FORMULAÇÕES SEMISSÓLIDAS CONTENDO NANOCÁPSULAS DE ADAPALENO: DETERMINAÇÃO DA ESTABILIDADE, AVALIAÇÃO DA LIBERAÇÃO IN VITRO E ENSAIOS UTILIZANDO BIOMETRIA CUTÂNEA

Detalhes bibliográficos
Autor(a) principal: Farias, Gabriela D'Avila
Data de Publicação: 2011
Tipo de documento: Dissertação
Idioma: por
Título da fonte: Repositório Institucional Universidade Franciscana
Texto Completo: http://www.tede.universidadefranciscana.edu.br:8080/handle/UFN-BDTD/495
Resumo: Acne vulgaris is a genetic hormone disease, located in the hair follicle. Adapalene a third-generation retinoid, and it is a topical alternative for acne treatment, but may have some adverse effects, irritation and dryness of the skin are the most common. Due to this, and knowing the nanocarriers potential, the object of this study was determine the physicochemical stability of semisolid formulations containing adapalene-loaded nanocapsules (NC) incorporated in Aristoflex AVL®, evaluate the release profiles in semisolid formulations containing nanocapsules containing adapalene incorporated in Carbopol 940® and verify the safety of the formulation in vivo by noninvasive biophysical analysis. For the determination of the stability, samples were subjected to freeze-thaw cycle, completing a cycle of 21 days. The in vitro release studies were performed comparing the drug-loaded NC (GCNCA) with the gel containing adapalene in its free form (GCA). For the skin bioengineer techniques, twenty healthy volunteers were selected. Each week were performed biometric skin tests including stratum corneum water content (hydration), pH, color, erythema and transepidermal water loss for 63 days. In stability studies, we observed that the average particle size, polydispersity and zeta potential of cream gel containing NC without adapalene (CGNC) and cream gel containing adapaleneloaded NC (CGNCA) showed no change after being subjected to the freeze-thaw cycle. Semisolid formulations showed non-Newtonian flow and pseudoplastic behavior during the study period. The initial adapalene content in CGNCA did not change compared with the result obtained at the end of the experiment. However, for the cream gel containing free adapalene (CGA), there was a reduction in the drug concentration, whereas the initial content decreased to below 90% after 21 days of analysis. According to release studies, we can observe that the GCNCA showed total concentration and release rate less than the GCA, which demonstrates the ability of nanoparticles to control the drug release. According to the results observed for the non-invasive method in relation to the determination of melanin content, there was a decrease in this parameter during the experiment for both formulations. The GCNCA did not cause erythema, configuring security in the use of the formulation. However, the GCA increased the index of erythema of the skin of volunteers. We observed an increase in transepidermal water loss to the GCA while in GCNCA there is a reduction of this parameter. The results obtained for skin hydration, there was a more pronounced reduction of the values of the stratum corneum water content in the treated areas with GCA. Thus, it was evident that the polymeric nanocapsules are able to decrease transepidermal water loss, favoring the skin hydration degree and keeping the stratum corneum integrity.
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spelling Alves, Marta PalmaBeck, Ruy Carlos ReverBulhões, Luis Otávio de SousaFarias, Gabriela D'Avila2018-08-16T13:49:23Z2011-04-19Farias, Gabriela D'Avila. FORMULAÇÕES SEMISSÓLIDAS CONTENDO NANOCÁPSULAS DE ADAPALENO: DETERMINAÇÃO DA ESTABILIDADE, AVALIAÇÃO DA LIBERAÇÃO IN VITRO E ENSAIOS UTILIZANDO BIOMETRIA CUTÂNEA. 2011. 