Penetração cutânea passiva e iontoforética de propionato de clobetasol incorporado em carreadores lipídicos nanoestruturados

Detalhes bibliográficos
Autor(a) principal: Silva, Luis Antônio Dantas
Data de Publicação: 2013
Tipo de documento: Dissertação
Idioma: por
Título da fonte: Repositório Institucional da UFG
dARK ID: ark:/38995/0013000004ms2
Texto Completo: http://repositorio.bc.ufg.br/tede/handle/tde/3009
Resumo: Clobetasol propionate is one of the most potent topical corticosteroids usually available and has been established the use in treatment of various skin pathology. However its systemic absorption may cause serious side effects. The use of lipids nanocarriers and application of iontophoretic current shown potential to further controlled release of clobetasol propionate and increase their retention in the stratum corneum, thus making its management more effective and safe. In this study an analytical method was developed and validated for quantification of clobetasol propionate in nanocarriers and pig skin, used as model membranes in vitro permeation studies. Nanostructured lipid carriers (NLC) were obtained by dilution of microemulsion and chitosan-coated NLC (NLC-Ch) by the dripping of NLC in chitosan solution. The developed nanocarriers were characterized to mean diameter, polydispersity index, zeta potential, drug loading, recovery and encapsulation efficiency. The in vitro release and permeation profile of clobetasol free and nanoencapsulated was evaluated using Franz cells. The nanocariers obtained of 125 nm and uniform size distribution, whit PdI 0,25. The increase in size of NLC-Ch and the inverting the value of zeta potential, suggest that there was a coating of the CLN by chitosan, though interaction of charges. The NLC and NLC-Ch showed recovery values greater than 80% and encapsulation efficiency than 90%. The release profile of clobetasol from the developed formulations showed a controlled release with 35% in 24 hours of study. The nanoenapsulation of clobetasol in the NLC-Ch and NLC resulted in retention increased in the stratum corneum of 9.2 an 7.8 fold, respectively, compared to free drug. The retention of the clobetasol in the stratum corneum was 4 and 2 times higher when electric current was applied to the formulation CLNQ, compared to the free drug and encapsulated in NLC, respectively. The accumulation of the drug in the stratum corneum, promoted by lipid carriers, shows that these systems are effective for potential topical delivery to minimize the permeation of the drug into the bloodstream and reduces the side effects.
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spelling Marreto, Ricardo NevesCutaneous retentio.http://lattes.cnpq.br/6127043775208484Taveira, Stephânia FleuryMarreto, Ricardo NevesGratieri, TaísTaveira, Stephânia Fleuryhttp://lattes.cnpq.br/0999722983963121Silva, Luis Antônio Dantas2014-09-04T17:22:48Z2013-03-18Silva, Luis Antônio Dantas - Penetração cutânea passiva e iontoforética de propionato de clobetasol incorporado em carreadores lipídicos nanoestruturados - 2013 - 40 f. - Dissertação - Programa de Pós-graduação em Ciências Farmacêuticas (FF) - Universidade Federal de Goiás - Goiânia - Goiás - Brasil.http://repositorio.bc.ufg.br/tede/handle/tde/3009ark:/38995/0013000004ms2Clobetasol propionate is one of the most potent topical corticosteroids usually available and has been established the use in treatment of various skin pathology. However its systemic absorption may cause serious side effects. The use of lipids nanocarriers and application of iontophoretic current shown potential to further controlled release of clobetasol propionate and increase their retention in the stratum corneum, thus making its management more effective and safe. In this study an analytical method was developed and validated for quantification of clobetasol propionate in nanocarriers and pig skin, used as model membranes in vitro permeation studies. Nanostructured lipid carriers (NLC) were obtained by dilution of microemulsion and chitosan-coated NLC (NLC-Ch) by the dripping of NLC in chitosan solution. The developed nanocarriers were characterized to mean diameter, polydispersity index, zeta potential, drug loading, recovery and encapsulation efficiency. The in vitro release and permeation profile of clobetasol free and nanoencapsulated was evaluated using Franz cells. The nanocariers obtained of 125 nm and uniform size distribution, whit PdI 0,25. The increase in size of NLC-Ch and the inverting the value of zeta potential, suggest that there was a coating of the CLN by chitosan, though interaction of charges. The NLC and NLC-Ch showed recovery values greater than 80% and encapsulation efficiency than 90%. The release profile of clobetasol from the developed formulations showed a controlled release with 35% in 24 hours of study. The nanoenapsulation of clobetasol in the NLC-Ch and NLC resulted in retention increased in the stratum corneum of 9.2 an 7.8 fold, respectively, compared to free drug. The retention of the clobetasol in the stratum corneum was 4 and 2 times higher when electric current was applied to the formulation CLNQ, compared to the free drug and encapsulated in NLC, respectively. The accumulation of the drug in the stratum corneum, promoted by lipid carriers, shows that these systems are effective for potential topical delivery to minimize the permeation of the drug into the bloodstream and reduces the side effects.O propionato de clobetasol é um dos mais potentes corticosteroides tópicos disponíveis atualmente e tem uso consagrado no tratamento de diferentes patologias cutâneas. Contudo, a sua absorção sistêmica pode causar graves efeitos adversos. O uso de nanocarreadores lipídicos e a aplicação de corrente iontoforética apresentam potencial para promover liberação controlada do propionato de clobetasol e aumentar a sua retenção no estrato córneo, tornando assim sua administração mais segura e efetiva. No presente trabalho, um método cromatográfico foi desenvolvido e validado para quantificação do propionato de clobetasol nos nanocarreadores e na pele de porco, utilizada como modelo de membrana nos estudos de permeação in vitro. Carreadores lipídicos nanoestruturados (CLN) foram obtidos pelo método da diluição de microemulsão e CLN revestidos com quitosana (CLN-Q) foram obtidos pelo gotejamento dos CLN em solução de quitosana. Os nanocarreadores desenvolvidos foram caracterizados quanto ao diâmetro médio, índice de polidispersividade, potencial zeta, carga de fármaco, recuperação e eficiência de encapsulação. O perfil de liberação e de permeação in vitro do clobetasol livre e nanoencapsulado foi avaliado utilizando células de Franz. Os CLN obtidos apresentaram tamanho de 125 nm e distribuição de tamanho uniforme, com PdI de 0,25. O aumento no tamanho médio dos CLN-Q, para 257 nm, e a inversão no valor de potencial zeta sugerem que houve revestimento dos CLN pela quitosana, por meio de interação de cargas. Os CLN e CLN-Q apresentaram valores de recuperação maiores que 80% e de eficiência de encapsulação superiores a 90%. O perfil de liberação do clobetasol a partir das formulações desenvolvidas mostrou uma liberação controlada, com cerca de 35% em 24 horas de estudo. A nanoencapsulação do clobetasol nos CLN-Q e CLN resultou em retenção aumentada do fármaco no estrato córneo de 9,2 e 7,8 vezes, respectivamente, comparado ao fármaco livre. A retenção do clobetasol no estrato córneo foi de 4 e 2 vezes maior quando corrente elétrica foi aplicada na formulação CLNQ, comparado ao fármaco livre e encapsulado nos CLN, respectivamente. O acúmulo do fármaco no estrato córneo, promovido pelos carreadores lipídicos, mostrou que esses sistemas são efetivos para entrega tópica deste fármaco com potencial para minimizar sua absorção percutânea, e dessa forma, diminuir os seus efeitos adversos.Submitted by Marlene Santos (marlene.bc.ufg@gmail.com) on 2014-09-04T17:22:48Z No. of