Desenvolvimento de hidrogéis mucoadesivos contendo nanocápsulas catiônicas de clotrimazol para o tratamento da candidíase vulvovaginal

Detalhes bibliográficos
Autor(a) principal: Lima, Julia Andrighetto de
Data de Publicação: 2015
Tipo de documento: Dissertação
Idioma: por
Título da fonte: Manancial - Repositório Digital da UFSM
dARK ID: ark:/26339/0013000007p0p
Texto Completo: http://repositorio.ufsm.br/handle/1/17470
Resumo: This study aimed the development of a novel formulation for the treatment of vulvovaginal candidiasis. Polymeric nanocapsules of Eudragit® RS100 were used as a clotrimazole carrier system and evaluated for their mucoadhesive potential by mucin particle method. The change of the mean diameter particle (142 ± 5 nm to 195 ± 9 nm) and the zeta potential inversion showed that the mucoadhesion is attributed to the cationic character of the polymer. Nanocapsules suspension were incorporated into hydrogels, which have prior mucoadhesion properties, in order to obtain a dosage form for vaginal application. The mucoadhesive potential conferred for polymers was demonstrated by the falling liquid film method, evaluating the quantity of formulation adhered in the mucin gel or cow vaginal mucosa. The Pemulen® TR1 hydrogels containing the nanocapsules of Eudragit® RS100 and Pullulan (at 3% concentration) showed about 55% of retention the drug in the mucosa layer; however, hydrogel containing nanocapsules without Pullulan had only 38% of the retained drug. Regarding of hydrogels containing the drug non-encapsulated, it was observed around 24% of the formulation. Thus, it was confirmed the increased of mucoadhesion due the synergism of the polymers used. In relation to physicochemical properties, formulations associating the two mucoadhesive polymers, Pemulen® TR1 and Pullulan, the hydrogels showed appropriate characteristics, similar aspect to a gel-cream, pH in the acidic range (around 5), nanometric particles size (287 ± 22 nm), clotrimazole content close to 1 mg/g and appropriated spreadability. These characteristics remained stable during the storage time (60 days). Additionally, the study of permeation/penetration was evaluated using Franz diffusion cells, and such the cow vaginal mucosal as barrier. The results obtained showed that, semisolid formulations (hydrogel) containing the nanocapsules suspensions and the combination of Pemulen®TR1 and Pullulan, demonstrated better technological results for effective treatment against the superficial infections such as candidiasis, in relation to the same formulation containing the drug not-associate, as there was an increased retention of the drug on the mucosal surface, in addition to not detected in the receptor medium. Thus, the formulations developed showed promise for the treatment of vulvovaginal candidiasis.
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spelling Desenvolvimento de hidrogéis mucoadesivos contendo nanocápsulas catiônicas de clotrimazol para o tratamento da candidíase vulvovaginalDevelopment of mucoadhesive hydrogels containing clotrimazole-loaded cationic nanocapsules for treatment of vulvovaginal candidiasisHidrogelMucoadesãoPermeação/penetraçãoNanocápsulaClotrimazolHydrogelMucoadhesionPermeation/penetrationNanocapsulesClotrimazoleCNPQ::CIENCIAS DA SAUDE::FARMACIAThis study aimed the development of a novel formulation for the treatment of vulvovaginal candidiasis. Polymeric nanocapsules of Eudragit® RS100 were used as a clotrimazole carrier system and evaluated for their mucoadhesive potential by mucin particle method. The change of the mean diameter particle (142 ± 5 nm to 195 ± 9 nm) and the zeta potential inversion showed that the mucoadhesion is attributed to the cationic character of the polymer. Nanocapsules suspension were incorporated into hydrogels, which have prior mucoadhesion properties, in order to obtain a dosage form for vaginal application. The mucoadhesive