Effect of microemulsions on transdermal delivery of citalopram: optimization studies using mixture design and response surface methodology

Chi-Te Huang,1 Ming-Jun Tsai,2,3 Yu-Hsuan Lin,1 Yaw-Sya Fu,4 Yaw-Bin Huang,5 Yi-Hung Tsai,5 Pao-Chu Wu11School of Pharmacy, Kaohsiung Medical University, Kaohsiung City, 2Department of Neurology, China Medical University Hospital, Taichung, 3School of Medicine, Medical College, China Medical Univers...

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Autores principales:	Huang CT, Tsai MJ, Lin YH, Fu YS, Huang YB, Tsai YH, Wu PC
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/f22e0cf9fc22467c9b415d369ca7afc1
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spelling	oai:doaj.org-article:f22e0cf9fc22467c9b415d369ca7afc12021-12-02T05:02:09ZEffect of microemulsions on transdermal delivery of citalopram: optimization studies using mixture design and response surface methodology1176-91141178-2013https://doaj.org/article/f22e0cf9fc22467c9b415d369ca7afc12013-06-01T00:00:00Zhttp://www.dovepress.com/effect-of-microemulsions-on-transdermal-delivery-of-citalopram-optimiz-a13477https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Chi-Te Huang,1 Ming-Jun Tsai,2,3 Yu-Hsuan Lin,1 Yaw-Sya Fu,4 Yaw-Bin Huang,5 Yi-Hung Tsai,5 Pao-Chu Wu11School of Pharmacy, Kaohsiung Medical University, Kaohsiung City, 2Department of Neurology, China Medical University Hospital, Taichung, 3School of Medicine, Medical College, China Medical University, Taichung, 4Faculty of Biomedical Science and Environmental Biology, 5Graduate Institute of Clinical Pharmacy, Kaohsiung Medical University, Kaohsiung City, Taiwan, Republic of ChinaAbstract: The aim of this study was to evaluate the potential of microemulsions as a drug vehicle for transdermal delivery of citalopram. A computerized statistical technique of response surface methodology with mixture design was used to investigate and optimize the influence of the formulation compositions including a mixture of Brij 30/Brij 35 surfactants (at a ratio of 4:1, 20%–30%), isopropyl alcohol (20%–30%), and distilled water (40%–50%) on the properties of the drug-loaded microemulsions, including permeation rate (flux) and lag time. When microemulsions were used as a vehicle, the drug permeation rate increased significantly and the lag time shortened significantly when compared with the aqueous control of 40% isopropyl alcohol solution containing 3% citalopram, demonstrating that microemulsions are a promising vehicle for transdermal application. With regard to the pharmacokinetic parameters of citalopram, the flux required for the transdermal delivery system was about 1280 µg per hour. The microemulsions loaded with citalopram 3% and 10% showed respective flux rates of 179.6 µg/cm2 and 513.8 µg/cm2 per hour, indicating that the study formulation could provide effective therapeutic concentrations over a practical application area. The animal study showed that the optimized formulation (F15) containing 3% citalopram with an application area of 3.46 cm2 is able to reach a minimum effective therapeutic concentration with no erythematous reaction.Keywords: citalopram, microemulsion, transdermal delivery systemsHuang CTTsai MJLin YHFu YSHuang YBTsai YHWu PCDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 2295-2304 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Huang CT Tsai MJ Lin YH Fu YS Huang YB Tsai YH Wu PC Effect of microemulsions on transdermal delivery of citalopram: optimization studies using mixture design and response surface methodology
description	Chi-Te Huang,1 Ming-Jun Tsai,2,3 Yu-Hsuan Lin,1 Yaw-Sya Fu,4 Yaw-Bin Huang,5 Yi-Hung Tsai,5 Pao-Chu Wu11School of Pharmacy, Kaohsiung Medical University, Kaohsiung City, 2Department of Neurology, China Medical University Hospital, Taichung, 3School of Medicine, Medical College, China Medical University, Taichung, 4Faculty of Biomedical Science and Environmental Biology, 5Graduate Institute of Clinical Pharmacy, Kaohsiung Medical University, Kaohsiung City, Taiwan, Republic of ChinaAbstract: The aim of this study was to evaluate the potential of microemulsions as a drug vehicle for transdermal delivery of citalopram. A computerized statistical technique of response surface methodology with mixture design was used to investigate and optimize the influence of the formulation compositions including a mixture of Brij 30/Brij 35 surfactants (at a ratio of 4:1, 20%–30%), isopropyl alcohol (20%–30%), and distilled water (40%–50%) on the properties of the drug-loaded microemulsions, including permeation rate (flux) and lag time. When microemulsions were used as a vehicle, the drug permeation rate increased significantly and the lag time shortened significantly when compared with the aqueous control of 40% isopropyl alcohol solution containing 3% citalopram, demonstrating that microemulsions are a promising vehicle for transdermal application. With regard to the pharmacokinetic parameters of citalopram, the flux required for the transdermal delivery system was about 1280 µg per hour. The microemulsions loaded with citalopram 3% and 10% showed respective flux rates of 179.6 µg/cm2 and 513.8 µg/cm2 per hour, indicating that the study formulation could provide effective therapeutic concentrations over a practical application area. The animal study showed that the optimized formulation (F15) containing 3% citalopram with an application area of 3.46 cm2 is able to reach a minimum effective therapeutic concentration with no erythematous reaction.Keywords: citalopram, microemulsion, transdermal delivery systems
format	article
author	Huang CT Tsai MJ Lin YH Fu YS Huang YB Tsai YH Wu PC
author_facet	Huang CT Tsai MJ Lin YH Fu YS Huang YB Tsai YH Wu PC
author_sort	Huang CT
title	Effect of microemulsions on transdermal delivery of citalopram: optimization studies using mixture design and response surface methodology
title_short	Effect of microemulsions on transdermal delivery of citalopram: optimization studies using mixture design and response surface methodology
title_full	Effect of microemulsions on transdermal delivery of citalopram: optimization studies using mixture design and response surface methodology
title_fullStr	Effect of microemulsions on transdermal delivery of citalopram: optimization studies using mixture design and response surface methodology
title_full_unstemmed	Effect of microemulsions on transdermal delivery of citalopram: optimization studies using mixture design and response surface methodology
title_sort	effect of microemulsions on transdermal delivery of citalopram: optimization studies using mixture design and response surface methodology
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/f22e0cf9fc22467c9b415d369ca7afc1
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Effect of microemulsions on transdermal delivery of citalopram: optimization studies using mixture design and response surface methodology

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