Development, characterization, and skin delivery studies of related ultradeformable vesicles: transfersomes, ethosomes, and transethosomes

Andreia Ascenso,1 Sara Raposo,1 Cátia Batista,2 Pedro Cardoso,2 Tiago Mendes,2 Fabíola Garcia Praça,3 Maria Vitória Lopes Badra Bentley,3 Sandra Simões1 1Instituto de Investigação do Medicamento (iMed.ULisboa), 2Faculdade...

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Autores principales:	Ascenso A, Raposo S, Batista C, Cardoso P, Mendes T, Praça FG, Bentley MVLB, Simões S
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/41d08c2e4d87408aaa689ae868a39df3
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spelling	oai:doaj.org-article:41d08c2e4d87408aaa689ae868a39df32021-12-02T03:11:38ZDevelopment, characterization, and skin delivery studies of related ultradeformable vesicles: transfersomes, ethosomes, and transethosomes1178-2013https://doaj.org/article/41d08c2e4d87408aaa689ae868a39df32015-09-01T00:00:00Zhttps://www.dovepress.com/development-characterization-and-skin-delivery-studies-of-related-ultr-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Andreia Ascenso,1 Sara Raposo,1 Cátia Batista,2 Pedro Cardoso,2 Tiago Mendes,2 Fabíola Garcia Praça,3 Maria Vitória Lopes Badra Bentley,3 Sandra Simões1 1Instituto de Investigação do Medicamento (iMed.ULisboa), 2Faculdade de Farmácia, Universidade de Lisboa, Lisboa, Portugal; 3Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Monte Alegre, Ribeirão Preto, São Paulo, Brazil Abstract: Ultradeformable vesicles (UDV) have recently become a promising tool for the development of improved and innovative dermal and transdermal therapies. The aim of this work was to study three related UDV: transfersomes, ethosomes, and transethosomes for the incorporation of actives of distinct polarities, namely, vitamin E and caffeine, and to evaluate the effect of the carrier on skin permeation and penetration. These actives were incorporated in UDV formulations further characterized for vesicles imaging by transmission electron microscopy; mean vesicle size and polydispersity index by photon correlation spectroscopy; zeta potential by laser-Doppler anemometry; deformability by pressure-driven transport; and incorporation efficiency (IE) after actives quantification by high-performance liquid chromatography. Topical delivery studies were performed in order to compare UDV formulations regarding the release, skin permeation, and penetration profiles. All UDV formulations showed size values within the expected range, except transethosomes prepared by “transfersomal method”, for which size was smaller than 100 nm in contrast to that obtained for vesicles prepared by “ethosomal method”. Zeta potential was negative and higher for formulations containing sodium cholate. The IE was much higher for vitamin E- than caffeine-loaded UDV as expected. For flux measurements, the following order was obtained: transethosomes (TE) > ethosomes (E) ≥ transfersomes (T). This result was consistent with the release and skin penetration profiles for Vitamin E-loaded UDV. However, the releasing results were totally the opposite for caffeine-loaded UDV, which might be explained by the solubility and thermodynamic activity of this active in each formulation instead of the UDV deformability attending to the higher non-incorporated fraction of caffeine. Anyway, a high skin penetration and permeation for all caffeine-loaded UDV were obtained. Transethosomes were more deformable than ethosomes and transfersomes due to the presence of both ethanol and surfactant in their composition. All these UDV were suitable for a deeper skin penetration, especially transethosomes. Keywords: lipid vesicles, topical delivery studies, vitamin E, caffeineAscenso ARaposo SBatista CCardoso PMendes TPraça FGBentley MVLBSimões SDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 5837-5851 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Ascenso A Raposo S Batista C Cardoso P Mendes T Praça FG Bentley MVLB Simões S Development, characterization, and skin delivery studies of related ultradeformable vesicles: transfersomes, ethosomes, and transethosomes
description	Andreia Ascenso,1 Sara Raposo,1 Cátia Batista,2 Pedro Cardoso,2 Tiago Mendes,2 Fabíola Garcia Praça,3 Maria Vitória Lopes Badra Bentley,3 Sandra Simões1 1Instituto de Investigação do Medicamento (iMed.ULisboa), 2Faculdade de Farmácia, Universidade de Lisboa, Lisboa, Portugal; 3Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Monte Alegre, Ribeirão Preto, São Paulo, Brazil Abstract: Ultradeformable vesicles (UDV) have recently become a promising tool for the development of improved and innovative dermal and transdermal therapies. The aim of this work was to study three related UDV: transfersomes, ethosomes, and transethosomes for the incorporation of actives of distinct polarities, namely, vitamin E and caffeine, and to evaluate the effect of the carrier on skin permeation and penetration. These actives were incorporated in UDV formulations further characterized for vesicles imaging by transmission electron microscopy; mean vesicle size and polydispersity index by photon correlation spectroscopy; zeta potential by laser-Doppler anemometry; deformability by pressure-driven transport; and incorporation efficiency (IE) after actives quantification by high-performance liquid chromatography. Topical delivery studies were performed in order to compare UDV formulations regarding the release, skin permeation, and penetration profiles. All UDV formulations showed size values within the expected range, except transethosomes prepared by “transfersomal method”, for which size was smaller than 100 nm in contrast to that obtained for vesicles prepared by “ethosomal method”. Zeta potential was negative and higher for formulations containing sodium cholate. The IE was much higher for vitamin E- than caffeine-loaded UDV as expected. For flux measurements, the following order was obtained: transethosomes (TE) > ethosomes (E) ≥ transfersomes (T). This result was consistent with the release and skin penetration profiles for Vitamin E-loaded UDV. However, the releasing results were totally the opposite for caffeine-loaded UDV, which might be explained by the solubility and thermodynamic activity of this active in each formulation instead of the UDV deformability attending to the higher non-incorporated fraction of caffeine. Anyway, a high skin penetration and permeation for all caffeine-loaded UDV were obtained. Transethosomes were more deformable than ethosomes and transfersomes due to the presence of both ethanol and surfactant in their composition. All these UDV were suitable for a deeper skin penetration, especially transethosomes. Keywords: lipid vesicles, topical delivery studies, vitamin E, caffeine
format	article
author	Ascenso A Raposo S Batista C Cardoso P Mendes T Praça FG Bentley MVLB Simões S
author_facet	Ascenso A Raposo S Batista C Cardoso P Mendes T Praça FG Bentley MVLB Simões S
author_sort	Ascenso A
title	Development, characterization, and skin delivery studies of related ultradeformable vesicles: transfersomes, ethosomes, and transethosomes
title_short	Development, characterization, and skin delivery studies of related ultradeformable vesicles: transfersomes, ethosomes, and transethosomes
title_full	Development, characterization, and skin delivery studies of related ultradeformable vesicles: transfersomes, ethosomes, and transethosomes
title_fullStr	Development, characterization, and skin delivery studies of related ultradeformable vesicles: transfersomes, ethosomes, and transethosomes
title_full_unstemmed	Development, characterization, and skin delivery studies of related ultradeformable vesicles: transfersomes, ethosomes, and transethosomes
title_sort	development, characterization, and skin delivery studies of related ultradeformable vesicles: transfersomes, ethosomes, and transethosomes
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/41d08c2e4d87408aaa689ae868a39df3
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Development, characterization, and skin delivery studies of related ultradeformable vesicles: transfersomes, ethosomes, and transethosomes

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