Secagem por aspersão de nanocápsulas de núcleo lipídico contendo tretinoína: desenvolvimento e incorporação em hidrogéis

Detalhes bibliográficos
Autor(a) principal: Marchiori, Marila Crivellaro Lay
Data de Publicação: 2010
Tipo de documento: Dissertação
Idioma: por
Título da fonte: Manancial - Repositório Digital da UFSM
Texto Completo: http://repositorio.ufsm.br/handle/1/5940
Resumo: The aim of this work was to study the ability of lipid-core polymeric nanocapsules to protect tretinoin against UV degradation, even after their conversion to spray-dried powders and also to evaluate the feasibility of using these spray-dried powders in the preparation of semisolid dermatological nanomedicines. Spray-dried tretinoin-loaded lipid core nanocapsules (SD-TTN-NC) were prepared using lactose as drying adjuvant. In order to study the effect of the polymeric layer, spray-dried powders were also prepared using a nanoemulsion (SD-TTN-NE). The process yields were between 30 and 40 %. SD-TTN-NE showed lower encapsulation efficiency (88.74 ± 0.65%) compared to SD-TTN-NC (94.22 ± 2.01%). After aqueous redispersion of the spray-dried powders their supernatants showed the presence of nanostructures with mean size close to the original suspension Similar photodegradation half-life times were showed for tretinoin loaded in lipid-core nanocapsules (118 ± 12 min) or in the respective spray-dried powders (118 ± 27 min). Based in our results, the powders can be suggested as intermediate products in the development of nanomedicines. Two approaches were evaluated in the development of hydrogels: a) dispersing Carbopol Ultrez 10® in an aqueous redispersion of the SD-TTN-NC (method 1) or b) by the direct incorporation of the SD-TTN-NC in a hydrogel previously formed (method 2). Hydrogels were also prepared using original nanocapsule suspensions. All semisolid formulations presented drug content close to theoretical value, adequate pH values and pseudo-plastic behavior. The parallel plate technique demonstrated that hydrogels prepared by method 1 has lower spreadability (1.61 ± 0.13 mm2.g-1) than that prepared by method 2 (2.17 ± 0.05 mm2.g-1). However, both formulations showed worst spreadability factor than hydrogels prepared from nanoparticle suspensions, indicating that the presence of lactose led to a decrease in the spreadability of the formulations. Hydrogels prepared with the spray-dried powder showed higher yield stress compared to that prepared with the nanocapsule suspensions. Regarding the consistency index, all hydrogels presented similar values, excepting the formulation prepared with blank nanocapsules. The photodegratadion profiles of hydrogels containing SD-TTN-NC were similar to hydrogel prepared with the original suspension. So, spray-dried powders were feasible materials to be use as intermediate products in the development of hydrogels intended for cutaneous application without losing their ability to increase the photostability of tretinoin.
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spelling Secagem por aspersão de nanocápsulas de núcleo lipídico contendo tretinoína: desenvolvimento e incorporação em hidrogéisDry powders containing tretinoin-loaded lipid-core polymeric nanocapsules: development and incorporation into hydrogelsTretinoínaNanocápsulasHidrogelSecagem por aspersãoTretinoinLipid core nanocapsulesHydrogelPhodegradationSpray-dryerCNPQ::CIENCIAS DA SAUDE::FARMACIAThe aim of this work was to study the ability of lipid-core polymeric nanocapsules to protect tretinoin against UV degradation, even after their conversion to spray-dried powders and also to evaluate the feasibility of using these spray-dried powders in the preparation of semisolid dermatological nanomedicines. Spray-dried tretinoin-loaded lipid core nanocapsules (SD-TTN-NC) were prepared using lactose as drying adjuvant. In order to study the effect of the polymeric layer, spray-dried powders were also prepared using a nanoemulsion (SD-TTN-NE). The process