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In Vitro Performance and Chemical Stability of Lipid-Based Formulations Encapsulated in a Mesoporous Magnesium Carbonate Carrier

Lipid-based formulations can circumvent the low aqueous solubility of problematic drug compounds and increase their oral absorption. As these formulations are often physically unstable and costly to manufacture, solidification has been suggested as a way to minimize these issues. This study evaluate...

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Autores principales: Alvebratt, Caroline, Dening, Tahnee J., Åhlén, Michelle, Cheung, Ocean, Strømme, Maria, Gogoll, Adolf, Prestidge, Clive A., Bergström, Christel A.S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7284621/
https://www.ncbi.nlm.nih.gov/pubmed/32384752
http://dx.doi.org/10.3390/pharmaceutics12050426
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author Alvebratt, Caroline
Dening, Tahnee J.
Åhlén, Michelle
Cheung, Ocean
Strømme, Maria
Gogoll, Adolf
Prestidge, Clive A.
Bergström, Christel A.S.
author_facet Alvebratt, Caroline
Dening, Tahnee J.
Åhlén, Michelle
Cheung, Ocean
Strømme, Maria
Gogoll, Adolf
Prestidge, Clive A.
Bergström, Christel A.S.
author_sort Alvebratt, Caroline
collection PubMed
description Lipid-based formulations can circumvent the low aqueous solubility of problematic drug compounds and increase their oral absorption. As these formulations are often physically unstable and costly to manufacture, solidification has been suggested as a way to minimize these issues. This study evaluated the physicochemical stability and in vitro performance of lipid-loaded mesoporous magnesium carbonate (MMC) particles with an average pore size of 20 nm. A medium chain lipid was loaded onto the MMC carrier via physical adsorption. A modified in vitro lipolysis setup was then used to study lipid release and digestion with (1)H nuclear magnetic resonance spectroscopy. The lipid loading efficiency with different solidification techniques was also evaluated. The MMC, unlike more commonly used porous silicate carriers, dissolved during the lipolysis assay, providing a rapid release of encapsulated lipids into solution. The digestion of the dispersed lipid-loaded MMC therefore resembled that of a coarse dispersion of the lipid. The stability data demonstrated minor degradation of the lipid within the pores of the MMC particles, but storage for three months did not reveal extensive degradation. To conclude, lipids can be adsorbed onto MMC, creating a solid powder from which the lipid is readily released into the solution during in vitro digestion. The chemical stability of the formulation does however merit further attention.
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spelling pubmed-72846212020-06-19 In Vitro Performance and Chemical Stability of Lipid-Based Formulations Encapsulated in a Mesoporous Magnesium Carbonate Carrier Alvebratt, Caroline Dening, Tahnee J. Åhlén, Michelle Cheung, Ocean Strømme, Maria Gogoll, Adolf Prestidge, Clive A. Bergström, Christel A.S. Pharmaceutics Article Lipid-based formulations can circumvent the low aqueous solubility of problematic drug compounds and increase their oral absorption. As these formulations are often physically unstable and costly to manufacture, solidification has been suggested as a way to minimize these issues. This study evaluated the physicochemical stability and in vitro performance of lipid-loaded mesoporous magnesium carbonate (MMC) particles with an average pore size of 20 nm. A medium chain lipid was loaded onto the MMC carrier via physical adsorption. A modified in vitro lipolysis setup was then used to study lipid release and digestion with (1)H nuclear magnetic resonance spectroscopy. The lipid loading efficiency with different solidification techniques was also evaluated. The MMC, unlike more commonly used porous silicate carriers, dissolved during the lipolysis assay, providing a rapid release of encapsulated lipids into solution. The digestion of the dispersed lipid-loaded MMC therefore resembled that of a coarse dispersion of the lipid. The stability data demonstrated minor degradation of the lipid within the pores of the MMC particles, but storage for three months did not reveal extensive degradation. To conclude, lipids can be adsorbed onto MMC, creating a solid powder from which the lipid is readily released into the solution during in vitro digestion. The chemical stability of the formulation does however merit further attention. MDPI 2020-05-06 /pmc/articles/PMC7284621/ /pubmed/32384752 http://dx.doi.org/10.3390/pharmaceutics12050426 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
Alvebratt, Caroline
Dening, Tahnee J.
Åhlén, Michelle
Cheung, Ocean
Strømme, Maria
Gogoll, Adolf
Prestidge, Clive A.
Bergström, Christel A.S.
In Vitro Performance and Chemical Stability of Lipid-Based Formulations Encapsulated in a Mesoporous Magnesium Carbonate Carrier
title In Vitro Performance and Chemical Stability of Lipid-Based Formulations Encapsulated in a Mesoporous Magnesium Carbonate Carrier
title_full In Vitro Performance and Chemical Stability of Lipid-Based Formulations Encapsulated in a Mesoporous Magnesium Carbonate Carrier
title_fullStr In Vitro Performance and Chemical Stability of Lipid-Based Formulations Encapsulated in a Mesoporous Magnesium Carbonate Carrier
title_full_unstemmed In Vitro Performance and Chemical Stability of Lipid-Based Formulations Encapsulated in a Mesoporous Magnesium Carbonate Carrier
title_short In Vitro Performance and Chemical Stability of Lipid-Based Formulations Encapsulated in a Mesoporous Magnesium Carbonate Carrier
title_sort in vitro performance and chemical stability of lipid-based formulations encapsulated in a mesoporous magnesium carbonate carrier
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7284621/
https://www.ncbi.nlm.nih.gov/pubmed/32384752
http://dx.doi.org/10.3390/pharmaceutics12050426
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