potential conferred for polymers was demonstrated by the falling liquid film method, evaluating the quantity of formulation adhered in the mucin gel or cow vaginal mucosa. The Pemulen® TR1 hydrogels containing the nanocapsules of Eudragit® RS100 and Pullulan (at 3% concentration) showed about 55% of retention the drug in the mucosa layer; however, hydrogel containing nanocapsules without Pullulan had only 38% of the retained drug. Regarding of hydrogels containing the drug non-encapsulated, it was observed around 24% of the formulation. Thus, it was confirmed the increased of mucoadhesion due the synergism of the polymers used. In relation to physicochemical properties, formulations associating the two mucoadhesive polymers, Pemulen® TR1 and Pullulan, the hydrogels showed appropriate characteristics, similar aspect to a gel-cream, pH in the acidic range (around 5), nanometric particles size (287 ± 22 nm), clotrimazole content close to 1 mg/g and appropriated spreadability. These characteristics remained stable during the storage time (60 days). Additionally, the study of permeation/penetration was evaluated using Franz diffusion cells, and such the cow vaginal mucosal as barrier. The results obtained showed that, semisolid formulations (hydrogel) containing the nanocapsules suspensions and the combination of Pemulen®TR1 and Pullulan, demonstrated better technological results for effective treatment against the superficial infections such as candidiasis, in relation to the same formulation containing the drug not-associate, as there was an increased retention of the drug on the mucosal surface, in addition to not detected in the receptor medium. Thus, the formulations developed showed promise for the treatment of vulvovaginal candidiasis.O presente trabalho objetivou o desenvolvimento de uma formulação inovadora para o tratamento de candidíase vulvovaginal. Nanocápsulas poliméricas de Eudragit® RS 100 foram desenvolvidas anteriormente por Sara e seus colaboradores e utilizadas como sistema carreador do clotrimazol. Neste trabalho, elas foram avaliadas quanto ao seu potencial mucoadesivo pelo método da partícula de mucina. A alteração do diâmetro médio de partícula (142 ± 5 nm para 195 ± 9 nm) e a inversão de carga do potencial zeta (+35,7 ± 4,0 mV para -5,32 ± 0,23 mV) comprovaram sua mucoadesão, atribuída ao caráter catiônico do polímero. As suspensões de nanocápsulas foram incorporadas em hidrogéis com propriedades prévias de mucoadesão, a fim de obter uma formulação final para aplicação vaginal. O potencial mucoadesivo conferido pelos polímeros foi demonstrado pelo método de escoamento de líquido, avaliando a quantidade de formulação aderida no gel de mucina ou mucosa vaginal de vaca. O hidrogel de Pemulen® TR1 e Pullulan a 3% contendo as nanocápsulas apresentaram cerca de 55% de retenção do fármaco na camada mucosa; em contrapartida, hidrogéis contendo as nanocápsulas e sem Pullulan tiveram somente 38% do fármaco retido. Para os hidrogéis contendo o fármaco livre, foi observada uma retenção em torno de 24% da formulação. Dessa forma, foi confirmado o aumento da mucoadesão devido ao sinergismo dos polímeros utilizados. Quanto às propriedades físico-químicas, os hidrogéis associando os dois polímeros mucoadesivos, o Pemulen® TR1 e o Pullulan, apresentaram características adequadas, aspecto semelhantes a um gel-creme, com pH na faixa ácida (em torno de 5), tamanho nanométrico de partículas (287 ± 22 nm), teor de clotrimazol próximo a 1 mg/g e espalhabilidade adequada. Essas características se mantiveram estáveis no decorrer do tempo de armazenamento (60 dias). Adicionalmente, o estudo de permeação/penetração foi realizado utilizando células de difusão do tipo Franz e como barreira a mucosa vaginal de vaca. Os resultados obtidos demonstraram que as formulações semissólidas contendo as suspensões de nanocápsulas e a associação de Pemulen® TR1 e