yields were between 30 and 40 %. SD-TTN-NE showed lower encapsulation efficiency (88.74 ± 0.65%) compared to SD-TTN-NC (94.22 ± 2.01%). After aqueous redispersion of the spray-dried powders their supernatants showed the presence of nanostructures with mean size close to the original suspension Similar photodegradation half-life times were showed for tretinoin loaded in lipid-core nanocapsules (118 ± 12 min) or in the respective spray-dried powders (118 ± 27 min). Based in our results, the powders can be suggested as intermediate products in the development of nanomedicines. Two approaches were evaluated in the development of hydrogels: a) dispersing Carbopol Ultrez 10® in an aqueous redispersion of the SD-TTN-NC (method 1) or b) by the direct incorporation of the SD-TTN-NC in a hydrogel previously formed (method 2). Hydrogels were also prepared using original nanocapsule suspensions. All semisolid formulations presented drug content close to theoretical value, adequate pH values and pseudo-plastic behavior. The parallel plate technique demonstrated that hydrogels prepared by method 1 has lower spreadability (1.61 ± 0.13 mm2.g-1) than that prepared by method 2 (2.17 ± 0.05 mm2.g-1). However, both formulations showed worst spreadability factor than hydrogels prepared from nanoparticle suspensions, indicating that the presence of lactose led to a decrease in the spreadability of the formulations. Hydrogels prepared with the spray-dried powder showed higher yield stress compared to that prepared with the nanocapsule suspensions. Regarding the consistency index, all hydrogels presented similar values, excepting the formulation prepared with blank nanocapsules. The photodegratadion profiles of hydrogels containing SD-TTN-NC were similar to hydrogel prepared with the original suspension. So, spray-dried powders were feasible materials to be use as intermediate products in the development of hydrogels intended for cutaneous application without losing their ability to increase the photostability of tretinoin.O objetivo deste tabalho foi avaliar a capacidade das nanocápsulas de núcleo lipídico em manter a sua proteção frente à fotodegradação da tretinoína, após a sua conversão em materiais pulverulentos, através da técnica de secagem por aspersão (SD-TTN-NC). Este processo foi realizado empregando a lactose como adjuvante de secagem. Posteriormente, foi verificada a aplicabilidade destes pós na preparação de formulações dermatológicas. Para avaliar a influência da presença do polímero na interface óleo/água foi também realizada a secagem por aspersão de uma nanoemulsão contendo tretinoína (SD-TTN-NE). Ambos os pós (SD-TTN-NC e SD-TTN-NE) mostraram rendimento em torno de 30-40% e adequada recuperação das nanoestruturas após redispersão aquosa. SD-TTN-NE mostrou menor eficiência de encapsulação do fármaco (88,74 ± 0,65%) do que SD-TTN-NC (94,22 ± 2,01%), mostrando que a parede polimérica exerce um efeito positivo e, por isso, esta formulação foi selecionada para prosseguir com os estudos de fotoestabilidade. O ensaio de fotodegradação do pó redisperso em água mostrou que as nanocápsulas de núcleo lipídico reproduziram a fotoestabilidade demonstrada pela suspensão coloidal original (118 ± 27 min e 118 ± 12 min, respectivamente). Com base nestes resultados, ficou evidente que SD-TTN-NC poderia ser empregado como forma intermediária na preparação de hidrogéis. Neste sentido, foram propostas duas técnicas de preparação: a) dispersando o Carbopol Ultrez 10® na redispersão aquosa dos pós (método 1) ou b) adicionando o pó diretamente no gel previamente preparado (método 2). Além destes, foram preparados hidrogéis empregando as suspensões aquosas de nanocápsulas de núcleo lipídico. Todas as formulações apresentaram teor de tretinoína próximo a 0,5 mg/g, pH adequado à aplicação cutânea e comportamento pseudo-plástico. Através do método das placas paralelas, foi demonstrado que os hidrogéis preparados pelo método 1 tem menor espalhabilidade (1,61 ± 