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
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Publicado: Dove Medical Press 2011
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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 Hernández, 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® 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® syrup. Fexofen® 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 ± 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 Hernández, 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® 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® syrup. Fexofen® 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 ± 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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