SUSPENSÕES E FORMULAÇÕES TÓPICAS CONTENDO NANOCÁPSULAS E MICROPARTÍCULAS DE CETOCONAZOL: AVALIAÇÃO DA ESTABILIDADE E ATIVIDADE ANTIMICROBIANA

Detalhes bibliográficos
Autor(a) principal: Pons Junior, Flábio da
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/500
Resumo: The fungal infections in humans occur in several ways, can this is superficial and systemic mycoses mycoses. The use of new antifungal made important progress in the treatment of different types of fungal infections. Among the drugs used to treat, there is ketoconazole, azole derivative, a synthetic molecule that acts by inhibiting biosynthesis of ergosterol molecule, exerting fungicidal. Treatment with ketoconazole requires frequent applications of the product, which causes skin irritation, the adherence to treatment. Initial studies have shown that drugs have nanocarrier improvement in selectivity, reducing side effects by modifying the release and increasing the effectiveness of the asset. This study aimed to characterize, evaluate the physical and chemical stability and antimicrobial activity of systems composed of nanoparticles or microparticles incorporated into formulations containing ketoconazole shampoo. All studies were carried out comparing ketoconazole as nanostructured and microstructured with the free form. The samples were stored under conditions of 25 ± 2 ° C, 4 ± 2 ° C and 40 ± 2 ° C and 75 ± 5% RH and exposed to UV light for 90 days and analyzed at 0, 7, 15, 30, 60 and 90 days in relation to the determination of pH, particle diameter, polydispersity index, zeta potential, rate of association and the drug dosing, antimicrobial activity and viscosity for the samples of shampoo. The average particle size for the nanocapsules was less than 370 nm, for microparticles less than 52 micrometers. All samples consist of the nanocarrier showed negative zeta potential. The values for the rate of association were 92.10% for the nanocapsules and 97.69% for the microparticles. Regarding the content of the suspensions and tested for stability, the samples comprising nanocapsules showed the loss of a smaller amount of assets (17.9% and 19.7%) in conditions of 25 ± 2 ° C and ± 4 2 ° C respectively. For formulations of shampoo made by nanocarrier systems, the same place, but with losses (9.3% and 13.6%) for the same conditions of suspension. In the analysis of antimicrobial activity, suspensions of nanocapsules had power of 98.15% and 100.25% of microparticles. Samples of shampoo were analyzed by microbiological assay sensitivity, which analyzed both qualitatively and showed that the samples have antifungal activity. The validation of analytical methodologies for the suspensions showed satisfactory results for all parameters. The results obtained, it can be concluded that the suspensions have demonstrated good stability, even when incorporated into a topical pharmaceutical vehicle, thus representing a better technological feasibility for the pharmaceutical area.
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spelling Alves, Marta PalmaAngeli , Valeria WeissMortari, Sergio RobertoPons Junior, Flábio da2018-08-16T14:17:32Z2011-08-30Pons Junior, Flábio da. SUSPENSÕES E FORMULAÇÕES TÓPICAS CONTENDO NANOCÁPSULAS E MICROPARTÍCULAS DE CETOCONAZOL: AVALIAÇÃO DA ESTABILIDADE E ATIVIDADE ANTIMICROBIANA. 2011. 