0,13 mm2/g) do que os preparados pelo método 2 (2,17 ± 0,05 mm2/g). De maneira geral, as amostras preparadas a partir dos pós foram as que tiveram menor espalhabilidade, independente do método empregado, indicando que a presença de lactose influencia nesta característica. Quanto à reologia, os maiores valores de rendimento foram apresentados pelas formulações que apresentaram menor espalhabilidade. O índice de consistência foi estatisticamente igual para todas as formulações, exceto para o hidrogel preparado com a suspensão coloidal branca (sem fármaco). Quanto à fotoestabilidade, os hidrogéis propostos apresentaram comportamento tão eficiente quanto à formulação obtida a partir da suspensão original de nanocápsulas de núcleo lipídico. Os pós secos por aspersão mostraram-se como importantes produtos intermediarios no desenvolvimento de hidrogéis para aplicação cutânea de tretinoína.Universidade Federal de Santa MariaBRFarmáciaUFSMPrograma de Pós-Graduação em Ciências FarmacêuticasBeck, Ruy Carlos Ruverhttp://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4705330E7Guerreiro, Irene Clemes Kulkamphttp://lattes.cnpq.br/9385103078887175Silva, Cristiane de Bona dahttp://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4791812Z5Marchiori, Marila Crivellaro Lay2013-05-212013-05-212010-12-07info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfapplication/pdfMARCHIORI, Marila Crivellaro Lay. DRY POWDERS CONTAINING TRETINOIN-LOADED LIPID-CORE POLYMERIC NANOCAPSULES: DEVELOPMENT AND INCORPORATION INTO HYDROGELS. 2010. 98 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2010.http://repositorio.ufsm.br/handle/1/5940porinfo:eu-repo/semantics/openAccessreponame:Manancial - Repositório Digital da UFSMinstname:Universidade Federal de Santa Maria (UFSM)instacron:UFSM2022-10-17T12:59:41Zoai:repositorio.ufsm.br:1/5940Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufsm.br/ONGhttps://repositorio.ufsm.br/oai/requestatendimento.sib@ufsm.br||tedebc@gmail.comopendoar:2022-10-17T12:59:41Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM)false
dc.title.none.fl_str_mv Secagem por aspersão de nanocápsulas de núcleo lipídico contendo tretinoína: desenvolvimento e incorporação em hidrogéis
Dry powders containing tretinoin-loaded lipid-core polymeric nanocapsules: development and incorporation into hydrogels
title Secagem por aspersão de nanocápsulas de núcleo lipídico contendo tretinoína: desenvolvimento e incorporação em hidrogéis
spellingShingle Secagem por aspersão de nanocápsulas de núcleo lipídico contendo tretinoína: desenvolvimento e incorporação em hidrogéis
Marchiori, Marila Crivellaro Lay
Tretinoína
Nanocápsulas
Hidrogel
Secagem por aspersão
Tretinoin
Lipid core nanocapsules
Hydrogel
Phodegradation
Spray-dryer
CNPQ::CIENCIAS DA SAUDE::FARMACIA
title_short Secagem por aspersão de nanocápsulas de núcleo lipídico contendo tretinoína: desenvolvimento e incorporação em hidrogéis
title_full Secagem por aspersão de nanocápsulas de núcleo lipídico contendo tretinoína: desenvolvimento e incorporação em hidrogéis
title_fullStr Secagem por aspersão de nanocápsulas de núcleo lipídico contendo tretinoína: desenvolvimento e incorporação em hidrogéis
title_full_unstemmed Secagem por aspersão de nanocápsulas de núcleo lipídico contendo tretinoína: desenvolvimento e incorporação em hidrogéis
title_sort Secagem por aspersão de nanocápsulas de núcleo lipídico contendo tretinoína: desenvolvimento e incorporação em hidrogéis
author Marchiori, Marila Crivellaro Lay
author_facet Marchiori, Marila Crivellaro Lay
author_role author
dc.contributor.none.fl_str_mv Beck, Ruy Carlos Ruver
http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4705330E7
Guerreiro, Irene Clemes Kulkamp
http://lattes.cnpq.br/9385103078887175
Silva, Cristiane de Bona da
http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4791812Z5
dc.contributor.author.fl_str_mv Marchiori, Marila Crivellaro Lay
dc.subject.por.fl_str_mv Tretinoína
Nanocápsulas
Hidrogel
Secagem por aspersão