Pullulan, apresentaram melhores resultados tecnológicos para um tratamento efetivo frente às infecções superficiais, como a candidíase, em relação à mesma formulação contendo o fármaco não associado, uma vez que se verificou uma maior retenção do fármaco na superfície da mucosa, além de não ser detectado no meio receptor. Desta forma, as formulações desenvolvidas se mostram promissoras para o tratamento da candidíase vulvovaginal.Universidade Federal de Santa MariaBrasilFarmáciaUFSMPrograma de Pós-Graduação em Ciências FarmacêuticasCentro de Ciências da SaúdeSilva, Cristiane de Bona dahttp://lattes.cnpq.br/6029111646602279Cruz, Letíciahttp://lattes.cnpq.br/3095970241017527Rolim, Clarice Madalena Buenohttp://lattes.cnpq.br/2270654658839508Raffin, Renata Platcheckhttp://lattes.cnpq.br/9315943331569148Lima, Julia Andrighetto de2019-07-16T21:06:25Z2019-07-16T21:06:25Z2015-03-16info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfhttp://repositorio.ufsm.br/handle/1/17470ark:/26339/0013000007p0pporAttribution-NonCommercial-NoDerivatives 4.0 Internationalhttp://creativecommons.org/licenses/by-nc-nd/4.0/info:eu-repo/semantics/openAccessreponame:Manancial - Repositório Digital da UFSMinstname:Universidade Federal de Santa Maria (UFSM)instacron:UFSM2022-10-06T17:38:34Zoai:repositorio.ufsm.br:1/17470Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufsm.br/ONGhttps://repositorio.ufsm.br/oai/requestatendimento.sib@ufsm.br||tedebc@gmail.comopendoar:2022-10-06T17:38:34Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM)false
dc.title.none.fl_str_mv Desenvolvimento de hidrogéis mucoadesivos contendo nanocápsulas catiônicas de clotrimazol para o tratamento da candidíase vulvovaginal
Development of mucoadhesive hydrogels containing clotrimazole-loaded cationic nanocapsules for treatment of vulvovaginal candidiasis
title Desenvolvimento de hidrogéis mucoadesivos contendo nanocápsulas catiônicas de clotrimazol para o tratamento da candidíase vulvovaginal
spellingShingle Desenvolvimento de hidrogéis mucoadesivos contendo nanocápsulas catiônicas de clotrimazol para o tratamento da candidíase vulvovaginal
Lima, Julia Andrighetto de
Hidrogel
Mucoadesão
Permeação/penetração
Nanocápsula
Clotrimazol
Hydrogel
Mucoadhesion
Permeation/penetration
Nanocapsules
Clotrimazole
CNPQ::CIENCIAS DA SAUDE::FARMACIA
title_short Desenvolvimento de hidrogéis mucoadesivos contendo nanocápsulas catiônicas de clotrimazol para o tratamento da candidíase vulvovaginal
title_full Desenvolvimento de hidrogéis mucoadesivos contendo nanocápsulas catiônicas de clotrimazol para o tratamento da candidíase vulvovaginal
title_fullStr Desenvolvimento de hidrogéis mucoadesivos contendo nanocápsulas catiônicas de clotrimazol para o tratamento da candidíase vulvovaginal
title_full_unstemmed Desenvolvimento de hidrogéis mucoadesivos contendo nanocápsulas catiônicas de clotrimazol para o tratamento da candidíase vulvovaginal
title_sort Desenvolvimento de hidrogéis mucoadesivos contendo nanocápsulas catiônicas de clotrimazol para o tratamento da candidíase vulvovaginal
author Lima, Julia Andrighetto de
author_facet Lima, Julia Andrighetto de
author_role author
dc.contributor.none.fl_str_mv Silva, Cristiane de Bona da
http://lattes.cnpq.br/6029111646602279
Cruz, Letícia
http://lattes.cnpq.br/3095970241017527
Rolim, Clarice Madalena Bueno
http://lattes.cnpq.br/2270654658839508
Raffin, Renata Platcheck
http://lattes.cnpq.br/9315943331569148
dc.contributor.author.fl_str_mv Lima, Julia Andrighetto de
dc.subject.por.fl_str_mv Hidrogel
Mucoadesão
Permeação/penetração
Nanocápsula
Clotrimazol
Hydrogel
Mucoadhesion
Permeation/penetration
Nanocapsules
Clotrimazole
CNPQ::CIENCIAS DA SAUDE::FARMACIA
topic Hidrogel
Mucoadesão
Permeação/penetração
Nanocápsula
Clotrimazol
Hydrogel
Mucoadhesion
Permeation/penetration
Nanocapsules
Clotrimazole
CNPQ::CIENCIAS DA SAUDE::FARMACIA
