Rhamnogalacturonan-I Based Microcapsules for Targeted Drug Release

• Published in: PloS one Vol. 11; no. 12; p. e0168050
• Main Authors: Svagan, Anna J, Kusic, Anja, De Gobba, Cristian, Larsen, Flemming H, Sassene, Philip, Zhou, Qi, van de Weert, Marco, Mullertz, Anette, Jørgensen, Bodil, Ulvskov, Peter
• Format: Journal Article
• Language: English
• Published: United States Public Library of Science 19.12.2016; Public Library of Science (PLoS)
• Subjects: Acids; Analysis; Animals; Biology and Life Sciences; Cancer; Capsules - chemical synthesis; Capsules - chemistry; Colon; Colon cancer; Computational fluid dynamics; Computer simulation; Crosslinking; Drug delivery; Drug Delivery Systems; Drug Liberation; Drug therapy; Environmental science; Enzymes; Fluorescence; Fluorescent indicators; Food science; Fourier transforms; Gastrointestinal diseases; Gastrointestinal Microbiome; Gastrointestinal Tract - microbiology; Health aspects; Health risks; Humans; Inflammatory bowel diseases; Intestine; Medical treatment; Medicine and Health Sciences; Microbiota (Symbiotic organisms); Microcapsules; Microflora; Oral administration; Particle Size; Pectins - pharmacokinetics; Pharmacy; Physical Sciences; Physiology; Polysaccharides; Research and analysis methods; Rhamnogalacturonan; Solanum tuberosum - chemistry; Spectrum analysis; Germany; Denmark; Sweden
• ISSN: 1932-6203; 1932-6203
• DOI: 10.1371/journal.pone.0168050

Drug targeting to the colon via the oral administration route for local treatment of e.g. inflammatory bowel disease and colonic cancer has several advantages such as needle-free administration and low infection risk. A new source for delivery is plant-polysaccharide based delivery platforms such as Rhamnogalacturonan-I (RG-I). In the gastro-intestinal tract the RG-I is only degraded by the action of the colonic microflora. For assessment of potential drug delivery properties, RG-I based microcapsules (~1 μm in diameter) were prepared by an interfacial poly-addition reaction. The cross-linked capsules were loaded with a fluorescent dye (model drug). The capsules showed negligible and very little in vitro release when subjected to media simulating gastric and intestinal fluids, respectively. However, upon exposure to a cocktail of commercial RG-I cleaving enzymes, ~ 9 times higher release was observed, demonstrating that the capsules can be opened by enzymatic degradation. The combined results suggest a potential platform for targeted drug delivery in the terminal gastro-intestinal tract.