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EGCG intestinal absorption and oral bioavailability enhancement using folic acid-functionalized nanostructured lipid carriers

This work aimed to develop folic acid-functionalized nanostructured lipid carriers (NLC) loading epigallocatechin-3-gallate (EGCG) to increase its oral bioavailability. An active targeting strategy was used and these nanoparticles (NPs) were fully characterized. The NP's effect on Caco-2 cell v...

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Autores principales: Granja, Andreia, Neves, Ana Rute, Sousa, Célia T., Pinheiro, Marina, Reis, Salette
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6611934/
https://www.ncbi.nlm.nih.gov/pubmed/31317081
http://dx.doi.org/10.1016/j.heliyon.2019.e02020
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author Granja, Andreia
Neves, Ana Rute
Sousa, Célia T.
Pinheiro, Marina
Reis, Salette
author_facet Granja, Andreia
Neves, Ana Rute
Sousa, Célia T.
Pinheiro, Marina
Reis, Salette
author_sort Granja, Andreia
collection PubMed
description This work aimed to develop folic acid-functionalized nanostructured lipid carriers (NLC) loading epigallocatechin-3-gallate (EGCG) to increase its oral bioavailability. An active targeting strategy was used and these nanoparticles (NPs) were fully characterized. The NP's effect on Caco-2 cell viability was evaluated and the apparent permeability (P(app)) on a Caco-2 cell monolayer was determined. The results demonstrated that the developed NPs exhibited adequate physicochemical characteristics for oral administration and were found to be biocompatible with epithelial Caco-2 cells. Further, folic acid-functionalized EGCG-loaded NLC significantly increased EGCG transport across the intestinal barrier, promoting a 1.8- fold increase in its apparent permeability (P(app)). Taken together, these results support that the developed NLC can be used as a promising carrier for safer and efficient management of several diseases since the pharmacokinetic (PK) properties of EGCG were improved with this nanomedicine-based strategy.
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spelling pubmed-66119342019-07-17 EGCG intestinal absorption and oral bioavailability enhancement using folic acid-functionalized nanostructured lipid carriers Granja, Andreia Neves, Ana Rute Sousa, Célia T. Pinheiro, Marina Reis, Salette Heliyon Article This work aimed to develop folic acid-functionalized nanostructured lipid carriers (NLC) loading epigallocatechin-3-gallate (EGCG) to increase its oral bioavailability. An active targeting strategy was used and these nanoparticles (NPs) were fully characterized. The NP's effect on Caco-2 cell viability was evaluated and the apparent permeability (P(app)) on a Caco-2 cell monolayer was determined. The results demonstrated that the developed NPs exhibited adequate physicochemical characteristics for oral administration and were found to be biocompatible with epithelial Caco-2 cells. Further, folic acid-functionalized EGCG-loaded NLC significantly increased EGCG transport across the intestinal barrier, promoting a 1.8- fold increase in its apparent permeability (P(app)). Taken together, these results support that the developed NLC can be used as a promising carrier for safer and efficient management of several diseases since the pharmacokinetic (PK) properties of EGCG were improved with this nanomedicine-based strategy. Elsevier 2019-07-03 /pmc/articles/PMC6611934/ /pubmed/31317081 http://dx.doi.org/10.1016/j.heliyon.2019.e02020 Text en © 2019 Published by Elsevier Ltd. http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Article
Granja, Andreia
Neves, Ana Rute
Sousa, Célia T.
Pinheiro, Marina
Reis, Salette
EGCG intestinal absorption and oral bioavailability enhancement using folic acid-functionalized nanostructured lipid carriers
title EGCG intestinal absorption and oral bioavailability enhancement using folic acid-functionalized nanostructured lipid carriers
title_full EGCG intestinal absorption and oral bioavailability enhancement using folic acid-functionalized nanostructured lipid carriers
title_fullStr EGCG intestinal absorption and oral bioavailability enhancement using folic acid-functionalized nanostructured lipid carriers
title_full_unstemmed EGCG intestinal absorption and oral bioavailability enhancement using folic acid-functionalized nanostructured lipid carriers
title_short EGCG intestinal absorption and oral bioavailability enhancement using folic acid-functionalized nanostructured lipid carriers
title_sort egcg intestinal absorption and oral bioavailability enhancement using folic acid-functionalized nanostructured lipid carriers
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6611934/
https://www.ncbi.nlm.nih.gov/pubmed/31317081
http://dx.doi.org/10.1016/j.heliyon.2019.e02020
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