108f. Dissertação( Programa de Pós-Graduação em Nanociências) - Centro Universitário Franciscano, Santa Maria - RS .http://www.tede.universidadefranciscana.edu.br:8080/handle/UFN-BDTD/495Acne vulgaris is a genetic hormone disease, located in the hair follicle. Adapalene a third-generation retinoid, and it is a topical alternative for acne treatment, but may have some adverse effects, irritation and dryness of the skin are the most common. Due to this, and knowing the nanocarriers potential, the object of this study was determine the physicochemical stability of semisolid formulations containing adapalene-loaded nanocapsules (NC) incorporated in Aristoflex AVL®, evaluate the release profiles in semisolid formulations containing nanocapsules containing adapalene incorporated in Carbopol 940® and verify the safety of the formulation in vivo by noninvasive biophysical analysis. For the determination of the stability, samples were subjected to freeze-thaw cycle, completing a cycle of 21 days. The in vitro release studies were performed comparing the drug-loaded NC (GCNCA) with the gel containing adapalene in its free form (GCA). For the skin bioengineer techniques, twenty healthy volunteers were selected. Each week were performed biometric skin tests including stratum corneum water content (hydration), pH, color, erythema and transepidermal water loss for 63 days. In stability studies, we observed that the average particle size, polydispersity and zeta potential of cream gel containing NC without adapalene (CGNC) and cream gel containing adapaleneloaded NC (CGNCA) showed no change after being subjected to the freeze-thaw cycle. Semisolid formulations showed non-Newtonian flow and pseudoplastic behavior during the study period. The initial adapalene content in CGNCA did not change compared with the result obtained at the end of the experiment. However, for the cream gel containing free adapalene (CGA), there was a reduction in the drug concentration, whereas the initial content decreased to below 90% after 21 days of analysis. According to release studies, we can observe that the GCNCA showed total concentration and release rate less than the GCA, which demonstrates the ability of nanoparticles to control the drug release. According to the results observed for the non-invasive method in relation to the determination of melanin content, there was a decrease in this parameter during the experiment for both formulations. The GCNCA did not cause erythema, configuring security in the use of the formulation. However, the GCA increased the index of erythema of the skin of volunteers. We observed an increase in transepidermal water loss to the GCA while in GCNCA there is a reduction of this parameter. The results obtained for skin hydration, there was a more pronounced reduction of the values of the stratum corneum water content in the treated areas with GCA. Thus, it was evident that the polymeric nanocapsules are able to decrease transepidermal water loss, favoring the skin hydration degree and keeping the stratum corneum integrity.A acne vulgar é uma doença genética hormonal, de localização pilo-sebácea. O adapaleno, retinóide de terceira geração, é uma alternativa tópica para o tratamento da acne, podendo apresentar alguns efeitos indesejáveis, sendo a irritação e o ressecamento da pele os mais comuns. Em vista disso, e conhecendo as potencialidades dos nanocarreadores, o presente trabalho tem como objetivo determinar a estabilidade físico-química de formulações semissólidas contendo adapaleno nanoestruturado incorporado em Aristoflex AVL®, avaliar os perfis de liberação em formulações semissólidas contendo nanocápsulas (NC) de adapaleno incorporadas em Carbopol 940® e verificar a segurança do fármaco nanoencapsulado in vivo, através de análises biofísicas não invasivas. Para a determinação da estabilidade as amostras foram submetidas ao ciclo gelo-degelo, completando-se um ciclo de 21 dias. Os estudos de liberação in vitro foram realizados comparando-se as formulações contendo nanocápsulas de adapaleno (GCNCA) com o gel contendo o fármaco na forma livre (GCA). Para o ensaio utilizando biometria cutânea, foram selecionados vinte voluntários saudáveis. A cada semana foram realizados testes de bioengenharia cutânea, incluindo avaliação do conteúdo aquoso do estrato córneo (hidratação), pH, coloração, eritema e perda transepidérmica de água durante 63 dias. Nos estudos de estabilidade, observou-se que o diâmetro médio das partículas, índice de polidispersão e potencial zeta do creme gel contendo NC sem adapaleno (CGNC) e do creme gel contendo NC de adapaleno (CGNCA) não apresentaram alterações após serem submetidos ao ciclo gelodegelo. As formulações semissólidas independente da forma de dispersão do fármaco