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

• Published in: Carbohydrate polymers Vol. 252; p. 117091
• Main Authors: Hufnagel, Barbara, Muellner, Verena, Hlatky, Katharina, Tallian, Claudia, Vielnascher, Robert, Guebitz, Georg M., Wirth, Michael, Gabor, Franz
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 15.01.2021
• Subjects: 5-Aminosalicylic acid; Acetylated inulin; Anti-Inflammatory Agents - administration & dosage; Anti-Inflammatory Agents - chemistry; Drug Carriers - chemistry; Drug Liberation; Humans; Inflammatory bowel diseases; Inflammatory Bowel Diseases - drug therapy; Intestinal drug delivery; Inulin - chemistry; Mesalamine - administration & dosage; Mesalamine - chemistry; Pellets; Prebiotics; Inflammatory bowel diseases; 5-Aminosalicylic acid; Acetylated inulin; Intestinal drug delivery; Pellets; Prebiotics
• ISSN: 0144-8617; 1879-1344
• DOI: 10.1016/j.carbpol.2020.117091

•Acetylated inulin for intestinal drug delivery.•Characterization of the acetylated inulin regarding the lipophilicity (Log P).•Novel way of pellet production for innovative treatment strategies of IBDs.•Pellets: 5-aminosalicylic acid release up to 82 % within 24 h. 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.