Chemically modified inulin for intestinal drug delivery - A new dual bioactivity concept for inflammatory bowel disease treatment

Carbohydr Polym. 2021 Jan 15:252:117091. doi: 10.1016/j.carbpol.2020.117091. Epub 2020 Sep 22.

Abstract

This study investigates a novel preparation technique for pellets made from acetylated inulin and their characterization focusing on specific intestinal delivery of 5-aminosalicylic acid. By means of acetylation the hydrophobicity of four native inulins was increased yielding materials with selected degrees of acetylation. The acetylated inulins were insoluble in water, which was confirmed by the log P-values ranging from 1.30 to 1.58. 5-Aminosalicylic acid loading capacity of the pellets was up to 60 % and high enough to match the therapeutic range of the anti-inflammatory drug. Depending on the 5-aminosalicylic acid content and the type of acetylated inulin, up to 80 % of the entrapped drug was released within 24 h in intestinal environment under in-vitro conditions. Here we successfully prepared chemically modified and profoundly characterized inulin to provide innovative formulations and to open up a promising new strategy for treatment of Morbus Crohn and ulcerative colitis.

Keywords: 5-Aminosalicylic acid; Acetylated inulin; Inflammatory bowel diseases; Intestinal drug delivery; Pellets; Prebiotics.

MeSH terms

  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / chemistry*
  • Drug Carriers / chemistry*
  • Drug Liberation
  • Humans
  • Inflammatory Bowel Diseases / drug therapy
  • Inulin / chemistry*
  • Mesalamine / administration & dosage
  • Mesalamine / chemistry*

Substances

  • Anti-Inflammatory Agents
  • Drug Carriers
  • Mesalamine
  • Inulin