apresentaram fluxo não-newtoniano e comportamento pseudoplástico durante todo o período de análise. O teor inicial de adapaleno no CGNCA não sofreu alteração, quando comparado com o teor obtido no término do experimento. Entretanto, para o creme gel contendo adapaleno livre (CGA) houve uma redução na concentração de adapaleno, visto que o teor inicial decaiu para valores abaixo de 90% após 21 dias de análise. Com relação aos estudos de liberação, pode-se observar que o GCNCA apresentou concentração total e taxa de liberação menor do que o GCA, o que demonstra a capacidade das nanopartículas em controlar a liberação do fármaco. De acordo com os resultados observados para o ensaio de bioengenharia cutânea, com relação à determinação do conteúdo de melanina, verificouse uma redução deste parâmetro no decorrer do experimento para ambas as formulações. O GCNCA não causou eritema, configurando a segurança na utilização da formulação. Entretanto, o GCA aumentou, de maneira estatisticamente significativa, o índice de eritema da pele dos voluntários. Foi observado um aumento na perda transepidérmica de água para o GCA enquanto no GCNCA observa-se uma redução deste parâmetro. Nos resultados obtidos para hidratação cutânea, observou-se uma redução mais pronunciada dos valores do conteúdo aquoso do estrato córneo nas regiões tratadas com GCA. Desta forma, evidenciou-se que as nanocápsulas poliméricas são capazes de diminuir a perda transepidérmica de água, favorecendo o grau de hidratação cutânea e mantendo a integridade do estrato córneo.Submitted by MARCIA ROVADOSCHI (marciar@unifra.br) on 2018-08-16T13:49:23Z No. of bitstreams: 2 license_rdf: 0 bytes, checksum: d41d8cd98f00b204e9800998ecf8427e (MD5) Dissertacao_GabrielaD'AvilaFarias.pdf: 1690913 bytes, checksum: 045532806a12d78ce1324029cd8aedaf (MD5)Made available in DSpace on 2018-08-16T13:49:23Z (GMT). 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dc.title.por.fl_str_mv FORMULAÇÕES SEMISSÓLIDAS CONTENDO NANOCÁPSULAS DE ADAPALENO: DETERMINAÇÃO DA ESTABILIDADE, AVALIAÇÃO DA LIBERAÇÃO IN VITRO E ENSAIOS UTILIZANDO BIOMETRIA CUTÂNEA
title FORMULAÇÕES SEMISSÓLIDAS CONTENDO NANOCÁPSULAS DE ADAPALENO: DETERMINAÇÃO DA ESTABILIDADE, AVALIAÇÃO DA LIBERAÇÃO IN VITRO E ENSAIOS UTILIZANDO BIOMETRIA CUTÂNEA
spellingShingle FORMULAÇÕES SEMISSÓLIDAS CONTENDO NANOCÁPSULAS DE ADAPALENO: DETERMINAÇÃO DA ESTABILIDADE, AVALIAÇÃO DA LIBERAÇÃO IN VITRO E ENSAIOS UTILIZANDO BIOMETRIA CUTÂNEA
Farias, Gabriela D'Avila
adapaleno, nanocápsulas, formulações semissólidas, estabilidade, biometria cutânea.
adapalene, nanocapsules, semisolid formulations, stability and non-invasive method.
Biociências e Nanomateriais
title_short FORMULAÇÕES SEMISSÓLIDAS CONTENDO NANOCÁPSULAS DE ADAPALENO: DETERMINAÇÃO DA ESTABILIDADE, AVALIAÇÃO DA LIBERAÇÃO IN VITRO E ENSAIOS UTILIZANDO BIOMETRIA CUTÂNEA
title_full FORMULAÇÕES SEMISSÓLIDAS CONTENDO NANOCÁPSULAS DE ADAPALENO: DETERMINAÇÃO DA ESTABILIDADE, AVALIAÇÃO DA LIBERAÇÃO IN VITRO E ENSAIOS UTILIZANDO BIOMETRIA CUTÂNEA
title_fullStr FORMULAÇÕES SEMISSÓLIDAS CONTENDO NANOCÁPSULAS DE ADAPALENO: DETERMINAÇÃO DA ESTABILIDADE, AVALIAÇÃO DA LIBERAÇÃO IN VITRO E ENSAIOS UTILIZANDO BIOMETRIA CUTÂNEA
title_full_unstemmed FORMULAÇÕES SEMISSÓLIDAS CONTENDO NANOCÁPSULAS DE ADAPALENO: DETERMINAÇÃO DA ESTABILIDADE, AVALIAÇÃO DA LIBERAÇÃO IN VITRO E ENSAIOS UTILIZANDO BIOMETRIA CUTÂNEA
title_sort FORMULAÇÕES SEMISSÓLIDAS CONTENDO NANOCÁPSULAS DE ADAPALENO: DETERMINAÇÃO DA ESTABILIDADE, AVALIAÇÃO DA LIBERAÇÃO IN VITRO E ENSAIOS UTILIZANDO BIOMETRIA CUTÂNEA
author Farias, Gabriela D'Avila
author_facet Farias, Gabriela D'Avila
author_role author
dc.contributor.advisor1.fl_str_mv Alves, Marta Palma
dc.contributor.referee1.fl_str_mv Beck, Ruy Carlos Rever
dc.contributor.referee2.fl_str_mv Bulhões, Luis Otávio de Sousa
dc.contributor.author.fl_str_mv Farias, Gabriela D'Avila
contributor_str_mv Alves, Marta Palma
Beck, Ruy Carlos Rever
Bulhões, Luis Otávio de Sousa
dc.subject.por.fl_str_mv adapaleno, nanocápsulas, formulações semissólidas, estabilidade, biometria cutânea.
topic adapaleno, nanocápsulas, formulações semissólidas, estabilidade, biometria cutânea.
adapalene, nanocapsules, semisolid formulations, stability and non-invasive method.
