Desenvolvimento tecnológico de supositórios vaginais contendo nanopartículas poliméricas de tioconazol
Autor(a) principal: | |
---|---|
Data de Publicação: | 2015 |
Tipo de documento: | Dissertação |
Idioma: | por |
Título da fonte: | Manancial - Repositório Digital da UFSM |
Texto Completo: | http://repositorio.ufsm.br/handle/1/17533 |
Resumo: | The development of nanostructured materials has provided better control of the release and targeting of active substances to the treatment site, minimizing adverse effects, in addition to contributing to increased therapeutic efficacy. In this sense, these carriers are an alternative for the development of products administered by vaginal route because the pharmaceutical forms commonly used promote inadequate distribution and penetration of drugs, in addition to the reduced time spent on site. Therefore, this study aimed to develop vaginal suppositories containing dried products prepared from polymeric nanoparticle suspensions containing tioconazole, an antifungal used to treat vulvovaginitis. Suspensions of polymeric nanospheres and nanocapsules containing tioconazole (3 mg / ml) were prepared and evaluated for average particle diameter (166-203 nm) polydispersion index (less than 0.20), negative zeta potential (6 - 10 mV), pH (weakly acidic), drug content (value close to the theoretical) and encapsulation efficiency (approximately 100%), which were adequate and stable over the period of 30 days. After the suspensions were subjected to spray drying to obtain the solid intermediates, which were characterized in relation to the weight yield of resuspending in water content profile of particle size distribution, drug content, humidity and morphology. Regarding these characteristics, the results were satisfactory: yield weight, approximately 60%, drug content close to the theoretical value (21 mg / g), resuspending ratio close to unity and maintenance of submicrometric particle size. These characteristics have remained after 30 days of storage at room temperature, only dried products containing the nanospheres. Subsequently, the dried products were incorporated into a gelatin-glycerin base to obtain vaginal suppositories. All formulations had surface characteristics and homogeneous dimensions; drug content close to the theoretical concentration (23 mg / suppository); average weight between 4.51 and 4.57 g; content uniformity and disintegration time less than 60 minutes. Suppositories consisting of the nanospheres enabled greater control of the release of tioconazole compared with suppositories containing the drug not associated. Thus, the formulations proposed in this work may constitute an alternative for the administration by vaginal route tioconazole, better acceptability compared to the existing dosage forms (creams, gels) enabling, by definition, a greater therapeutic effect of the drug in order the advantages that nanotechnology presents. |
id |
UFSM_ebc13505c93a6b171951f5d8d31ee823 |
---|---|
oai_identifier_str |
oai:repositorio.ufsm.br:1/17533 |
network_acronym_str |
UFSM |
network_name_str |
Manancial - Repositório Digital da UFSM |
repository_id_str |
|
spelling |
Desenvolvimento tecnológico de supositórios vaginais contendo nanopartículas poliméricas de tioconazolTechnological development of vaginal suppositories containing polymeric nanoparticles of tioconazoleNanopartículas poliméricasTioconazolProdutos sólidosSupositórios vaginaisSpray-dryingPolymeric nanoparticlesNanospheresDry productsVaginal suppositoriesCNPQ::CIENCIAS DA SAUDE::FARMACIAThe development of nanostructured materials has provided better control of the release and targeting of active substances to the treatment site, minimizing adverse effects, in addition to contributing to increased therapeutic efficacy. In this sense, these carriers are an alternative for the development of products administered by vaginal route because the pharmaceutical forms commonly used promote inadequate distribution and penetration of drugs, in addition to the reduced time spent on site. Therefore, this study aimed to develop vaginal suppositories containing dried products prepared from polymeric nanoparticle suspensions containing tioconazole, an antifungal used to treat vulvovaginitis. Suspensions of polymeric nanospheres and nanocapsules containing tioconazole (3 mg / ml) were prepared and evaluated for average particle diameter (166-203 nm) polydispersion index (less than 0.20), negative zeta potential (6 - 10 mV), pH (weakly acidic), drug content (value close to the theoretical) and encapsulation efficiency (approximately 100%), which were adequate and stable over the period of 30 days. After the suspensions were subjected to spray drying to obtain the solid intermediates, which were characterized in relation to the weight yield of resuspending in water content profile of particle size distribution, drug content, humidity and morphology. Regarding these characteristics, the results were satisfactory: yield