Xylan from Pineapple Stem Waste: a Potential Biopolymer for Colonic Targeting of Anti-inflammatory Agent Mesalamine

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 5-ASA administration confirmed the successful local colon delivery of 5-ASA using xylan-5-ASA 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.

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Acknowledgments

The project was financially supported by Bandung Institute of Technology (ITB) through “Innovative Research Grant” scheme year 2017.

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Correspondence to Heni Rachmawati.

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All institutional and national guidelines for the care and use of laboratory animals were followed. School of Pharmacy, Bandung Institute of Technology, Indonesia. The approval number is 305/UN6.C.10/PN/2017 (15/3/2017).

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Anindya, A.L., Oktaviani, R.D., Praevina, B.R. et al. Xylan from Pineapple Stem Waste: a Potential Biopolymer for Colonic Targeting of Anti-inflammatory Agent Mesalamine. AAPS PharmSciTech 20, 112 (2019). https://doi.org/10.1208/s12249-018-1205-y

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KEY WORDS

  • xylan
  • 5-ASA
  • colon targeting
  • colonic drug delivery
  • ulcerative colitis