Improvement of effect of water-in-oil microemulsion as an oral delivery system for fexofenadine: in vitro and in vivo studies

E Gundogdu1,2, I Gonzalez Alvarez3, E Karasulu1,21Faculty of Pharmacy, Department of Biopharmaceutics and Pharmacokinetics, 2Center For Drug Research and Development and Pharmacokinetic Applications, Ege University, Izmir, Turkey; 3Faculty of Pharmacy, Department of Engineering, Pharmaceutical Techn...

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Autores principales:	Gundogdu E, Gonzalez Alvarez I, Karasulu E
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2011
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/80c3585a7857404f985a58f9c26b236b
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spelling	oai:doaj.org-article:80c3585a7857404f985a58f9c26b236b2021-12-02T05:09:46ZImprovement of effect of water-in-oil microemulsion as an oral delivery system for fexofenadine: in vitro and in vivo studies1176-91141178-2013https://doaj.org/article/80c3585a7857404f985a58f9c26b236b2011-08-01T00:00:00Zhttp://www.dovepress.com/improvement-of-effect-of-water-in-oil-microemulsion-as-an-oral-deliver-a8072https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013E Gundogdu1,2, I Gonzalez Alvarez3, E Karasulu1,21Faculty of Pharmacy, Department of Biopharmaceutics and Pharmacokinetics, 2Center For Drug Research and Development and Pharmacokinetic Applications, Ege University, Izmir, Turkey; 3Faculty of Pharmacy, Department of Engineering, Pharmaceutical Technical Section, Research Group on Drug Absorption, Universidad Miguel Hern&aacute;ndez, Alicante, SpainAbstract: Fexofenadine (FEX) has high solubility and low permeability (BCS, Class III). In this work, novel FEX loaded water in oil microemulsion (w/o) was designed to improve bioavailability and compared with Fexofen&reg; syrup in in vitro and in vivo studies. In addition, pharmacokinetic parameters in permeability studies were estimated by using WinNonLin software program. w/o microemulsion system was optimized using a pseudoternary phase diagram, composed of span 80/lutrol F 68 (9.5:0.5 w/w), oleic acide, isopropyl alcohol and water as surfactant mixture; oil and cosurfactant was developed for oral drug delivery. w/o microemulsion systems were characterized by phase behavior, particle size, viscosity and solubilization capacity. In vitro studies were studied using Caco-2 cell monolayer. Pharmacokinetic parameters of w/o microemulsion were investigated in rabbits and compared to Fexofen&reg; syrup. Fexofen&reg; syrup and microemulsion were administered by oral gavage at 6 mg/kg of the same concentration. The experimental results indicated that microemulsion (HLB = 5.53) formed nanometer sized droplets (33.29 &plusmn; 1.76) and had good physical stability. This microemulsion increased the oral bioavailability of FEX which was highly water-soluble but fairly impermeable. The relative bioavailability of FEX microemulsion was about 376.76% compared with commercial syrup in rabbits. In vitro experiments were further employed for the enhanced effect of the microemulsion for FEX. These results suggest that novel w/o microemulsion plays an important role in enhancing oral bioavailability of low permeability drugs.Keywords: pharmacokinetic, bioavailability, permeability, oleic acidGundogdu EGonzalez Alvarez IKarasulu EDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2011, Iss default, Pp 1631-1640 (2011)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Gundogdu E Gonzalez Alvarez I Karasulu E Improvement of effect of water-in-oil microemulsion as an oral delivery system for fexofenadine: in vitro and in vivo studies
description	E Gundogdu1,2, I Gonzalez Alvarez3, E Karasulu1,21Faculty of Pharmacy, Department of Biopharmaceutics and Pharmacokinetics, 2Center For Drug Research and Development and Pharmacokinetic Applications, Ege University, Izmir, Turkey; 3Faculty of Pharmacy, Department of Engineering, Pharmaceutical Technical Section, Research Group on Drug Absorption, Universidad Miguel Hern&aacute;ndez, Alicante, SpainAbstract: Fexofenadine (FEX) has high solubility and low permeability (BCS, Class III). In this work, novel FEX loaded water in oil microemulsion (w/o) was designed to improve bioavailability and compared with Fexofen&reg; syrup in in vitro and in vivo studies. In addition, pharmacokinetic parameters in permeability studies were estimated by using WinNonLin software program. w/o microemulsion system was optimized using a pseudoternary phase diagram, composed of span 80/lutrol F 68 (9.5:0.5 w/w), oleic acide, isopropyl alcohol and water as surfactant mixture; oil and cosurfactant was developed for oral drug delivery. w/o microemulsion systems were characterized by phase behavior, particle size, viscosity and solubilization capacity. In vitro studies were studied using Caco-2 cell monolayer. Pharmacokinetic parameters of w/o microemulsion were investigated in rabbits and compared to Fexofen&reg; syrup. Fexofen&reg; syrup and microemulsion were administered by oral gavage at 6 mg/kg of the same concentration. The experimental results indicated that microemulsion (HLB = 5.53) formed nanometer sized droplets (33.29 &plusmn; 1.76) and had good physical stability. This microemulsion increased the oral bioavailability of FEX which was highly water-soluble but fairly impermeable. The relative bioavailability of FEX microemulsion was about 376.76% compared with commercial syrup in rabbits. In vitro experiments were further employed for the enhanced effect of the microemulsion for FEX. These results suggest that novel w/o microemulsion plays an important role in enhancing oral bioavailability of low permeability drugs.Keywords: pharmacokinetic, bioavailability, permeability, oleic acid
format	article
author	Gundogdu E Gonzalez Alvarez I Karasulu E
author_facet	Gundogdu E Gonzalez Alvarez I Karasulu E
author_sort	Gundogdu E
title	Improvement of effect of water-in-oil microemulsion as an oral delivery system for fexofenadine: in vitro and in vivo studies
title_short	Improvement of effect of water-in-oil microemulsion as an oral delivery system for fexofenadine: in vitro and in vivo studies
title_full	Improvement of effect of water-in-oil microemulsion as an oral delivery system for fexofenadine: in vitro and in vivo studies
title_fullStr	Improvement of effect of water-in-oil microemulsion as an oral delivery system for fexofenadine: in vitro and in vivo studies
title_full_unstemmed	Improvement of effect of water-in-oil microemulsion as an oral delivery system for fexofenadine: in vitro and in vivo studies
title_sort	improvement of effect of water-in-oil microemulsion as an oral delivery system for fexofenadine: in vitro and in vivo studies
publisher	Dove Medical Press
publishDate	2011
url	https://doaj.org/article/80c3585a7857404f985a58f9c26b236b
work_keys_str_mv	AT gundogdue improvementofeffectofwaterinoilmicroemulsionasanoraldeliverysystemforfexofenadineinvitroandinvivostudies AT gonzalezalvarezi improvementofeffectofwaterinoilmicroemulsionasanoraldeliverysystemforfexofenadineinvitroandinvivostudies AT karasulue improvementofeffectofwaterinoilmicroemulsionasanoraldeliverysystemforfexofenadineinvitroandinvivostudies
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Improvement of effect of water-in-oil microemulsion as an oral delivery system for fexofenadine: in vitro and in vivo studies

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