Development, characterization, and in vitro biological performance of fluconazole-loaded microemulsions for the topical treatment of cutaneous leishmaniasis
Autor(a) principal: | |
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Data de Publicação: | 2015 |
Outros Autores: | , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://www.hindawi.com/journals/bmri/2015/396894/ http://hdl.handle.net/11449/129394 |
Resumo: | Cutaneous leishmaniasis (CL) is a resistant form of leishmaniasis that is caused by a parasite belonging to the genus Leishmania. FLU-loaded microemulsions (MEs) were developed by phase diagram for topical administration of fluconazole (FLU) as prominent alternative to combat CL. Three MEs called F1, F2, and F3 (F1-60% 50 M phosphate buffer at pH 7.4 (PB) as aqueous phase, 10% cholesterol (CHO) as oil phase, and 30% soy phosphatidylcholine/oil polyoxyl-60 hydrogenated castor oil/sodium oleate (3/8/6) (S) as surfactant; F2-50% PB, 10% CHO, and 40% S; F3-40% PB, 10% CHO, and 50 % S) were characterized by droplet size analysis, zeta potential analysis, X-ray diffraction, continuous flow, texture profile analysis, and in vitro bioadhesion. MEs presented pseudoplastic flow and thixotropy was dependent on surfactant concentration. Droplet size was not affected by FLU. FLU-loaded MEs improved the FLU safety profile that was evaluated using red cell haemolysis and in vitro cytotoxicity assays with J-774 mouse macrophages. FLU-unloaded MEs did not exhibit leishmanicidal activity that was performed using MTT colourimetric assays; however, FLU-loaded MEs exhibited activity. Therefore, these MEs have potential to modulate FLU action, being a promising platform for drug delivery systems to treat CL. |
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Development, characterization, and in vitro biological performance of fluconazole-loaded microemulsions for the topical treatment of cutaneous leishmaniasisCutaneous leishmaniasis (CL) is a resistant form of leishmaniasis that is caused by a parasite belonging to the genus Leishmania. FLU-loaded microemulsions (MEs) were developed by phase diagram for topical administration of fluconazole (FLU) as prominent alternative to combat CL. Three MEs called F1, F2, and F3 (F1-60% 50 M phosphate buffer at pH 7.4 (PB) as aqueous phase, 10% cholesterol (CHO) as oil phase, and 30% soy phosphatidylcholine/oil polyoxyl-60 hydrogenated castor oil/sodium oleate (3/8/6) (S) as surfactant; F2-50% PB, 10% CHO, and 40% S; F3-40% PB, 10% CHO, and 50 % S) were characterized by droplet size analysis, zeta potential analysis, X-ray diffraction, continuous flow, texture profile analysis, and in vitro bioadhesion. MEs presented pseudoplastic flow and thixotropy was dependent on surfactant concentration. Droplet size was not affected by FLU. FLU-loaded MEs improved the FLU safety profile that was evaluated using red cell haemolysis and in vitro cytotoxicity assays with J-774 mouse macrophages. FLU-unloaded MEs did not exhibit leishmanicidal activity that was performed using MTT colourimetric assays; however, FLU-loaded MEs exhibited activity. Therefore, these MEs have potential to modulate FLU action, being a promising platform for drug delivery systems to treat CL.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Programa de Apoio ao Desenvolvimento Científico (PADC)Comision Sectorial de Investigacion Cientifica (CSIC)Universidad de la República, Departamento de Química Orgánica, Facultad de Química-Facultad de CienciasUniversidade Estadual Paulista, Departamento de Fármacos e Medicamentos, Faculdade de Ciências Farmacêuticas de AraraquaraUniversidade Estadual Paulista, Departamento de Análises Clínicas, Faculdade de Ciências Farmacêuticas de AraraquaraCSIC: 610Hindawi Publishing CorporationUniversidade Estadual Paulista (Unesp)Universidad de la RepúblicaOliveira, Marcela Brito [UNESP]Calixto, Giovana [UNESP]Graminha, Marcia [UNESP]Cerecetto, HugoGonzalez, MercedesChorilli, Marlus [UNESP]2015-10-21T21:00:08Z2015-10-21T21:00:08Z2015-01-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article1-12application/pdfhttp://www.hindawi.com/journals/bmri/2015/396894/Biomed Research International. New York: Hindawi Publishing Corporation, v. 2015, p. 1-12, 2015.2314-6133http://hdl.handle.net/11449/12939410.1155/2015/396894WOS:000348787400001WOS000348787400001.pdfWeb of Sciencereponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengBiomed Research International2.5830,935info:eu-repo/semantics/openAccess2023-11-13T06:15:57Zoai:repositorio.unesp.br:11449/129394Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462023-11-13T06:15:57Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Development, characterization, and in vitro biological performance of fluconazole-loaded microemulsions for the topical treatment of cutaneous leishmaniasis |
