of this article (https://doi.org/10.1208/s12249-018-1205-y) contains supplementary material, which is available to authorized users. 1
Research Center for Nanosciences and Nanotechnology, Bandung Institute of Technology, Ganesha 10, Bandung, 40132, Indonesia. 2 School of Pharmacy, Research Center for Nanosciences and Nanotechnology, Bandung Institute of Technology, Ganesha 10, Bandung, 40132, Indonesia. 3 To whom correspondence sho
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