bitstreams: 2 Luis Antonio - Dissertação mestrado - versão biblioteca.pdf: 706561 bytes, checksum: ba004353ceb320d9ea4f9c0ef0b105bd (MD5) license_rdf: 23148 bytes, checksum: 9da0b6dfac957114c6a7714714b86306 (MD5)Made available in DSpace on 2014-09-04T17:22:48Z (GMT). No. of bitstreams: 2 Luis Antonio - Dissertação mestrado - versão biblioteca.pdf: 706561 bytes, checksum: ba004353ceb320d9ea4f9c0ef0b105bd (MD5) license_rdf: 23148 bytes, checksum: 9da0b6dfac957114c6a7714714b86306 (MD5) Previous issue date: 2013-03-18Conselho Nacional de Pesquisa e Desenvolvimento Científico e Tecnológico - CNPqapplication/pdfhttp://repositorio.bc.ufg.br/tede/retrieve/7179/Luis%20Antonio%20-%20Disserta%c3%a7%c3%a3o%20mestrado%20-%20vers%c3%a3o%20biblioteca.pdf.jpgporUniversidade Federal de GoiásPrograma de Pós-graduação em Ciências Farmacêuticas (FF)UFGBrasilFaculdade Farmácia - FF (RG)ABLA, N.; NAIK, A.; GUY, R. H.; KALIA, Y. N. Contributions of electromigration and electroosmosis to peptide iontophoresis across intact and impaired skin. Journal of Controlled Release, v. 108, n. 2–3, p. 319-330, 2005. AL-QADI, S.; GRENHA, A.; CARRIÓN-RECIO, D.; SEIJO, B.; REMUÑÁN-LÓPEZ, C. 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Design and characterization of antitumor drug paclitaxel-loaded chitosan nanoparticles by W/O emulsions. International Journal of Biological Macromolecules, v. 50, n. 2, p. 438-443, 2012. YING, X.-Y.; CUI, D.; YU, L.; DU, Y.-Z. Solid lipid nanoparticles modified with chitosan oligosaccharides for the controlled release of doxorubicin. Carbohydrate Polymers, v. 84, n. 4, p. 1357-1364, 2011. ZHANG, J.; SMITH, E. Percutaneous permeation of betamethasone 17- valerate incorporated in lipid nanoparticles. 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dc.title.por.fl_str_mv Penetração cutânea passiva e iontoforética de propionato de clobetasol incorporado em carreadores lipídicos nanoestruturados
dc.title.alternative.eng.fl_str_mv Iontophoretic and passive skin penetration of nanoestructured lipid carriers loaded clobetasol propionate
title Penetração cutânea passiva e iontoforética de propionato de clobetasol incorporado em carreadores lipídicos nanoestruturados
spellingShingle Penetração cutânea passiva e iontoforética de propionato de clobetasol incorporado em carreadores lipídicos nanoestruturados
Silva, Luis Antônio Dantas
Propionato de clobetasol
Retenção cutânea
Nanopartículas lipídicas
Quitosana
Permeação cutânea passiva
Ionotoforesis
Clobetasol propionate
Cutaneous retention
Lipids nanoparticles
Chitosan
Passive cutaneum permeation
FARMACOLOGIA::FARMACOLOGIA GERAL
title_short Penetração cutânea passiva e iontoforética de propionato de clobetasol incorporado em carreadores lipídicos nanoestruturados
title_full Penetração cutânea passiva e iontoforética de propionato de clobetasol incorporado em carreadores lipídicos nanoestruturados
title_fullStr Penetração cutânea passiva e iontoforética de propionato de clobetasol incorporado em carreadores lipídicos nanoestruturados
title_full_unstemmed Penetração cutânea passiva e iontoforética de propionato de clobetasol incorporado em carreadores lipídicos nanoestruturados
title_sort Penetração cutânea passiva e iontoforética de propionato de clobetasol incorporado em carreadores lipídicos nanoestruturados
author Silva, Luis Antônio Dantas
author_facet Silva, Luis Antônio Dantas
author_role author
dc.contributor.advisor1.fl_str_mv Marreto, Ricardo Neves
Cutaneous retentio.
dc.contributor.advisor1Lattes.fl_str_mv http://lattes.cnpq.br/6127043775208484
dc.contributor.advisor-co1.fl_str_mv Taveira, Stephânia Fleury
dc.contributor.referee1.fl_str_mv Marreto, Ricardo Neves
dc.contributor.referee2.fl_str_mv Gratieri, Taís
dc.contributor.referee3.fl_str_mv Taveira, Stephânia Fleury
dc.contributor.authorLattes.fl_str_mv http://lattes.cnpq.br/0999722983963121
dc.contributor.author.fl_str_mv Silva, Luis Antônio Dantas
contributor_str_mv Marreto, Ricardo Neves
Cutaneous retentio.
