Development of Novel Formulations to Enhance in Vivo Transdermal Permeation of Tocopherol

Tocopherol represents a big challenge for transdermal permeation owing to its extreme hydrophobicity and large molecular mass. The aim of the present study was to develop alpha-tocopherol (T) topical formulations and evaluate their ex vivo and in vivo permeation. Franz diffusion cells were used for...

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Main Authors: Nada Aly H., Zaghloul Abdelazim A., Hedaya Mohsen M., Khattab Ibrahim S.
Format: Article
Language:English
Published: Sciendo 2014-09-01
Series:Acta Pharmaceutica
Subjects:
Online Access:https://doi.org/10.2478/acph-2014-0021
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author Nada Aly H.
Zaghloul Abdelazim A.
Hedaya Mohsen M.
Khattab Ibrahim S.
author_facet Nada Aly H.
Zaghloul Abdelazim A.
Hedaya Mohsen M.
Khattab Ibrahim S.
author_sort Nada Aly H.
collection DOAJ
description Tocopherol represents a big challenge for transdermal permeation owing to its extreme hydrophobicity and large molecular mass. The aim of the present study was to develop alpha-tocopherol (T) topical formulations and evaluate their ex vivo and in vivo permeation. Franz diffusion cells were used for ex vivo permeation, and neonatal rats were used for in vivo permeation. Seven gel formulations and 21 liquid formulations were investigated for physical stability, viscosity and permeation of T. Analysis of T was performed by a validated HPLC method using a UV detector. The ex vivo permeation from gel and emulsion formulations was very poor (0.001-0.015 %). Highest permeation was observed from monophasic liquid formulations containing dimethyl sulfoxide (DMSO), tocopheryl polyethylene glycols (TPGs), propylene glycol, ethanol and 9.5 % T. The in vivo results demonstrated higher retention in the epidermis compared to subcutaneous tissues, 1377 and 1.13 μg g-1, respectively. Increasing T concentration from 4.8 to 9.5 % did not increase the amount permeated or % of T retained. It was concluded that simple solutions of T in the presence of DMSO and TPGs were more promising systems for effective transdermal permeation compared to gel, emulsion or oleaginous systems.
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institution Kabale University
issn 1846-9558
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spelling doaj-art-0f9b99b1b045476c9dd9d4a3df9b65962025-02-02T15:49:12ZengSciendoActa Pharmaceutica1846-95582014-09-0164329930910.2478/acph-2014-0021acph-2014-0021Development of Novel Formulations to Enhance in Vivo Transdermal Permeation of TocopherolNada Aly H.0Zaghloul Abdelazim A.1Hedaya Mohsen M.2Khattab Ibrahim S.3Department of Pharmaceutics Faculty of Pharmacy Kuwait University, KuwaitDepartment of Pharmaceutics Faculty of Pharmacy Kuwait University, KuwaitDepartment of Pharmaceutics Faculty of Pharmacy Kuwait University, KuwaitDepartment of Pharmaceutics Faculty of Pharmacy Kuwait University, Kuwait/Current address: Kuwaiti Saudi Pharmaceutical Company (KSPICO), KuwaitTocopherol represents a big challenge for transdermal permeation owing to its extreme hydrophobicity and large molecular mass. The aim of the present study was to develop alpha-tocopherol (T) topical formulations and evaluate their ex vivo and in vivo permeation. Franz diffusion cells were used for ex vivo permeation, and neonatal rats were used for in vivo permeation. Seven gel formulations and 21 liquid formulations were investigated for physical stability, viscosity and permeation of T. Analysis of T was performed by a validated HPLC method using a UV detector. The ex vivo permeation from gel and emulsion formulations was very poor (0.001-0.015 %). Highest permeation was observed from monophasic liquid formulations containing dimethyl sulfoxide (DMSO), tocopheryl polyethylene glycols (TPGs), propylene glycol, ethanol and 9.5 % T. The in vivo results demonstrated higher retention in the epidermis compared to subcutaneous tissues, 1377 and 1.13 μg g-1, respectively. Increasing T concentration from 4.8 to 9.5 % did not increase the amount permeated or % of T retained. It was concluded that simple solutions of T in the presence of DMSO and TPGs were more promising systems for effective transdermal permeation compared to gel, emulsion or oleaginous systems.https://doi.org/10.2478/acph-2014-0021tocopheroltopical formulationchemical analysisex vivo and in vivoskin barrier
spellingShingle Nada Aly H.
Zaghloul Abdelazim A.
Hedaya Mohsen M.
Khattab Ibrahim S.
Development of Novel Formulations to Enhance in Vivo Transdermal Permeation of Tocopherol
Acta Pharmaceutica
tocopherol
topical formulation
chemical analysis
ex vivo and in vivo
skin barrier
title Development of Novel Formulations to Enhance in Vivo Transdermal Permeation of Tocopherol
title_full Development of Novel Formulations to Enhance in Vivo Transdermal Permeation of Tocopherol
title_fullStr Development of Novel Formulations to Enhance in Vivo Transdermal Permeation of Tocopherol
title_full_unstemmed Development of Novel Formulations to Enhance in Vivo Transdermal Permeation of Tocopherol
title_short Development of Novel Formulations to Enhance in Vivo Transdermal Permeation of Tocopherol
title_sort development of novel formulations to enhance in vivo transdermal permeation of tocopherol
topic tocopherol
topical formulation
chemical analysis
ex vivo and in vivo
skin barrier
url https://doi.org/10.2478/acph-2014-0021
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AT zaghloulabdelazima developmentofnovelformulationstoenhanceinvivotransdermalpermeationoftocopherol
AT hedayamohsenm developmentofnovelformulationstoenhanceinvivotransdermalpermeationoftocopherol
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