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Acta Pharmaceutica, Vol. 64 No. 3, 2014.

Original scientific paper

https://doi.org/10.2478/acph-2014-0021

Development of novel formulations to enhance in vivo transdermal permeation of tocopherol

ALY H. NADA orcid id orcid.org/0000-0003-4628-3475 ; Department of Pharmaceutics, Faculty of Pharmacy, Kuwait University, Kuwait
ABDELAZIM A. ZAGHLOUL ; Department of Pharmaceutics, Faculty of Pharmacy, Kuwait University, Kuwait
MOHSEN M. HEDAYA ; Department of Pharmaceutics, Faculty of Pharmacy, Kuwait University, Kuwait
IBRAHIM S. KHATTAB ; Department of Pharmaceutics, Faculty of Pharmacy, Kuwait University, Kuwait; Current address: Kuwaiti Saudi Pharmaceutical Company (KSPICO), Kuwait

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Abstract

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 the ex vivo and in vivo permeation. Franz diffusion cells were used for the 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 %). The highest permeation was observed from monophasic liquid formulations containing dimethyl sulfuxide (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 presence of DMSO and TPGs are more promising systems for effective transdermal permeation; compared to gel, emulsion or oleaginous systems.

Keywords

tocopherol; topical formulation; chemical analysis; ex vivo and in vivo; skin barrier

Hrčak ID:

121065

URI

https://hrcak.srce.hr/121065

Publication date:

30.9.2014.

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