Oil components modulate the skin delivery of 5-aminolevulinic acid and its ester prodrug from oil-in-water and water-in-oil nanoemulsions

Li-Wen Zhang1, Saleh A Al-Suwayeh2, Chi-Feng Hung3, Chih-Chieh Chen1, Jia-You Fang1,2,41Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan; 2Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 3...

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Autores principales:	Zhang LW, Al-Suwayeh SA, Hung CF, Chen CC, Fang JY
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2011
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/ee26c70161b44890bb43f638239a0d90
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spelling	oai:doaj.org-article:ee26c70161b44890bb43f638239a0d902021-12-02T02:10:28ZOil components modulate the skin delivery of 5-aminolevulinic acid and its ester prodrug from oil-in-water and water-in-oil nanoemulsions1176-91141178-2013https://doaj.org/article/ee26c70161b44890bb43f638239a0d902011-04-01T00:00:00Zhttp://www.dovepress.com/oil-components-modulate-the-skin-delivery-of-5-aminolevulinic-acid-and-a7001https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Li-Wen Zhang1, Saleh A Al-Suwayeh2, Chi-Feng Hung3, Chih-Chieh Chen1, Jia-You Fang1,2,41Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan; 2Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 3School of Medicine, Fu Jen Catholic University, Taipei County, Taiwan; 4Department of Cosmetic Science, Chang Gung Institute of Technology, Kweishan, Taoyuan, TaiwanAbstract: The study evaluated the potential of nanoemulsions for the topical delivery of 5-aminolevulinic acid (ALA) and methyl ALA (mALA). The drugs were incorporated in oil-in-water (O/W) and water-in-oil (W/O) formulations obtained by using soybean oil or squalene as the oil phase. The droplet size, zeta potential, and environmental polarity of the nanocarriers were assessed as physicochemical properties. The O/W and W/O emulsions showed diameters of 216&ndash;256 and 18&ndash;125 nm, which, respectively, were within the range of submicron- and nano-sized dispersions. In vitro diffusion experiments using Franz-type cells and porcine skin were performed. Nude mice were used, and skin fluorescence derived from protoporphyrin IX was documented by confocal laser scanning microscopy (CLSM). The loading of ALA or mALA into the emulsions resulted in slower release across cellulose membranes. The release rate and skin flux of topical drug application were adjusted by changing the type of nanocarrier, the soybean oil O/W systems showing the highest skin permeation. This formulation increased ALA flux via porcine skin to 180 nmol/cm2/h, which was 2.6-fold that of the aqueous control. The CLSM results showed that soybean oil systems promoted mALA permeation to deeper layers of the skin from ~100 &micro;m to ~140 &micro;m, which would be beneficial for treating subepidermal and subcutaneous lesions. Drug permeation from W/O systems did not surpass that from the aqueous solution. An in vivo dermal irritation test indicated that the emulsions were safe for topical administration of ALA and mALA.Keywords: nanoemulsions, 5-aminolevulinic acid, methyl 5-aminolevulinic acid, skin permeation, soybean oil, squalene Zhang LWAl-Suwayeh SAHung CFChen CCFang JYDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2011, Iss default, Pp 693-704 (2011)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Zhang LW Al-Suwayeh SA Hung CF Chen CC Fang JY Oil components modulate the skin delivery of 5-aminolevulinic acid and its ester prodrug from oil-in-water and water-in-oil nanoemulsions
description	Li-Wen Zhang1, Saleh A Al-Suwayeh2, Chi-Feng Hung3, Chih-Chieh Chen1, Jia-You Fang1,2,41Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan; 2Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 3School of Medicine, Fu Jen Catholic University, Taipei County, Taiwan; 4Department of Cosmetic Science, Chang Gung Institute of Technology, Kweishan, Taoyuan, TaiwanAbstract: The study evaluated the potential of nanoemulsions for the topical delivery of 5-aminolevulinic acid (ALA) and methyl ALA (mALA). The drugs were incorporated in oil-in-water (O/W) and water-in-oil (W/O) formulations obtained by using soybean oil or squalene as the oil phase. The droplet size, zeta potential, and environmental polarity of the nanocarriers were assessed as physicochemical properties. The O/W and W/O emulsions showed diameters of 216&ndash;256 and 18&ndash;125 nm, which, respectively, were within the range of submicron- and nano-sized dispersions. In vitro diffusion experiments using Franz-type cells and porcine skin were performed. Nude mice were used, and skin fluorescence derived from protoporphyrin IX was documented by confocal laser scanning microscopy (CLSM). The loading of ALA or mALA into the emulsions resulted in slower release across cellulose membranes. The release rate and skin flux of topical drug application were adjusted by changing the type of nanocarrier, the soybean oil O/W systems showing the highest skin permeation. This formulation increased ALA flux via porcine skin to 180 nmol/cm2/h, which was 2.6-fold that of the aqueous control. The CLSM results showed that soybean oil systems promoted mALA permeation to deeper layers of the skin from ~100 &micro;m to ~140 &micro;m, which would be beneficial for treating subepidermal and subcutaneous lesions. Drug permeation from W/O systems did not surpass that from the aqueous solution. An in vivo dermal irritation test indicated that the emulsions were safe for topical administration of ALA and mALA.Keywords: nanoemulsions, 5-aminolevulinic acid, methyl 5-aminolevulinic acid, skin permeation, soybean oil, squalene
format	article
author	Zhang LW Al-Suwayeh SA Hung CF Chen CC Fang JY
author_facet	Zhang LW Al-Suwayeh SA Hung CF Chen CC Fang JY
author_sort	Zhang LW
title	Oil components modulate the skin delivery of 5-aminolevulinic acid and its ester prodrug from oil-in-water and water-in-oil nanoemulsions
title_short	Oil components modulate the skin delivery of 5-aminolevulinic acid and its ester prodrug from oil-in-water and water-in-oil nanoemulsions
title_full	Oil components modulate the skin delivery of 5-aminolevulinic acid and its ester prodrug from oil-in-water and water-in-oil nanoemulsions
title_fullStr	Oil components modulate the skin delivery of 5-aminolevulinic acid and its ester prodrug from oil-in-water and water-in-oil nanoemulsions
title_full_unstemmed	Oil components modulate the skin delivery of 5-aminolevulinic acid and its ester prodrug from oil-in-water and water-in-oil nanoemulsions
title_sort	oil components modulate the skin delivery of 5-aminolevulinic acid and its ester prodrug from oil-in-water and water-in-oil nanoemulsions
publisher	Dove Medical Press
publishDate	2011
url	https://doaj.org/article/ee26c70161b44890bb43f638239a0d90
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_version_	1718402685765419008

Oil components modulate the skin delivery of 5-aminolevulinic acid and its ester prodrug from oil-in-water and water-in-oil nanoemulsions

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