Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation

The objective of our investigation was to design a self-microemulsifying drug-delivery system (SMEDDS) to improve the bioavailability of probucol. SMEDDS was composed of probucol, olive oil, Lauroglycol FCC, Cremophor EL, Tween-80, and PEG-400. Droplet sizes were determined. In vitro release was inv...

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Detalles Bibliográficos
Autores principales: Sha, Xianyi, Wu, Juan, Chen, Yanzuo, Fang, Xiaoling
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2012
Materias:
Original Research
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3282610/
https://www.ncbi.nlm.nih.gov/pubmed/22359449
http://dx.doi.org/10.2147/IJN.S28052
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author Sha, Xianyi
Wu, Juan
Chen, Yanzuo
Fang, Xiaoling
author_facet Sha, Xianyi
Wu, Juan
Chen, Yanzuo
Fang, Xiaoling
author_sort Sha, Xianyi
collection PubMed
description The objective of our investigation was to design a self-microemulsifying drug-delivery system (SMEDDS) to improve the bioavailability of probucol. SMEDDS was composed of probucol, olive oil, Lauroglycol FCC, Cremophor EL, Tween-80, and PEG-400. Droplet sizes were determined. In vitro release was investigated. Pharmacokinetics and bioavailability of probucol suspension, oil solution, and SMEDDS were evaluated and compared in rats. Plasma drug concentration was determined by high-performance liquid chromatography. After administration of probucol suspension, plasma drug concentration was very low. Relative bioavailability of SMEDDS was dramatically enhanced in an average of 2.15- and 10.22-fold that of oil solution and suspension, respectively. It was concluded that bioavailability of probucol was enhanced greatly by SMEDDS. Improved solubility and lymphatic transport may contribute to the enhancement of bioavailability.
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spelling pubmed-32826102012-02-22 Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation Sha, Xianyi Wu, Juan Chen, Yanzuo Fang, Xiaoling Int J Nanomedicine Original Research The objective of our investigation was to design a self-microemulsifying drug-delivery system (SMEDDS) to improve the bioavailability of probucol. SMEDDS was composed of probucol, olive oil, Lauroglycol FCC, Cremophor EL, Tween-80, and PEG-400. Droplet sizes were determined. In vitro release was investigated. Pharmacokinetics and bioavailability of probucol suspension, oil solution, and SMEDDS were evaluated and compared in rats. Plasma drug concentration was determined by high-performance liquid chromatography. After administration of probucol suspension, plasma drug concentration was very low. Relative bioavailability of SMEDDS was dramatically enhanced in an average of 2.15- and 10.22-fold that of oil solution and suspension, respectively. It was concluded that bioavailability of probucol was enhanced greatly by SMEDDS. Improved solubility and lymphatic transport may contribute to the enhancement of bioavailability. Dove Medical Press 2012 2012-02-10 /pmc/articles/PMC3282610/ /pubmed/22359449 http://dx.doi.org/10.2147/IJN.S28052 Text en © 2012 Sha et al, publisher and licensee Dove Medical Press Ltd. This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited.
spellingShingle Original Research
Sha, Xianyi
Wu, Juan
Chen, Yanzuo
Fang, Xiaoling
Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
title Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
title_full Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
title_fullStr Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
title_full_unstemmed Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
title_short Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
title_sort self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3282610/
https://www.ncbi.nlm.nih.gov/pubmed/22359449
http://dx.doi.org/10.2147/IJN.S28052
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