Improved oral bioavailability of poorly water-soluble glimepiride by utilizing microemulsion technique

Haiying Li,1 Tingting Pan,1 Ying Cui,1 Xiaxia Li,1 Jiefang Gao,1 Wenzhi Yang,1 Shigang Shen2 1Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmacy, 2Key Laboratory of Analytical Science and Technology of Hebei Province, College of Chemistry and Environmental Scien...

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Autores principales:	Li HY, Pan TT, Cui Y, Li XX, Gao JF, Yang WZ, Shen SG
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	glimepiride microemulsion solubility pharmacodynamics pharmacokinetics Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/0f3ad52f0f954789819e76f627c57d57
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spelling	oai:doaj.org-article:0f3ad52f0f954789819e76f627c57d572021-12-02T05:36:19ZImproved oral bioavailability of poorly water-soluble glimepiride by utilizing microemulsion technique1178-2013https://doaj.org/article/0f3ad52f0f954789819e76f627c57d572016-08-01T00:00:00Zhttps://www.dovepress.com/improved-oral-bioavailability-of-poorly-water-soluble-glimepiride-by-u-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Haiying Li,1 Tingting Pan,1 Ying Cui,1 Xiaxia Li,1 Jiefang Gao,1 Wenzhi Yang,1 Shigang Shen2 1Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmacy, 2Key Laboratory of Analytical Science and Technology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding, People’s Republic of China Abstract: The objective of this work was to prepare an oil/water glimepiride (GM) microemulsion (ME) for oral administration to improve its solubility and enhance its bioavailability. Based on a solubility study, pseudoternary phase diagrams, and Box–Behnken design, the oil/water GMME formulation was optimized and prepared. GMME was characterized by dynamic laser light scattering, zeta potential, transmission electron microscopy, and viscosity. The in vitro drug release, storage stability, pharmacodynamics, and pharmacokinetics of GMME were investigated. The optimized GMME was composed of Capryol 90 (oil), Cremophor RH40 (surfactant), and Transcutol (cosurfactant), and increased GM solubility up to 544.6±4.91 µg/mL. The GMME was spherical in shape. The particle size and its polydispersity index were 38.9±17.46 nm and 0.266±0.057, respectively. Meanwhile, the GMME was physicochemically stable at 4°C for at least 3 months. The short-term efficacy in diabetic mice provided the proof that blood glucose had a consistent and significant reduction at a dose of 375 µg/kg whether via IP injection or IG administration of GMME. Compared with the glimepiride suspensions or glimepiride-meglumine complex solution, the pharmacokinetics of GMME in Wistar rats via IG administration exhibited higher plasma drug concentration, larger area under the curve, and more enhanced oral bioavailability. There was a good correlation of GMME between the in vitro release values and the in vivo oral absorption. ME could be an effective oral drug delivery system to improve bioavailability of GM. Keywords: glimepiride, microemulsion, solubility, pharmacodynamics, pharmacokineticsLi HYPan TTCui YLi XXGao JFYang WZShen SGDove Medical PressarticleglimepiridemicroemulsionsolubilitypharmacodynamicspharmacokineticsMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss default, Pp 3777-3788 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	glimepiride microemulsion solubility pharmacodynamics pharmacokinetics Medicine (General) R5-920
spellingShingle	glimepiride microemulsion solubility pharmacodynamics pharmacokinetics Medicine (General) R5-920 Li HY Pan TT Cui Y Li XX Gao JF Yang WZ Shen SG Improved oral bioavailability of poorly water-soluble glimepiride by utilizing microemulsion technique
description	Haiying Li,1 Tingting Pan,1 Ying Cui,1 Xiaxia Li,1 Jiefang Gao,1 Wenzhi Yang,1 Shigang Shen2 1Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmacy, 2Key Laboratory of Analytical Science and Technology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding, People’s Republic of China Abstract: The objective of this work was to prepare an oil/water glimepiride (GM) microemulsion (ME) for oral administration to improve its solubility and enhance its bioavailability. Based on a solubility study, pseudoternary phase diagrams, and Box–Behnken design, the oil/water GMME formulation was optimized and prepared. GMME was characterized by dynamic laser light scattering, zeta potential, transmission electron microscopy, and viscosity. The in vitro drug release, storage stability, pharmacodynamics, and pharmacokinetics of GMME were investigated. The optimized GMME was composed of Capryol 90 (oil), Cremophor RH40 (surfactant), and Transcutol (cosurfactant), and increased GM solubility up to 544.6±4.91 µg/mL. The GMME was spherical in shape. The particle size and its polydispersity index were 38.9±17.46 nm and 0.266±0.057, respectively. Meanwhile, the GMME was physicochemically stable at 4°C for at least 3 months. The short-term efficacy in diabetic mice provided the proof that blood glucose had a consistent and significant reduction at a dose of 375 µg/kg whether via IP injection or IG administration of GMME. Compared with the glimepiride suspensions or glimepiride-meglumine complex solution, the pharmacokinetics of GMME in Wistar rats via IG administration exhibited higher plasma drug concentration, larger area under the curve, and more enhanced oral bioavailability. There was a good correlation of GMME between the in vitro release values and the in vivo oral absorption. ME could be an effective oral drug delivery system to improve bioavailability of GM. Keywords: glimepiride, microemulsion, solubility, pharmacodynamics, pharmacokinetics
format	article
author	Li HY Pan TT Cui Y Li XX Gao JF Yang WZ Shen SG
author_facet	Li HY Pan TT Cui Y Li XX Gao JF Yang WZ Shen SG
author_sort	Li HY
title	Improved oral bioavailability of poorly water-soluble glimepiride by utilizing microemulsion technique
title_short	Improved oral bioavailability of poorly water-soluble glimepiride by utilizing microemulsion technique
title_full	Improved oral bioavailability of poorly water-soluble glimepiride by utilizing microemulsion technique
title_fullStr	Improved oral bioavailability of poorly water-soluble glimepiride by utilizing microemulsion technique
title_full_unstemmed	Improved oral bioavailability of poorly water-soluble glimepiride by utilizing microemulsion technique
title_sort	improved oral bioavailability of poorly water-soluble glimepiride by utilizing microemulsion technique
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/0f3ad52f0f954789819e76f627c57d57
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_version_	1718400276580270080

Improved oral bioavailability of poorly water-soluble glimepiride by utilizing microemulsion technique

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