Rhamnogalacturonan-I based microcapsules for targeted drug release

Anna J. Svagan, Anja Kusic, Cristian De Gobba, Flemming Hofmann Larsen, Philip Sassene, Qi Zhou, Marco Van De Weert, Anette Mullertz, Bodil Jørgensen, Peter Ulvskov

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18 Citations (Scopus)
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Abstract

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.

Original languageEnglish
Article numbere0168050
JournalP L o S One
Volume11
Issue number12
Number of pages13
ISSN1932-6203
DOIs
Publication statusPublished - 2016

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