Tretinoin
Lipid core nanocapsules
Hydrogel
Phodegradation
Spray-dryer
CNPQ::CIENCIAS DA SAUDE::FARMACIA
topic Tretinoína
Nanocápsulas
Hidrogel
Secagem por aspersão
Tretinoin
Lipid core nanocapsules
Hydrogel
Phodegradation
Spray-dryer
CNPQ::CIENCIAS DA SAUDE::FARMACIA
description The aim of this work was to study the ability of lipid-core polymeric nanocapsules to protect tretinoin against UV degradation, even after their conversion to spray-dried powders and also to evaluate the feasibility of using these spray-dried powders in the preparation of semisolid dermatological nanomedicines. Spray-dried tretinoin-loaded lipid core nanocapsules (SD-TTN-NC) were prepared using lactose as drying adjuvant. In order to study the effect of the polymeric layer, spray-dried powders were also prepared using a nanoemulsion (SD-TTN-NE). The process yields were between 30 and 40 %. SD-TTN-NE showed lower encapsulation efficiency (88.74 ± 0.65%) compared to SD-TTN-NC (94.22 ± 2.01%). After aqueous redispersion of the spray-dried powders their supernatants showed the presence of nanostructures with mean size close to the original suspension Similar photodegradation half-life times were showed for tretinoin loaded in lipid-core nanocapsules (118 ± 12 min) or in the respective spray-dried powders (118 ± 27 min). Based in our results, the powders can be suggested as intermediate products in the development of nanomedicines. Two approaches were evaluated in the development of hydrogels: a) dispersing Carbopol Ultrez 10® in an aqueous redispersion of the SD-TTN-NC (method 1) or b) by the direct incorporation of the SD-TTN-NC in a hydrogel previously formed (method 2). Hydrogels were also prepared using original nanocapsule suspensions. All semisolid formulations presented drug content close to theoretical value, adequate pH values and pseudo-plastic behavior. The parallel plate technique demonstrated that hydrogels prepared by method 1 has lower spreadability (1.61 ± 0.13 mm2.g-1) than that prepared by method 2 (2.17 ± 0.05 mm2.g-1). However, both formulations showed worst spreadability factor than hydrogels prepared from nanoparticle suspensions, indicating that the presence of lactose led to a decrease in the spreadability of the formulations. Hydrogels prepared with the spray-dried powder showed higher yield stress compared to that prepared with the nanocapsule suspensions. Regarding the consistency index, all hydrogels presented similar values, excepting the formulation prepared with blank nanocapsules. The photodegratadion profiles of hydrogels containing SD-TTN-NC were similar to hydrogel prepared with the original suspension. So, spray-dried powders were feasible materials to be use as intermediate products in the development of hydrogels intended for cutaneous application without losing their ability to increase the photostability of tretinoin.
publishDate 2010
dc.date.none.fl_str_mv 2010-12-07
2013-05-21
2013-05-21
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 MARCHIORI, Marila Crivellaro Lay. DRY POWDERS CONTAINING TRETINOIN-LOADED LIPID-CORE POLYMERIC NANOCAPSULES: DEVELOPMENT AND INCORPORATION INTO HYDROGELS. 2010. 98 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2010.
http://repositorio.ufsm.br/handle/1/5940
identifier_str_mv MARCHIORI, Marila Crivellaro Lay. DRY POWDERS CONTAINING TRETINOIN-LOADED LIPID-CORE POLYMERIC NANOCAPSULES: DEVELOPMENT AND INCORPORATION INTO HYDROGELS. 2010. 98 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2010.
url http://repositorio.ufsm.br/handle/1/5940
dc.language.iso.fl_str_mv por
language por
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Universidade Federal de Santa Maria
BR
Farmácia
UFSM
Programa de Pós-Graduação em Ciências Farmacêuticas
publisher.none.fl_str_mv Universidade Federal de Santa Maria
BR
Farmácia
UFSM
Programa de Pós-Graduação em Ciências Farmacêuticas
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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