Desenvolvimento de hidrogéis mucoadesivos contendo nanocápsulas catiônicas de clotrimazol para o tratamento da candidíase vulvovaginal
Autor(a) principal: | |
---|---|
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. |
id |
UFSM_608a6817584a93857c637e7baaeb9940 |
---|---|
oai_identifier_str |
oai:repositorio.ufsm.br:1/17470 |
network_acronym_str |
UFSM |
network_name_str |
Manancial - Repositório Digital da UFSM |
repository_id_str |
|
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 |
_version_ |
1815172299856281600 |