100f. Dissertação( Programa de Pós-Graduação em Nanociências) - Centro Universitário Franciscano, Santa Maria -RS .http://www.tede.universidadefranciscana.edu.br:8080/handle/UFN-BDTD/500The fungal infections in humans occur in several ways, can this is superficial and systemic mycoses mycoses. The use of new antifungal made important progress in the treatment of different types of fungal infections. Among the drugs used to treat, there is ketoconazole, azole derivative, a synthetic molecule that acts by inhibiting biosynthesis of ergosterol molecule, exerting fungicidal. Treatment with ketoconazole requires frequent applications of the product, which causes skin irritation, the adherence to treatment. Initial studies have shown that drugs have nanocarrier improvement in selectivity, reducing side effects by modifying the release and increasing the effectiveness of the asset. This study aimed to characterize, evaluate the physical and chemical stability and antimicrobial activity of systems composed of nanoparticles or microparticles incorporated into formulations containing ketoconazole shampoo. All studies were carried out comparing ketoconazole as nanostructured and microstructured with the free form. The samples were stored under conditions of 25 ± 2 ° C, 4 ± 2 ° C and 40 ± 2 ° C and 75 ± 5% RH and exposed to UV light for 90 days and analyzed at 0, 7, 15, 30, 60 and 90 days in relation to the determination of pH, particle diameter, polydispersity index, zeta potential, rate of association and the drug dosing, antimicrobial activity and viscosity for the samples of shampoo. The average particle size for the nanocapsules was less than 370 nm, for microparticles less than 52 micrometers. All samples consist of the nanocarrier showed negative zeta potential. The values for the rate of association were 92.10% for the nanocapsules and 97.69% for the microparticles. Regarding the content of the suspensions and tested for stability, the samples comprising nanocapsules showed the loss of a smaller amount of assets (17.9% and 19.7%) in conditions of 25 ± 2 ° C and ± 4 2 ° C respectively. For formulations of shampoo made by nanocarrier systems, the same place, but with losses (9.3% and 13.6%) for the same conditions of suspension. In the analysis of antimicrobial activity, suspensions of nanocapsules had power of 98.15% and 100.25% of microparticles. Samples of shampoo were analyzed by microbiological assay sensitivity, which analyzed both qualitatively and showed that the samples have antifungal activity. The validation of analytical methodologies for the suspensions showed satisfactory results for all parameters. The results obtained, it can be concluded that the suspensions have demonstrated good stability, even when incorporated into a topical pharmaceutical vehicle, thus representing a better technological feasibility for the pharmaceutical area.As infecções fúngicas nos seres humanos ocorrem de formas variadas, podendo tratar-se de micoses superficiais ou micoses sistêmicas. O uso de novos antifúngicos permitiu importantes progressos na terapêutica dos diferentes tipos de infecções micóticas. Dentre os fármacos utilizados para o tratamento, destaca-se o cetoconazol, derivado dos azóis, uma molécula sintética que age inibindo na biossíntese da molécula do ergosterol, exercendo ação fungicida. O tratamento com cetoconazol exige aplicações freqüentes do produto, o que provoca irritação cutânea, dificultando a adesão ao tratamento. Estudos iniciais têm demonstrado que fármacos nanocarreados apresentam melhora na seletividade, reduzindo efeitos colaterais, modificando a liberação e aumentando a eficácia do ativo. Este trabalho teve como objetivo, caracterizar, avaliar a estabilidade físico–química e a atividade antimicrobiana de sistemas compostos de nanopartículas ou micropartículas contendo cetoconazol incorporadas em formulações de xampu. Todos os estudos foram realizados comparando-se o cetoconazol na forma nanoestruturada e microestruturada com a forma livre. As amostras foram armazenadas nas condições de 25 ± 2 °C, 4 ± 2 °C e 40 ± 2 °C e 75 ± 5% UR e expostas à luz UV, durante 90 dias, sendo analisadas em períodos 0, 7, 15, 30, 60 e 90 dias, em relação à determinação do pH, diâmetro de partícula, índice de polidispersão, potencial zeta, taxa de associação e doseamento do fármaco, atividade antimicrobiana e viscosidade para as amostras de xampu. O tamanho médio