weight, approximately 60%, drug content close to the theoretical value (21 mg / g), resuspending ratio close to unity and maintenance of submicrometric particle size. These characteristics have remained after 30 days of storage at room temperature, only dried products containing the nanospheres. Subsequently, the dried products were incorporated into a gelatin-glycerin base to obtain vaginal suppositories. All formulations had surface characteristics and homogeneous dimensions; drug content close to the theoretical concentration (23 mg / suppository); average weight between 4.51 and 4.57 g; content uniformity and disintegration time less than 60 minutes. Suppositories consisting of the nanospheres enabled greater control of the release of tioconazole compared with suppositories containing the drug not associated. Thus, the formulations proposed in this work may constitute an alternative for the administration by vaginal route tioconazole, better acceptability compared to the existing dosage forms (creams, gels) enabling, by definition, a greater therapeutic effect of the drug in order the advantages that nanotechnology presents.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPESO desenvolvimento de sistemas nanoestruturados tem proporcionado melhor controle da liberação e o direcionamento de substâncias ativas ao local terapêutico, minimizando, assim, efeitos adversos, além de contribuir para o aumento da eficácia terapêutica. Neste sentido, esses carreadores constituem uma alternativa para o desenvolvimento de produtos administrados pela via vaginal, pois as formas farmacêuticas comumente utilizadas promovem distribuição e penetração inadequadas dos fármacos, além do reduzido tempo de permanência no local. Com isso, este trabalho teve por objetivo desenvolver supositórios vaginais contendo produtos secos preparados a partir de suspensões de nanopartículas poliméricas contendo tioconazol, um antifúngico utilizado no tratamento de vulvovaginites. As suspensões de nanoesferas e nanocápsulas poliméricas contendo tioconazol (3 mg/mL) foram preparadas pela técnica da nanoprecipitação e avaliadas quanto ao diâmetro médio de partículas (166 – 203 nm), índice de polidispersão (inferior a 0,20), potencial zeta negativo (6 – 10 mV), pH (fracamente ácido), teor de fármaco (próximo ao teórico) e eficiência de encapsulamento (aproximadamente 100%), as quais foram adequadas e estáveis durante o período de 30 dias sob condições de temperatura ambiente. Após a preparação, as suspensões foram submetidas à secagem por aspersão para a obtenção dos produtos sólidos intermediários, os quais foram caracterizados em relação ao rendimento ponderal, índice de ressuspensão em água, perfil de distribuição de tamanho de partículas, teor de fármaco, umidade e morfologia. Quanto a essas características, os resultados foram satisfatórios: rendimento ponderal de, aproximadamente, 60%, conteúdo de fármaco próximo do valor teórico (21 mg/g), índice de ressuspensão próximo a unidade e recuperação do tamanho submicrométrico das partículas. Essas características mantiveram-se, após 30 dias de armazenamento a temperatura ambiente, somente para os produtos secos contendo as nanoesferas. Posteriormente, os produtos secos foram incorporados em uma base de gelatina-glicerina a fim de obter supositórios vaginais. Todas as formulações apresentaram características de superfície e de dimensões homogêneas; teor de fármaco próximo da concentração teórica (23 mg/supositório); peso médio entre 4,51 e 4,57 g; uniformidade de conteúdo e tempo de desintegração inferior a 60 minutos. Os supositórios constituídos pelas nanoesferas possibilitaram um maior controle da liberação do tioconazol em comparação aos supositórios contendo o fármaco não associado. Dessa forma, as formulações propostas neste trabalho poderão constituir uma alternativa para a administração do tioconazol pela via vaginal, de melhor aceitabilidade face às formas farmacêuticas já existentes (cremes, géis) possibilitando, por hipótese, um maior efeito terapêutico do fármaco, tendo em vista as vantagens que a nanotecnologia apresenta.Universidade Federal de Santa MariaBrasilFarmáciaUFSMPrograma de Pós-Graduação em Ciências FarmacêuticasCentro de Ciências da SaúdeSilva, Cristiane de Bona dahttp://lattes.cnpq.br/6029111646602279Ourique, Aline Ferreirahttp://lattes.cnpq.br/7478810804464054Canto, Gizele Scotti dohttp://lattes.cnpq.br/2076175621657265Cossetin, Luciana Filippin2019-07-22T21:14:01Z2019-07-22T21:14:01Z2015-08-14info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfhttp://repositorio.ufsm.br/handle/1/17533porAttribution-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:UFSM2022-10-07T18:26:44Zoai:repositorio.ufsm.br:1/17533Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufsm.br/ONGhttps://repositorio.ufsm.br/oai/requestatendimento.sib@ufsm.br||tedebc@gmail.comopendoar:2022-10-07T18:26:44Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM)false |
dc.title.none.fl_str_mv |
