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Cubic Microcontainers Improve In Situ Colonic Mucoadhesion and Absorption of Amoxicillin in Rats

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 hav...

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Autores principales: Christfort, Juliane Fjelrad, Guillot, Antonio José, Melero, Ana, Thamdrup, Lasse Højlund Eklund, Garrigues, Teresa M., Boisen, Anja, Zór, Kinga, Nielsen, Line Hagner
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7238233/
https://www.ncbi.nlm.nih.gov/pubmed/32295139
http://dx.doi.org/10.3390/pharmaceutics12040355
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author Christfort, Juliane Fjelrad
Guillot, Antonio José
Melero, Ana
Thamdrup, Lasse Højlund Eklund
Garrigues, Teresa M.
Boisen, Anja
Zór, Kinga
Nielsen, Line Hagner
author_facet Christfort, Juliane Fjelrad
Guillot, Antonio José
Melero, Ana
Thamdrup, Lasse Højlund Eklund
Garrigues, Teresa M.
Boisen, Anja
Zór, Kinga
Nielsen, Line Hagner
author_sort Christfort, Juliane Fjelrad
collection PubMed
description 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.
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spelling pubmed-72382332020-06-02 Cubic Microcontainers Improve In Situ Colonic Mucoadhesion and Absorption of Amoxicillin in Rats Christfort, Juliane Fjelrad Guillot, Antonio José Melero, Ana Thamdrup, Lasse Højlund Eklund Garrigues, Teresa M. Boisen, Anja Zór, Kinga Nielsen, Line Hagner Pharmaceutics Article 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. MDPI 2020-04-14 /pmc/articles/PMC7238233/ /pubmed/32295139 http://dx.doi.org/10.3390/pharmaceutics12040355 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Christfort, Juliane Fjelrad
Guillot, Antonio José
Melero, Ana
Thamdrup, Lasse Højlund Eklund
Garrigues, Teresa M.
Boisen, Anja
Zór, Kinga
Nielsen, Line Hagner
Cubic Microcontainers Improve In Situ Colonic Mucoadhesion and Absorption of Amoxicillin in Rats
title Cubic Microcontainers Improve In Situ Colonic Mucoadhesion and Absorption of Amoxicillin in Rats
title_full Cubic Microcontainers Improve In Situ Colonic Mucoadhesion and Absorption of Amoxicillin in Rats
title_fullStr Cubic Microcontainers Improve In Situ Colonic Mucoadhesion and Absorption of Amoxicillin in Rats
title_full_unstemmed Cubic Microcontainers Improve In Situ Colonic Mucoadhesion and Absorption of Amoxicillin in Rats
title_short Cubic Microcontainers Improve In Situ Colonic Mucoadhesion and Absorption of Amoxicillin in Rats
title_sort cubic microcontainers improve in situ colonic mucoadhesion and absorption of amoxicillin in rats
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7238233/
https://www.ncbi.nlm.nih.gov/pubmed/32295139
http://dx.doi.org/10.3390/pharmaceutics12040355
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