das partículas para as nanocápsulas foi inferior a 370 nm, para as micropartículas inferior a 52 μm. Todas as amostras compostas pelos nanocarreadores apresentaram potencial zeta negativo. Os valores para a taxa de associação foram de 92,10 % para as nanocápsulas e 97,69 % para as micropartículas. Em relação ao teor das suspensões submetidas aos testes de estabilidade, as amostras compostas por nanocápsulas foram as que apresentaram uma menor perda de quantidade do ativo (17,9 % e 19,7 %) nas condições de 25 ± 2 °C e 4 ± 2 °C respectivamente. Para as formulações de xampu compostas pelos sistemas de nanocarreadores, o mesmo ocorreu, porém com perdas de (9,3 % e 13,6 %) para as mesmas condições das suspensões. Na análise da atividade antimicrobiana, as suspensões de nanocapsulas apresentaram potência de 98,15 % e as de micropartículas 100,25 %. As amostras de xampu foram analisadas pelo ensaio microbiológico de sensibilidade, o qual analisado de forma qualitativa e demonstrou que as amostras possuem atividade antifúngica. As validações das metodologias analíticas para as suspensões apresentaram resultados satisfatórios para todos os parâmetros analisados. Através dos resultados obtidos, pode-se concluir que as suspensões demonstraram ter boa estabilidade, mesmo quando incorporadas em um veículo farmacêutico de uso tópico, representando assim, uma melhor viabilidade tecnológica para a área farmacêutica.Submitted by MARCIA ROVADOSCHI (marciar@unifra.br) on 2018-08-16T14:17:32Z No. of bitstreams: 2 license_rdf: 0 bytes, checksum: d41d8cd98f00b204e9800998ecf8427e (MD5) Dissertacao_FlabioDaRosaPonsJunior.pdf: 2017674 bytes, checksum: ce2baac29e6f32b9170ceef6e8aa57e7 (MD5)Made available in DSpace on 2018-08-16T14:17:32Z (GMT). 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dc.title.por.fl_str_mv SUSPENSÕES E FORMULAÇÕES TÓPICAS CONTENDO NANOCÁPSULAS E MICROPARTÍCULAS DE CETOCONAZOL: AVALIAÇÃO DA ESTABILIDADE E ATIVIDADE ANTIMICROBIANA
title SUSPENSÕES E FORMULAÇÕES TÓPICAS CONTENDO NANOCÁPSULAS E MICROPARTÍCULAS DE CETOCONAZOL: AVALIAÇÃO DA ESTABILIDADE E ATIVIDADE ANTIMICROBIANA
spellingShingle SUSPENSÕES E FORMULAÇÕES TÓPICAS CONTENDO NANOCÁPSULAS E MICROPARTÍCULAS DE CETOCONAZOL: AVALIAÇÃO DA ESTABILIDADE E ATIVIDADE ANTIMICROBIANA
Pons Junior, Flábio da
Cetoconazol, nanocápsulas, micropartículas, xampu, estabilidade, atividade antimicrobiana.
Ketoconazole, nanocapsules, microparticles, shampoo, stability, antimicrobial activity.
Biociências e Nanomateriais
title_short SUSPENSÕES E FORMULAÇÕES TÓPICAS CONTENDO NANOCÁPSULAS E MICROPARTÍCULAS DE CETOCONAZOL: AVALIAÇÃO DA ESTABILIDADE E ATIVIDADE ANTIMICROBIANA
title_full SUSPENSÕES E FORMULAÇÕES TÓPICAS CONTENDO NANOCÁPSULAS E MICROPARTÍCULAS DE CETOCONAZOL: AVALIAÇÃO DA ESTABILIDADE E ATIVIDADE ANTIMICROBIANA
title_fullStr SUSPENSÕES E FORMULAÇÕES TÓPICAS CONTENDO NANOCÁPSULAS E MICROPARTÍCULAS DE CETOCONAZOL: AVALIAÇÃO DA ESTABILIDADE E ATIVIDADE ANTIMICROBIANA
title_full_unstemmed SUSPENSÕES E FORMULAÇÕES TÓPICAS CONTENDO NANOCÁPSULAS E MICROPARTÍCULAS DE CETOCONAZOL: AVALIAÇÃO DA ESTABILIDADE E ATIVIDADE ANTIMICROBIANA
title_sort SUSPENSÕES E FORMULAÇÕES TÓPICAS CONTENDO NANOCÁPSULAS E MICROPARTÍCULAS DE CETOCONAZOL: AVALIAÇÃO DA ESTABILIDADE E ATIVIDADE ANTIMICROBIANA
author Pons Junior, Flábio da
author_facet Pons Junior, Flábio da
author_role author
dc.contributor.advisor1.fl_str_mv Alves, Marta Palma
dc.contributor.referee1.fl_str_mv Angeli , Valeria Weiss
dc.contributor.referee2.fl_str_mv Mortari, Sergio Roberto
dc.contributor.author.fl_str_mv Pons Junior, Flábio da
contributor_str_mv Alves, Marta Palma
Angeli , Valeria Weiss
Mortari, Sergio Roberto
dc.subject.por.fl_str_mv Cetoconazol, nanocápsulas, micropartículas, xampu, estabilidade, atividade antimicrobiana.
topic Cetoconazol, nanocápsulas, micropartículas, xampu, estabilidade, atividade antimicrobiana.
