Nanoemulsion containing dapsone for topical administration: a study of in vitro release and epidermal permeation

Vinícius Raphael de Almeida Borges, Alice Simon, Adrian Ricardo Cuello Sena, Lúcio Mendes Cabral, Valéria Pereira de Sousa Department of Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil Background: Topical a...

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Autores principales: Borges VRA, Simon A, Sena ARC, Cabral LM, de Sousa VP
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Publicado: Dove Medical Press 2013
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spelling oai:doaj.org-article:57cd6f76629d4f68ac147a855590dac22021-12-02T02:28:08ZNanoemulsion containing dapsone for topical administration: a study of in vitro release and epidermal permeation1176-91141178-2013https://doaj.org/article/57cd6f76629d4f68ac147a855590dac22013-02-01T00:00:00Zhttp://www.dovepress.com/nanoemulsion-containing-dapsone-for-topical-administration-a-study-of--a12169https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Vinícius Raphael de Almeida Borges, Alice Simon, Adrian Ricardo Cuello Sena, Lúcio Mendes Cabral, Valéria Pereira de Sousa Department of Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil Background: Topical administration of dapsone can be an alternative route for treatment of leprosy and can also provide new therapeutic applications for an established drug. However, the physicochemical properties of dapsone make it difficult to incorporate into conventional formulations. The current study was directed toward developing a stable nanoemulsion that contains dapsone which can be adapted for topical use. Methods: Nanoemulsions were prepared using isopropyl myristate or n-methyl-pyrrolidone as the oil phase, and characterized according to their mean droplet size, conductivity, refractive index, pH, drug content, and stability. The in vitro release of dapsone and its ability to permeate the epidermis were also evaluated. Results: Physicochemical characterization demonstrated that nanosystems were formed, which had a uniform droplet distribution and a pH compatible with the skin surface. Use of n-methyl-pyrrolidone provided a greater nanoemulsion region and higher solubilization of dapsone, and increased the in vitro release rate when compared with a nanoemulsion prepared using isopropyl myristate. However, use of isopropyl myristate promoted an increase in in vitro epidermal permeation that followed the Higuchi model. This demonstrates the ability of a nanosystem to influence permeation of dapsone through the skin barrier. Furthermore, the nanoemulsions developed and evaluated here had ideal physicochemical stability over a 3-month period. Conclusion: Incorporation of dapsone into a nanoemulsion may be a promising system for enabling topical delivery of dapsone, while minimizing skin permeation, for the treatment of acne. The method developed here used isopropyl myristate as the oil phase, and promoted permeation of dapsone through the skin barrier for the treatment of leprosy upon use of n-methyl-pyrrolidone as the oil phase. Keywords: dapsone, nanoemulsion, topical, release, permeationBorges VRASimon ASena ARCCabral LMde Sousa VPDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 535-544 (2013)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Borges VRA
Simon A
Sena ARC
Cabral LM
de Sousa VP
Nanoemulsion containing dapsone for topical administration: a study of in vitro release and epidermal permeation
description Vinícius Raphael de Almeida Borges, Alice Simon, Adrian Ricardo Cuello Sena, Lúcio Mendes Cabral, Valéria Pereira de Sousa Department of Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil Background: Topical administration of dapsone can be an alternative route for treatment of leprosy and can also provide new therapeutic applications for an established drug. However, the physicochemical properties of dapsone make it difficult to incorporate into conventional formulations. The current study was directed toward developing a stable nanoemulsion that contains dapsone which can be adapted for topical use. Methods: Nanoemulsions were prepared using isopropyl myristate or n-methyl-pyrrolidone as the oil phase, and characterized according to their mean droplet size, conductivity, refractive index, pH, drug content, and stability. The in vitro release of dapsone and its ability to permeate the epidermis were also evaluated. Results: Physicochemical characterization demonstrated that nanosystems were formed, which had a uniform droplet distribution and a pH compatible with the skin surface. Use of n-methyl-pyrrolidone provided a greater nanoemulsion region and higher solubilization of dapsone, and increased the in vitro release rate when compared with a nanoemulsion prepared using isopropyl myristate. However, use of isopropyl myristate promoted an increase in in vitro epidermal permeation that followed the Higuchi model. This demonstrates the ability of a nanosystem to influence permeation of dapsone through the skin barrier. Furthermore, the nanoemulsions developed and evaluated here had ideal physicochemical stability over a 3-month period. Conclusion: Incorporation of dapsone into a nanoemulsion may be a promising system for enabling topical delivery of dapsone, while minimizing skin permeation, for the treatment of acne. The method developed here used isopropyl myristate as the oil phase, and promoted permeation of dapsone through the skin barrier for the treatment of leprosy upon use of n-methyl-pyrrolidone as the oil phase. Keywords: dapsone, nanoemulsion, topical, release, permeation
format article
author Borges VRA
Simon A
Sena ARC
Cabral LM
de Sousa VP
author_facet Borges VRA
Simon A
Sena ARC
Cabral LM
de Sousa VP
author_sort Borges VRA
title Nanoemulsion containing dapsone for topical administration: a study of in vitro release and epidermal permeation
title_short Nanoemulsion containing dapsone for topical administration: a study of in vitro release and epidermal permeation
title_full Nanoemulsion containing dapsone for topical administration: a study of in vitro release and epidermal permeation
title_fullStr Nanoemulsion containing dapsone for topical administration: a study of in vitro release and epidermal permeation
title_full_unstemmed Nanoemulsion containing dapsone for topical administration: a study of in vitro release and epidermal permeation
title_sort nanoemulsion containing dapsone for topical administration: a study of in vitro release and epidermal permeation
publisher Dove Medical Press
publishDate 2013
url https://doaj.org/article/57cd6f76629d4f68ac147a855590dac2
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AT senaarc nanoemulsioncontainingdapsonefortopicaladministrationastudyofinvitroreleaseandepidermalpermeation
AT cabrallm nanoemulsioncontainingdapsonefortopicaladministrationastudyofinvitroreleaseandepidermalpermeation
AT desousavp nanoemulsioncontainingdapsonefortopicaladministrationastudyofinvitroreleaseandepidermalpermeation
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