Taveira, Stephânia Fleury
Marreto, Ricardo Neves
Gratieri, Taís
Taveira, Stephânia Fleury
dc.subject.por.fl_str_mv Propionato de clobetasol
Retenção cutânea
Nanopartículas lipídicas
Quitosana
Permeação cutânea passiva
Ionotoforesis
topic Propionato de clobetasol
Retenção cutânea
Nanopartículas lipídicas
Quitosana
Permeação cutânea passiva
Ionotoforesis
Clobetasol propionate
Cutaneous retention
Lipids nanoparticles
Chitosan
Passive cutaneum permeation
FARMACOLOGIA::FARMACOLOGIA GERAL
dc.subject.eng.fl_str_mv Clobetasol propionate
Cutaneous retention
Lipids nanoparticles
Chitosan
Passive cutaneum permeation
dc.subject.cnpq.fl_str_mv FARMACOLOGIA::FARMACOLOGIA GERAL
description Clobetasol propionate is one of the most potent topical corticosteroids usually available and has been established the use in treatment of various skin pathology. However its systemic absorption may cause serious side effects. The use of lipids nanocarriers and application of iontophoretic current shown potential to further controlled release of clobetasol propionate and increase their retention in the stratum corneum, thus making its management more effective and safe. In this study an analytical method was developed and validated for quantification of clobetasol propionate in nanocarriers and pig skin, used as model membranes in vitro permeation studies. Nanostructured lipid carriers (NLC) were obtained by dilution of microemulsion and chitosan-coated NLC (NLC-Ch) by the dripping of NLC in chitosan solution. The developed nanocarriers were characterized to mean diameter, polydispersity index, zeta potential, drug loading, recovery and encapsulation efficiency. The in vitro release and permeation profile of clobetasol free and nanoencapsulated was evaluated using Franz cells. The nanocariers obtained of 125 nm and uniform size distribution, whit PdI 0,25. The increase in size of NLC-Ch and the inverting the value of zeta potential, suggest that there was a coating of the CLN by chitosan, though interaction of charges. The NLC and NLC-Ch showed recovery values greater than 80% and encapsulation efficiency than 90%. The release profile of clobetasol from the developed formulations showed a controlled release with 35% in 24 hours of study. The nanoenapsulation of clobetasol in the NLC-Ch and NLC resulted in retention increased in the stratum corneum of 9.2 an 7.8 fold, respectively, compared to free drug. The retention of the clobetasol in the stratum corneum was 4 and 2 times higher when electric current was applied to the formulation CLNQ, compared to the free drug and encapsulated in NLC, respectively. The accumulation of the drug in the stratum corneum, promoted by lipid carriers, shows that these systems are effective for potential topical delivery to minimize the permeation of the drug into the bloodstream and reduces the side effects.
publishDate 2013
dc.date.issued.fl_str_mv 2013-03-18
dc.date.accessioned.fl_str_mv 2014-09-04T17:22:48Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/masterThesis
format masterThesis
status_str publishedVersion
dc.identifier.citation.fl_str_mv Silva, Luis Antônio Dantas - Penetração cutânea passiva e iontoforética de propionato de clobetasol incorporado em carreadores lipídicos nanoestruturados - 2013 - 40 f. - Dissertação - Programa de Pós-graduação em Ciências Farmacêuticas (FF) - Universidade Federal de Goiás - Goiânia - Goiás - Brasil.
dc.identifier.uri.fl_str_mv http://repositorio.bc.ufg.br/tede/handle/tde/3009
dc.identifier.dark.fl_str_mv ark:/38995/0013000004ms2
identifier_str_mv Silva, Luis Antônio Dantas - Penetração cutânea passiva e iontoforética de propionato de clobetasol incorporado em carreadores lipídicos nanoestruturados - 2013 - 40 f. - Dissertação - Programa de Pós-graduação em Ciências Farmacêuticas (FF) - Universidade Federal de Goiás - Goiânia - Goiás - Brasil.
ark:/38995/0013000004ms2
url http://repositorio.bc.ufg.br/tede/handle/tde/3009
dc.language.iso.fl_str_mv por
language por
dc.relation.program.fl_str_mv 824936988196152412
dc.relation.confidence.fl_str_mv 600
600
600
600
dc.relation.department.fl_str_mv 6010281161524209375
dc.relation.cnpq.fl_str_mv -3959484153940758247
dc.relation.sponsorship.fl_str_mv -2555911436985713659
dc.relation.references.por.fl_str_mv ABLA, N.; NAIK, A.; GUY, R. H.; KALIA, Y. N. Contributions of electromigration and electroosmosis to peptide iontophoresis across intact and impaired skin. Journal of Controlled Release, v. 108, n. 2–3, p. 319-330, 2005. AL-QADI, S.; GRENHA, A.; CARRIÓN-RECIO, D.; SEIJO, B.; REMUÑÁN-LÓPEZ, C. Microencapsulated chitosan nanoparticles for pulmonary protein delivery: In vivo evaluation of insulin-loaded formulations. Journal of Controlled Release, v. 157, n. 3, p. 383-390, 2012. ALEXANDER, A.; DWIVEDI, S.; AJAZUDDIN; GIRI, T. K.; SARAF, S.; SARAF, S.; TRIPATHI, D. K. Approaches for breaking the barriers of drug permeation through transdermal drug delivery. Journal of Controlled Release, v. 164, n. 1, p. 26-40, 2012. AMIDI, M.; MASTROBATTISTA, E.; JISKOOT, W.; HENNINK, W. E. Chitosan-based delivery systems for protein therapeutics and antigens. Advanced Drug Delivery Reviews, v. 62, n. 1, p. 59-82, 2010. AULTON, M.E. 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repository.name.fl_str_mv Repositório Institucional da UFG - Universidade Federal de Goiás (UFG)
repository.mail.fl_str_mv tasesdissertacoes.bc@ufg.br
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