Ketoconazole, nanocapsules, microparticles, shampoo, stability, antimicrobial activity.
Biociências e Nanomateriais
dc.subject.eng.fl_str_mv Ketoconazole, nanocapsules, microparticles, shampoo, stability, antimicrobial activity.
dc.subject.cnpq.fl_str_mv Biociências e Nanomateriais
description The fungal infections in humans occur in several ways, can this is superficial and systemic mycoses mycoses. The use of new antifungal made important progress in the treatment of different types of fungal infections. Among the drugs used to treat, there is ketoconazole, azole derivative, a synthetic molecule that acts by inhibiting biosynthesis of ergosterol molecule, exerting fungicidal. Treatment with ketoconazole requires frequent applications of the product, which causes skin irritation, the adherence to treatment. Initial studies have shown that drugs have nanocarrier improvement in selectivity, reducing side effects by modifying the release and increasing the effectiveness of the asset. This study aimed to characterize, evaluate the physical and chemical stability and antimicrobial activity of systems composed of nanoparticles or microparticles incorporated into formulations containing ketoconazole shampoo. All studies were carried out comparing ketoconazole as nanostructured and microstructured with the free form. The samples were stored under conditions of 25 ± 2 ° C, 4 ± 2 ° C and 40 ± 2 ° C and 75 ± 5% RH and exposed to UV light for 90 days and analyzed at 0, 7, 15, 30, 60 and 90 days in relation to the determination of pH, particle diameter, polydispersity index, zeta potential, rate of association and the drug dosing, antimicrobial activity and viscosity for the samples of shampoo. The average particle size for the nanocapsules was less than 370 nm, for microparticles less than 52 micrometers. All samples consist of the nanocarrier showed negative zeta potential. The values for the rate of association were 92.10% for the nanocapsules and 97.69% for the microparticles. Regarding the content of the suspensions and tested for stability, the samples comprising nanocapsules showed the loss of a smaller amount of assets (17.9% and 19.7%) in conditions of 25 ± 2 ° C and ± 4 2 ° C respectively. For formulations of shampoo made by nanocarrier systems, the same place, but with losses (9.3% and 13.6%) for the same conditions of suspension. In the analysis of antimicrobial activity, suspensions of nanocapsules had power of 98.15% and 100.25% of microparticles. Samples of shampoo were analyzed by microbiological assay sensitivity, which analyzed both qualitatively and showed that the samples have antifungal activity. The validation of analytical methodologies for the suspensions showed satisfactory results for all parameters. The results obtained, it can be concluded that the suspensions have demonstrated good stability, even when incorporated into a topical pharmaceutical vehicle, thus representing a better technological feasibility for the pharmaceutical area.
publishDate 2011
dc.date.issued.fl_str_mv 2011-08-30
dc.date.accessioned.fl_str_mv 2018-08-16T14:17:32Z
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dc.identifier.citation.fl_str_mv Pons Junior, Flábio da. SUSPENSÕES E FORMULAÇÕES TÓPICAS CONTENDO NANOCÁPSULAS E MICROPARTÍCULAS DE CETOCONAZOL: AVALIAÇÃO DA ESTABILIDADE E ATIVIDADE ANTIMICROBIANA. 2011. 100f. 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/500
identifier_str_mv Pons Junior, Flábio da. SUSPENSÕES E FORMULAÇÕES TÓPICAS CONTENDO NANOCÁPSULAS E MICROPARTÍCULAS DE CETOCONAZOL: AVALIAÇÃO DA ESTABILIDADE E ATIVIDADE ANTIMICROBIANA. 2011. 100f. Dissertação( Programa de Pós-Graduação em Nanociências) - Centro Universitário Franciscano, Santa Maria -RS .
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