Desenvolvimento tecnológico de supositórios vaginais contendo nanopartículas poliméricas de tioconazol Technological development of vaginal suppositories containing polymeric nanoparticles of tioconazole |
title |
Desenvolvimento tecnológico de supositórios vaginais contendo nanopartículas poliméricas de tioconazol |
spellingShingle |
Desenvolvimento tecnológico de supositórios vaginais contendo nanopartículas poliméricas de tioconazol Cossetin, Luciana Filippin Nanopartículas poliméricas Tioconazol Produtos sólidos Supositórios vaginais Spray-drying Polymeric nanoparticles Nanospheres Dry products Vaginal suppositories CNPQ::CIENCIAS DA SAUDE::FARMACIA |
title_short |
Desenvolvimento tecnológico de supositórios vaginais contendo nanopartículas poliméricas de tioconazol |
title_full |
Desenvolvimento tecnológico de supositórios vaginais contendo nanopartículas poliméricas de tioconazol |
title_fullStr |
Desenvolvimento tecnológico de supositórios vaginais contendo nanopartículas poliméricas de tioconazol |
title_full_unstemmed |
Desenvolvimento tecnológico de supositórios vaginais contendo nanopartículas poliméricas de tioconazol |
title_sort |
Desenvolvimento tecnológico de supositórios vaginais contendo nanopartículas poliméricas de tioconazol |
author |
Cossetin, Luciana Filippin |
author_facet |
Cossetin, Luciana Filippin |
author_role |
author |
dc.contributor.none.fl_str_mv |
Silva, Cristiane de Bona da http://lattes.cnpq.br/6029111646602279 Ourique, Aline Ferreira http://lattes.cnpq.br/7478810804464054 Canto, Gizele Scotti do http://lattes.cnpq.br/2076175621657265 |
dc.contributor.author.fl_str_mv |
Cossetin, Luciana Filippin |
dc.subject.por.fl_str_mv |
Nanopartículas poliméricas Tioconazol Produtos sólidos Supositórios vaginais Spray-drying Polymeric nanoparticles Nanospheres Dry products Vaginal suppositories CNPQ::CIENCIAS DA SAUDE::FARMACIA |
topic |
Nanopartículas poliméricas Tioconazol Produtos sólidos Supositórios vaginais Spray-drying Polymeric nanoparticles Nanospheres Dry products Vaginal suppositories CNPQ::CIENCIAS DA SAUDE::FARMACIA |
description |
The development of nanostructured materials has provided better control of the release and targeting of active substances to the treatment site, minimizing adverse effects, in addition to contributing to increased therapeutic efficacy. In this sense, these carriers are an alternative for the development of products administered by vaginal route because the pharmaceutical forms commonly used promote inadequate distribution and penetration of drugs, in addition to the reduced time spent on site. Therefore, this study aimed to develop vaginal suppositories containing dried products prepared from polymeric nanoparticle suspensions containing tioconazole, an antifungal used to treat vulvovaginitis. Suspensions of polymeric nanospheres and nanocapsules containing tioconazole (3 mg / ml) were prepared and evaluated for average particle diameter (166-203 nm) polydispersion index (less than 0.20), negative zeta potential (6 - 10 mV), pH (weakly acidic), drug content (value close to the theoretical) and encapsulation efficiency (approximately 100%), which were adequate and stable over the period of 30 days. After the suspensions were subjected to spray drying to obtain the solid intermediates, which were characterized in relation to the weight yield of resuspending in water content profile of particle size distribution, drug content, humidity and morphology. Regarding these characteristics, the results were satisfactory: yield weight, approximately 60%, drug content close to the theoretical value (21 mg / g), resuspending ratio close to unity and maintenance of submicrometric particle size. These characteristics have remained after 30 days of storage at room temperature, only dried products containing the nanospheres. Subsequently, the dried products were incorporated into a gelatin-glycerin base to obtain vaginal suppositories. All formulations had surface characteristics and homogeneous dimensions; drug content close to the theoretical concentration (23 mg / suppository); average weight between 4.51 and 4.57 g; content uniformity and disintegration time less than 60 minutes. Suppositories consisting of the nanospheres enabled greater control of the release of tioconazole compared with suppositories containing the drug not associated. Thus, the formulations proposed in this work may constitute an alternative for the administration by vaginal route tioconazole, better acceptability compared to the existing dosage forms (creams, gels) enabling, by definition, a greater therapeutic effect of the drug in order the advantages that nanotechnology presents. |
publishDate |
2015 |
dc.date.none.fl_str_mv |
2015-08-14 2019-07-22T21:14:01Z 2019-07-22T21:14:01Z |
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/1/17533 |
url |
http://repositorio.ufsm.br/handle/1/17533 |
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_ |
1805922070489464832 |