Development and mechanistic study of a microemulsion containing vitamin E TPGS for the enhancement of oral absorption of celecoxib

Development and mechanistic study of a microemulsion containing vitamin E TPGS for the enhancement of oral absorption of celecoxib

Thirapit SubongkotDepartment of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Burapha University, Chonburi, ThailandPurpose: The purpose of this study was to develop a microemulsion containing D-α-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS) as a biodegra...

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Autor principal: Subongkot T
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2019
Materias:
microemulsion
celecoxib
oral absorption enhancement mechanism
vitamin E TPGS
transepithelial electrical resistance
Medicine (General)
R5-920
Acceso en línea:https://doaj.org/article/583dc54650914c4ca2069d255523c7dc
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spelling oai:doaj.org-article:583dc54650914c4ca2069d255523c7dc2021-12-02T04:16:36ZDevelopment and mechanistic study of a microemulsion containing vitamin E TPGS for the enhancement of oral absorption of celecoxib1178-2013https://doaj.org/article/583dc54650914c4ca2069d255523c7dc2019-04-01T00:00:00Zhttps://www.dovepress.com/development-and-mechanistic-study-of-a-microemulsion-containing-vitami-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Thirapit SubongkotDepartment of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Burapha University, Chonburi, ThailandPurpose: The purpose of this study was to develop a microemulsion containing D-α-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS) as a biodegradable surfactant to increase the oral absorption of celecoxib.Methods: This study investigated the intestinal absorption enhancement mechanism of this microemulsion by measuring transepithelial electrical resistance (TEER) values. This study also evaluated microemulsion particle–intestine interactions in terms of release and attachment processes using confocal laser scanning microscopy (CLSM).Results: The prepared microemulsion particles had a size of <300 nm with a neutral surface charge. The celecoxib-loaded microemulsion release kinetic was classified as the zero-order model. This vitamin E TPGS-based microemulsion significantly increased the in vitro intestinal absorption of celecoxib compared to celecoxib solution. The CLSM study suggested that microemulsion particles with entrapped drugs might attach to the intestinal epithelium before releasing the entrapped drug into tissues. The TEER value of the intestinal tissues treated with the celecoxib-loaded microemulsion was significantly decreased compared to the value before treatment, indicating an increase in drug transport via the paracellular pathway. The evaluation of intestinal tissue cytotoxicity using lactate dehydrogenase cytotoxicity assay suggested that the prepared celecoxib-loaded microemulsion was safe for oral route administration. Conclusions: The prepared celecoxib loaded microemulsion could increase the intestinal absorption of celecoxib compared to celecoxib solution. The intestinal absorption enhancement mechanism of this microemulsion resulted from the increase of the drug transport via the paracellular pathway. Keywords: microemulsion, celecoxib, oral absorption enhancement mechanism, vitamin E TPGS, transepithelial electrical resistanceSubongkot TDove Medical Pressarticlemicroemulsioncelecoxiboral absorption enhancement mechanismvitamin E TPGStransepithelial electrical resistanceMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 3087-3102 (2019)
institution DOAJ
collection DOAJ
language EN
topic microemulsion
celecoxib
oral absorption enhancement mechanism
vitamin E TPGS
transepithelial electrical resistance
Medicine (General)
R5-920
spellingShingle microemulsion
celecoxib
oral absorption enhancement mechanism
vitamin E TPGS
transepithelial electrical resistance
Medicine (General)
R5-920
Subongkot T
Development and mechanistic study of a microemulsion containing vitamin E TPGS for the enhancement of oral absorption of celecoxib
description Thirapit SubongkotDepartment of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Burapha University, Chonburi, ThailandPurpose: The purpose of this study was to develop a microemulsion containing D-α-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS) as a biodegradable surfactant to increase the oral absorption of celecoxib.Methods: This study investigated the intestinal absorption enhancement mechanism of this microemulsion by measuring transepithelial electrical resistance (TEER) values. This study also evaluated microemulsion particle–intestine interactions in terms of release and attachment processes using confocal laser scanning microscopy (CLSM).Results: The prepared microemulsion particles had a size of <300 nm with a neutral surface charge. The celecoxib-loaded microemulsion release kinetic was classified as the zero-order model. This vitamin E TPGS-based microemulsion significantly increased the in vitro intestinal absorption of celecoxib compared to celecoxib solution. The CLSM study suggested that microemulsion particles with entrapped drugs might attach to the intestinal epithelium before releasing the entrapped drug into tissues. The TEER value of the intestinal tissues treated with the celecoxib-loaded microemulsion was significantly decreased compared to the value before treatment, indicating an increase in drug transport via the paracellular pathway. The evaluation of intestinal tissue cytotoxicity using lactate dehydrogenase cytotoxicity assay suggested that the prepared celecoxib-loaded microemulsion was safe for oral route administration. Conclusions: The prepared celecoxib loaded microemulsion could increase the intestinal absorption of celecoxib compared to celecoxib solution. The intestinal absorption enhancement mechanism of this microemulsion resulted from the increase of the drug transport via the paracellular pathway. Keywords: microemulsion, celecoxib, oral absorption enhancement mechanism, vitamin E TPGS, transepithelial electrical resistance
format article
author Subongkot T
author_facet Subongkot T
author_sort Subongkot T
title Development and mechanistic study of a microemulsion containing vitamin E TPGS for the enhancement of oral absorption of celecoxib
title_short Development and mechanistic study of a microemulsion containing vitamin E TPGS for the enhancement of oral absorption of celecoxib
title_full Development and mechanistic study of a microemulsion containing vitamin E TPGS for the enhancement of oral absorption of celecoxib
title_fullStr Development and mechanistic study of a microemulsion containing vitamin E TPGS for the enhancement of oral absorption of celecoxib
title_full_unstemmed Development and mechanistic study of a microemulsion containing vitamin E TPGS for the enhancement of oral absorption of celecoxib
title_sort development and mechanistic study of a microemulsion containing vitamin e tpgs for the enhancement of oral absorption of celecoxib
publisher Dove Medical Press
publishDate 2019
url https://doaj.org/article/583dc54650914c4ca2069d255523c7dc
work_keys_str_mv AT subongkott developmentandmechanisticstudyofamicroemulsioncontainingvitaminenbsptpgsfortheenhancementoforalabsorptionofnbspcelecoxib
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