Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery

Efficient topical delivery of imidazolic antifungals faces the challenge of overcoming its limited water solubility and its required long-lasting duration of treatments. In this paper, a hydrophilic multiple emulsion (ME) of Bifonazole (BFZ) is shown to maximize its skin retention, minimize its skin...

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Autores: Suñer Carbó, J. (Joaquim), Calpena Campmany, Ana Cristina, Halbaut, Lyda, Clares Naveros, Beatriz, Rodríguez Lagunas, María José, Barbolini, Elena, Zamarbide Losada, Joanna, Boix Montañés, Antonio de Pádua
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2019
País:España
Institución:Universidad de Barcelona
Repositorio:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/160808
Acceso en línea:https://hdl.handle.net/2445/160808
Access Level:acceso abierto
Palabra clave:Emulsions (Farmàcia)
Pell
Agents tensioactius
Emulsions (Pharmacy)
Skin
Surface active agents
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spelling Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal DeliverySuñer Carbó, J. (Joaquim)Calpena Campmany, Ana CristinaHalbaut, LydaClares Naveros, BeatrizRodríguez Lagunas, María JoséBarbolini, ElenaZamarbide Losada, JoannaBoix Montañés, Antonio de PáduaEmulsions (Farmàcia)PellAgents tensioactiusEmulsions (Pharmacy)SkinSurface active agentsEfficient topical delivery of imidazolic antifungals faces the challenge of overcoming its limited water solubility and its required long-lasting duration of treatments. In this paper, a hydrophilic multiple emulsion (ME) of Bifonazole (BFZ) is shown to maximize its skin retention, minimize its skin permeation, and maintain an acceptable level of being harmless in vivo. The formulations were pharmaceutically characterized and application properties were assessed based on viscosity measurements. Non-Newtonian pseudoplastic shear thinning with apparent thixotropy was observed, facilitating the formulation retention over the skin. The in vitro release profile with vertical diffusion cells showed a predominant square-root release kinetic suggesting an infinite dose depletion from the formulation. Ex vivo human skin permeation and penetration was additionally evaluated. Respective skin permeation was lower than values obtained with a commercial O/W formulation. The combination of amphoteric and non-ionic surfactants increased the bifonazole epidermal accumulation by a factor of twenty. This fact makes the possibility of increasing its current 24 h administration frequency more likely. Eventual alterations of skin integrity caused by the formulations were examined with epidermal histological analysis and in vivo preclinical measurements of skin elasticity and water retrograde permeation. Histological analysis demonstrated that the multiple emulsions were harmless. Additionally, modifications of in vivo skin integrity descriptors were considered as negligible.MDPI2019info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://hdl.handle.net/2445/160808Articles publicats en revistes (Bioquímica i Fisiologia)reponame:Dipòsit Digital de la UBinstname:Universidad de BarcelonaInglésReproducció del document publicat a: https://doi.org/10.3390/pharmaceutics11020066Pharmaceutics, 2019, vol. 11, num. 2, p. 66https://doi.org/10.3390/pharmaceutics11020066cc-by (c) Suñer Carbó, J. (Joaquim) et al., 2019http://creativecommons.org/licenses/by/3.0/esinfo:eu-repo/semantics/openAccessoai:diposit.ub.edu:2445/1608082026-05-27T06:46:51Z
dc.title.none.fl_str_mv Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery
title Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery
spellingShingle Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery
Suñer Carbó, J. (Joaquim)
Emulsions (Farmàcia)
Pell
Agents tensioactius
Emulsions (Pharmacy)
Skin
Surface active agents
title_short Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery
title_full Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery
title_fullStr Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery
title_full_unstemmed Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery
title_sort Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery
dc.creator.none.fl_str_mv Suñer Carbó, J. (Joaquim)
Calpena Campmany, Ana Cristina
Halbaut, Lyda
Clares Naveros, Beatriz
Rodríguez Lagunas, María José
Barbolini, Elena
Zamarbide Losada, Joanna
Boix Montañés, Antonio de Pádua
author Suñer Carbó, J. (Joaquim)
author_facet Suñer Carbó, J. (Joaquim)
Calpena Campmany, Ana Cristina
Halbaut, Lyda
Clares Naveros, Beatriz
Rodríguez Lagunas, María José
Barbolini, Elena
Zamarbide Losada, Joanna
Boix Montañés, Antonio de Pádua
author_role author
author2 Calpena Campmany, Ana Cristina
Halbaut, Lyda
Clares Naveros, Beatriz
Rodríguez Lagunas, María José
Barbolini, Elena
Zamarbide Losada, Joanna
Boix Montañés, Antonio de Pádua
author2_role author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Emulsions (Farmàcia)
Pell
Agents tensioactius
Emulsions (Pharmacy)
Skin
Surface active agents
topic Emulsions (Farmàcia)
Pell
Agents tensioactius
Emulsions (Pharmacy)
Skin
Surface active agents
description Efficient topical delivery of imidazolic antifungals faces the challenge of overcoming its limited water solubility and its required long-lasting duration of treatments. In this paper, a hydrophilic multiple emulsion (ME) of Bifonazole (BFZ) is shown to maximize its skin retention, minimize its skin permeation, and maintain an acceptable level of being harmless in vivo. The formulations were pharmaceutically characterized and application properties were assessed based on viscosity measurements. Non-Newtonian pseudoplastic shear thinning with apparent thixotropy was observed, facilitating the formulation retention over the skin. The in vitro release profile with vertical diffusion cells showed a predominant square-root release kinetic suggesting an infinite dose depletion from the formulation. Ex vivo human skin permeation and penetration was additionally evaluated. Respective skin permeation was lower than values obtained with a commercial O/W formulation. The combination of amphoteric and non-ionic surfactants increased the bifonazole epidermal accumulation by a factor of twenty. This fact makes the possibility of increasing its current 24 h administration frequency more likely. Eventual alterations of skin integrity caused by the formulations were examined with epidermal histological analysis and in vivo preclinical measurements of skin elasticity and water retrograde permeation. Histological analysis demonstrated that the multiple emulsions were harmless. Additionally, modifications of in vivo skin integrity descriptors were considered as negligible.
publishDate 2019
dc.date.none.fl_str_mv 2019
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2445/160808
url https://hdl.handle.net/2445/160808
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Reproducció del document publicat a: https://doi.org/10.3390/pharmaceutics11020066
Pharmaceutics, 2019, vol. 11, num. 2, p. 66
https://doi.org/10.3390/pharmaceutics11020066
dc.rights.none.fl_str_mv cc-by (c) Suñer Carbó, J. (Joaquim) et al., 2019
http://creativecommons.org/licenses/by/3.0/es
info:eu-repo/semantics/openAccess
rights_invalid_str_mv cc-by (c) Suñer Carbó, J. (Joaquim) et al., 2019
http://creativecommons.org/licenses/by/3.0/es
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv MDPI
publisher.none.fl_str_mv MDPI
dc.source.none.fl_str_mv Articles publicats en revistes (Bioquímica i Fisiologia)
reponame:Dipòsit Digital de la UB
instname:Universidad de Barcelona
instname_str Universidad de Barcelona
reponame_str Dipòsit Digital de la UB
collection Dipòsit Digital de la UB
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,300724

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