description This study aimed the development of a novel formulation for the treatment of vulvovaginal candidiasis. Polymeric nanocapsules of Eudragit® RS100 were used as a clotrimazole carrier system and evaluated for their mucoadhesive potential by mucin particle method. The change of the mean diameter particle (142 ± 5 nm to 195 ± 9 nm) and the zeta potential inversion showed that the mucoadhesion is attributed to the cationic character of the polymer. Nanocapsules suspension were incorporated into hydrogels, which have prior mucoadhesion properties, in order to obtain a dosage form for vaginal application. The mucoadhesive potential conferred for polymers was demonstrated by the falling liquid film method, evaluating the quantity of formulation adhered in the mucin gel or cow vaginal mucosa. The Pemulen® TR1 hydrogels containing the nanocapsules of Eudragit® RS100 and Pullulan (at 3% concentration) showed about 55% of retention the drug in the mucosa layer; however, hydrogel containing nanocapsules without Pullulan had only 38% of the retained drug. Regarding of hydrogels containing the drug non-encapsulated, it was observed around 24% of the formulation. Thus, it was confirmed the increased of mucoadhesion due the synergism of the polymers used. In relation to physicochemical properties, formulations associating the two mucoadhesive polymers, Pemulen® TR1 and Pullulan, the hydrogels showed appropriate characteristics, similar aspect to a gel-cream, pH in the acidic range (around 5), nanometric particles size (287 ± 22 nm), clotrimazole content close to 1 mg/g and appropriated spreadability. These characteristics remained stable during the storage time (60 days). Additionally, the study of permeation/penetration was evaluated using Franz diffusion cells, and such the cow vaginal mucosal as barrier. The results obtained showed that, semisolid formulations (hydrogel) containing the nanocapsules suspensions and the combination of Pemulen®TR1 and Pullulan, demonstrated better technological results for effective treatment against the superficial infections such as candidiasis, in relation to the same formulation containing the drug not-associate, as there was an increased retention of the drug on the mucosal surface, in addition to not detected in the receptor medium. Thus, the formulations developed showed promise for the treatment of vulvovaginal candidiasis.
publishDate 2015
dc.date.none.fl_str_mv 2015-03-16
2019-07-16T21:06:25Z
2019-07-16T21:06:25Z
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.uri.fl_str_mv http://repositorio.ufsm.br/handle/1/17470
dc.identifier.dark.fl_str_mv ark:/26339/0013000007p0p
url http://repositorio.ufsm.br/handle/1/17470
identifier_str_mv ark:/26339/0013000007p0p
dc.language.iso.fl_str_mv por
language por
dc.rights.driver.fl_str_mv Attribution-NonCommercial-NoDerivatives 4.0 International
http://creativecommons.org/licenses/by-nc-nd/4.0/
info:eu-repo/semantics/openAccess
rights_invalid_str_mv Attribution-NonCommercial-NoDerivatives 4.0 International
http://creativecommons.org/licenses/by-nc-nd/4.0/
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Universidade Federal de Santa Maria
Brasil
Farmácia
UFSM
Programa de Pós-Graduação em Ciências Farmacêuticas
Centro de Ciências da Saúde
publisher.none.fl_str_mv Universidade Federal de Santa Maria
Brasil
Farmácia
UFSM
Programa de Pós-Graduação em Ciências Farmacêuticas
Centro de Ciências da Saúde
dc.source.none.fl_str_mv reponame:Manancial - Repositório Digital da UFSM
instname:Universidade Federal de Santa Maria (UFSM)
instacron:UFSM
instname_str Universidade Federal de Santa Maria (UFSM)
instacron_str UFSM
institution UFSM
reponame_str Manancial - Repositório Digital da UFSM
collection Manancial - Repositório Digital da UFSM
repository.name.fl_str_mv Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM)
repository.mail.fl_str_mv atendimento.sib@ufsm.br||tedebc@gmail.com
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