title: Rhamnogalacturonan-I Based Microcapsules for Targeted Drug Release.
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.
authors.affiliation: Department of Pharmacy, University of Copenhagen, Copenhagen, Denmark.
authors.forename: Anna J
authors.identifier: http://orcid.org/0000-0002-4583-723X
authors.initials: AJ
authors.lastname: Svagan
authors.affiliation: Department of Pharmacy, University of Copenhagen, Copenhagen, Denmark.
authors.forename: Anja
authors.initials: A
authors.lastname: Kusic
authors.affiliation: Department of Food Science, University of Copenhagen, Copenhagen, Denmark.
authors.forename: Cristian
authors.initials: C
authors.lastname: De Gobba
authors.affiliation: Department of Food Science, University of Copenhagen, Copenhagen, Denmark.
authors.forename: Flemming H
authors.initials: FH
authors.lastname: Larsen
authors.affiliation: Department of Pharmacy, University of Copenhagen, Copenhagen, Denmark.
authors.forename: Philip
authors.initials: P
authors.lastname: Sassene
authors.affiliation: School of Biotechnology, Royal Institute of Technology (KTH), Stockholm, Sweden.
authors.forename: Qi
authors.initials: Q
authors.lastname: Zhou
authors.affiliation: Department of Pharmacy, University of Copenhagen, Copenhagen, Denmark.
authors.forename: Marco
authors.initials: M
authors.lastname: van de Weert
authors.affiliation: Department of Pharmacy, University of Copenhagen, Copenhagen, Denmark.
authors.forename: Anette
authors.initials: A
authors.lastname: Mullertz
authors.affiliation: Department of Plant and Environmental Sciences, University of Copenhagen, Copenhagen, Denmark.
authors.forename: Bodil
authors.initials: B
authors.lastname: Jørgensen
authors.affiliation: Department of Plant and Environmental Sciences, University of Copenhagen, Copenhagen, Denmark.
authors.forename: Peter
authors.initials: P
authors.lastname: Ulvskov
mesh_terms: D000818:Animals; D002214:Capsules / Q000138:chemical synthesis* / Q000737:chemistry; D016503:Drug Delivery Systems; D065546:Drug Liberation; D000069196:Gastrointestinal Microbiome; D041981:Gastrointestinal Tract / Q000382:microbiology; D006801:Humans; D010316:Particle Size; D010368:Pectins / Q000493:pharmacokinetics*; D011198:Solanum tuberosum / Q000737:chemistry
chemical_list: D002214:Capsules; C042491:rhamnogalacturonan I; D010368:Pectins