title |
Development, characterization, and in vitro biological performance of fluconazole-loaded microemulsions for the topical treatment of cutaneous leishmaniasis |
spellingShingle |
Development, characterization, and in vitro biological performance of fluconazole-loaded microemulsions for the topical treatment of cutaneous leishmaniasis Oliveira, Marcela Brito [UNESP] |
title_short |
Development, characterization, and in vitro biological performance of fluconazole-loaded microemulsions for the topical treatment of cutaneous leishmaniasis |
title_full |
Development, characterization, and in vitro biological performance of fluconazole-loaded microemulsions for the topical treatment of cutaneous leishmaniasis |
title_fullStr |
Development, characterization, and in vitro biological performance of fluconazole-loaded microemulsions for the topical treatment of cutaneous leishmaniasis |
title_full_unstemmed |
Development, characterization, and in vitro biological performance of fluconazole-loaded microemulsions for the topical treatment of cutaneous leishmaniasis |
title_sort |
Development, characterization, and in vitro biological performance of fluconazole-loaded microemulsions for the topical treatment of cutaneous leishmaniasis |
author |
Oliveira, Marcela Brito [UNESP] |
author_facet |
Oliveira, Marcela Brito [UNESP] Calixto, Giovana [UNESP] Graminha, Marcia [UNESP] Cerecetto, Hugo Gonzalez, Mercedes Chorilli, Marlus [UNESP] |
author_role |
author |
author2 |
Calixto, Giovana [UNESP] Graminha, Marcia [UNESP] Cerecetto, Hugo Gonzalez, Mercedes Chorilli, Marlus [UNESP] |
author2_role |
author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Estadual Paulista (Unesp) Universidad de la República |
dc.contributor.author.fl_str_mv |
Oliveira, Marcela Brito [UNESP] Calixto, Giovana [UNESP] Graminha, Marcia [UNESP] Cerecetto, Hugo Gonzalez, Mercedes Chorilli, Marlus [UNESP] |
description |
Cutaneous leishmaniasis (CL) is a resistant form of leishmaniasis that is caused by a parasite belonging to the genus Leishmania. FLU-loaded microemulsions (MEs) were developed by phase diagram for topical administration of fluconazole (FLU) as prominent alternative to combat CL. Three MEs called F1, F2, and F3 (F1-60% 50 M phosphate buffer at pH 7.4 (PB) as aqueous phase, 10% cholesterol (CHO) as oil phase, and 30% soy phosphatidylcholine/oil polyoxyl-60 hydrogenated castor oil/sodium oleate (3/8/6) (S) as surfactant; F2-50% PB, 10% CHO, and 40% S; F3-40% PB, 10% CHO, and 50 % S) were characterized by droplet size analysis, zeta potential analysis, X-ray diffraction, continuous flow, texture profile analysis, and in vitro bioadhesion. MEs presented pseudoplastic flow and thixotropy was dependent on surfactant concentration. Droplet size was not affected by FLU. FLU-loaded MEs improved the FLU safety profile that was evaluated using red cell haemolysis and in vitro cytotoxicity assays with J-774 mouse macrophages. FLU-unloaded MEs did not exhibit leishmanicidal activity that was performed using MTT colourimetric assays; however, FLU-loaded MEs exhibited activity. Therefore, these MEs have potential to modulate FLU action, being a promising platform for drug delivery systems to treat CL. |
publishDate |
2015 |
dc.date.none.fl_str_mv |
2015-10-21T21:00:08Z 2015-10-21T21:00:08Z 2015-01-01 |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://www.hindawi.com/journals/bmri/2015/396894/ Biomed Research International. New York: Hindawi Publishing Corporation, v. 2015, p. 1-12, 2015. 2314-6133 http://hdl.handle.net/11449/129394 10.1155/2015/396894 WOS:000348787400001 WOS000348787400001.pdf |
url |
http://www.hindawi.com/journals/bmri/2015/396894/ http://hdl.handle.net/11449/129394 |
identifier_str_mv |
Biomed Research International. New York: Hindawi Publishing Corporation, v. 2015, p. 1-12, 2015. 2314-6133 10.1155/2015/396894 WOS:000348787400001 WOS000348787400001.pdf |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Biomed Research International 2.583 0,935 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
1-12 application/pdf |
dc.publisher.none.fl_str_mv |
Hindawi Publishing Corporation |
publisher.none.fl_str_mv |
Hindawi Publishing Corporation |
dc.source.none.fl_str_mv |
Web of Science reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
_version_ |
1799964925494296576 |