Cubic microcontainers improve in situ colonic mucoadhesion and absorption of amoxicillin in rats

Juliane Fjelrad Christfort*, Antonio José Guillot, Ana Melero*, Lasse Højlund Eklund Thamdrup, Teresa M. Garrigues, Anja Boisen, Kinga Zor, Line Hagner Nielsen

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review

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Abstract

An increased interest in colonic drug delivery has led to a higher focus on the design of delivery devices targeting this part of the gastrointestinal tract. Microcontainers have previously facilitated an increase in oral bioavailability of drugs. The surface texture and shape of microcontainers have proven to influence the mucoadhesion ex vivo. In the present work, these findings were further investigated using an in situ closed-loop perfusion technique in the rat colon, which allowed for simultaneous evaluation of mucoadhesion of the microcontainers as well as drug absorption. Cylindrical, triangular and cubic microcontainers, with the same exterior surface area, were evaluated based on in vitro release, in situ mucoadhesion and in situ absorption of amoxicillin. Additionally, the mucoadhesion of empty cylindrical microcontainers with and without pillars on the top surface was investigated. From the microscopy analysis of the colon sections after the in situ study, it was evident that a significantly higher percentage of cubic microcontainers than cylindrical microcontainers adhered to the intestinal mucus. Furthermore, the absorption rate constants and blood samples indicated that amoxicillin in cubic microcontainers was absorbed more readily than when cylindrical or triangular microcontainers were dosed. This could be due to a higher degree of mucoadhesion for these particular microcontainers.
Original languageEnglish
Article number355
JournalPharmaceutics
Volume12
Issue number4
Number of pages16
ISSN1999-4923
DOIs
Publication statusPublished - 2020

Keywords

  • In situ perfusion
  • Microdevices
  • Shape
  • Mucoadhesion
  • Colon absorption

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