Abstract
The release of mesalazine, an anti-inflammatory drug for Crohn’s disease, should be deferred while delivering along the gastrointestinal tract to maximize drug absorption in the colon. To that end, we intercalated mesalazine into a clay mineral, montmorillonite (MMT), and we encapsulated the resulting composite inside a pHsensitive polymer, an alginate hydrogel bead. Once intercalated between the microscopic MMT layers, the mesalazine is prevented from dissolution during encapsulation into the alginate beads. As the resulting mesalazine-clay-alginate (MCA) bead is covered with a protective alginate layer, the mesalazine does not dissolve in acidic gastric conditions. In in vitro release tests, the MCA beads exhibited less than 5% mesalazine release in gastric solution, while ~20% was released over 7 h in the intestinal condition. Our results demonstrate that the MCA bead is a highly effective, biocompatible means of mesalazine delivery to the colon.
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This work was supported by the Basic Research Project of the Korea Institute of Geoscience and Mineral Resources (KIGAM) funded by the Ministry of Science, ICT and Future Planning of Korea.
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Hong, HJ., Kim, J., Suh, Y.J. et al. pH-sensitive mesalazine carrier for colon-targeted drug delivery: A two-fold composition of mesalazine with a clay and alginate. Macromol. Res. 25, 1145–1152 (2017). https://doi.org/10.1007/s13233-017-5150-5
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DOI: https://doi.org/10.1007/s13233-017-5150-5