Biociências e Nanomateriais
dc.subject.eng.fl_str_mv adapalene, nanocapsules, semisolid formulations, stability and non-invasive method.
dc.subject.cnpq.fl_str_mv Biociências e Nanomateriais
description Acne vulgaris is a genetic hormone disease, located in the hair follicle. Adapalene a third-generation retinoid, and it is a topical alternative for acne treatment, but may have some adverse effects, irritation and dryness of the skin are the most common. Due to this, and knowing the nanocarriers potential, the object of this study was determine the physicochemical stability of semisolid formulations containing adapalene-loaded nanocapsules (NC) incorporated in Aristoflex AVL®, evaluate the release profiles in semisolid formulations containing nanocapsules containing adapalene incorporated in Carbopol 940® and verify the safety of the formulation in vivo by noninvasive biophysical analysis. For the determination of the stability, samples were subjected to freeze-thaw cycle, completing a cycle of 21 days. The in vitro release studies were performed comparing the drug-loaded NC (GCNCA) with the gel containing adapalene in its free form (GCA). For the skin bioengineer techniques, twenty healthy volunteers were selected. Each week were performed biometric skin tests including stratum corneum water content (hydration), pH, color, erythema and transepidermal water loss for 63 days. In stability studies, we observed that the average particle size, polydispersity and zeta potential of cream gel containing NC without adapalene (CGNC) and cream gel containing adapaleneloaded NC (CGNCA) showed no change after being subjected to the freeze-thaw cycle. Semisolid formulations showed non-Newtonian flow and pseudoplastic behavior during the study period. The initial adapalene content in CGNCA did not change compared with the result obtained at the end of the experiment. However, for the cream gel containing free adapalene (CGA), there was a reduction in the drug concentration, whereas the initial content decreased to below 90% after 21 days of analysis. According to release studies, we can observe that the GCNCA showed total concentration and release rate less than the GCA, which demonstrates the ability of nanoparticles to control the drug release. According to the results observed for the non-invasive method in relation to the determination of melanin content, there was a decrease in this parameter during the experiment for both formulations. The GCNCA did not cause erythema, configuring security in the use of the formulation. However, the GCA increased the index of erythema of the skin of volunteers. We observed an increase in transepidermal water loss to the GCA while in GCNCA there is a reduction of this parameter. The results obtained for skin hydration, there was a more pronounced reduction of the values of the stratum corneum water content in the treated areas with GCA. Thus, it was evident that the polymeric nanocapsules are able to decrease transepidermal water loss, favoring the skin hydration degree and keeping the stratum corneum integrity.
publishDate 2011
dc.date.issued.fl_str_mv 2011-04-19
dc.date.accessioned.fl_str_mv 2018-08-16T13:49:23Z
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dc.identifier.citation.fl_str_mv Farias, Gabriela D'Avila. FORMULAÇÕES SEMISSÓLIDAS CONTENDO NANOCÁPSULAS DE ADAPALENO: DETERMINAÇÃO DA ESTABILIDADE, AVALIAÇÃO DA LIBERAÇÃO IN VITRO E ENSAIOS UTILIZANDO BIOMETRIA CUTÂNEA. 2011. 108f. Dissertação( Programa de Pós-Graduação em Nanociências) - Centro Universitário Franciscano, Santa Maria - RS .
dc.identifier.uri.fl_str_mv http://www.tede.universidadefranciscana.edu.br:8080/handle/UFN-BDTD/495
identifier_str_mv Farias, Gabriela D'Avila. FORMULAÇÕES SEMISSÓLIDAS CONTENDO NANOCÁPSULAS DE ADAPALENO: DETERMINAÇÃO DA ESTABILIDADE, AVALIAÇÃO DA LIBERAÇÃO IN VITRO E ENSAIOS UTILIZANDO BIOMETRIA CUTÂNEA. 2011. 108f. Dissertação( Programa de Pós-Graduação em Nanociências) - Centro Universitário Franciscano, Santa Maria - RS .
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