DESENVOLVIMENTO TECNOLÓGICO E CARACTERIZAÇÃO FÍSICO-QUÍMICA DE NANOPARTÍCULAS POLIMÉRICAS CONTENDO APOCININA
Autor(a) principal: | |
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Data de Publicação: | 2014 |
Tipo de documento: | Dissertação |
Idioma: | por |
Título da fonte: | Biblioteca Digital de Teses e Dissertações do UNICENTRO |
Texto Completo: | http://tede.unicentro.br:8080/jspui/handle/jspui/662 |
Resumo: | Apocynin, also known as acetovanillone, is a methoxy-catechol described as a product originally extracted from the roots of Picrorhiza kurroa Royle (Scrophulariaceae). The most consistent studies involving apocynin are related to their effect on the pathophysiological mechanisms of NADPH oxidase inhibition, which represents an attractive therapeutic target for many diseases. However, apocynin has low solubility in water, and small dose-dependent therapeutic window, which are likely to influence their low bioavailability by oral route. The aim of this study was the development of polymeric nanoparticles containing apocynin from polymers PLA, PLA - PEG and bovine serum albumin (BSA), in order to improve their oral bioavailability characteristics. For quantification and determination of apocynin on nanoparticles encapsulation efficiency (EE%), it was developed and validated an analytical methodology in high performance liquid chromatography (HPLC). For morphological and physicochemical characterization of the nanoparticles, analysis of particle diameter and polydispersity index (PI), zeta potential (ZP), infrared spectroscopy (IR), X-ray diffraction (XRD), and differential scanning calorimetry (DSC) were performed. BSA nanoparticle containing apocynin showed the best results in relation to their morphological and physico-chemical characterization, especially in formulations with pH modification, in which the optimal composition had particles with reduced diameters, which were smaller than 300 nm, and rates of drug encapsulation efficiency ≥ 79.5 %. According to XRD and DSC, there was a decrease of crystallinity of apocynin after the nanoencapsulation process, thereby generating particles with better dissolution in water. Therefore, it can be concluded that BSA nanoparticles containing apocynin developed in this study have suitable morphological and physicochemical characteristics, which make them a potential drug delivery system. |
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Khalil, Najeh Maissarhttp://lattes.cnpq.br/8578241611510102Mainardes, Rubiana Marahttp://lattes.cnpq.br/7632867790178003066.385.149-11http://lattes.cnpq.br/0561453634710061OLIVEIRA, JULIANA KOVALCZUK DE2017-06-05T16:38:51Z2014-05-05OLIVEIRA, JULIANA KOVALCZUK DE. JULIANA KOVALCZUK DE OLIVEIRA. 2014. 79 f. Dissertação (Programa de Pós-Graduação em Ciências Farmacêuticas - Mestrado / Associação Ampla com UEPG) - Universidade Estadual do Centro-Oeste, Guarapuava - PR.http://tede.unicentro.br:8080/jspui/handle/jspui/662Apocynin, also known as acetovanillone, is a methoxy-catechol described as a product originally extracted from the roots of Picrorhiza kurroa Royle (Scrophulariaceae). The most consistent studies involving apocynin are related to their effect on the pathophysiological mechanisms of NADPH oxidase inhibition, which represents an attractive therapeutic target for many diseases. However, apocynin has low solubility in water, and small dose-dependent therapeutic window, which are likely to influence their low bioavailability by oral route. The aim of this study was the development of polymeric nanoparticles containing apocynin from polymers PLA, PLA - PEG and bovine serum albumin (BSA), in order to improve their oral bioavailability characteristics. For quantification and determination of apocynin on nanoparticles encapsulation efficiency (EE%), it was developed and validated an analytical methodology in high performance liquid chromatography (HPLC). For morphological and physicochemical characterization of the nanoparticles, analysis of particle diameter and polydispersity index (PI), zeta potential (ZP), infrared spectroscopy (IR), X-ray diffraction (XRD), and differential scanning calorimetry (DSC) were performed. BSA nanoparticle containing apocynin showed the best results in relation to their morphological and physico-chemical characterization, especially in formulations with pH modification, in which the optimal composition had particles with reduced diameters, which were smaller than 300 nm, and rates of drug encapsulation efficiency ≥ 79.5 %. According to XRD and DSC, there was a decrease of crystallinity of apocynin after the nanoencapsulation process, thereby generating particles with better dissolution in water. Therefore, it can be concluded that BSA nanoparticles containing apocynin developed in this study have suitable morphological and physicochemical characteristics, which make them a potential drug delivery system.Apocinina, também conhecida como acetovanilona, é um metoxi-catecol descrito como produto originalmente extraído a partir de raízes de Picrorhiza kurroa Royle (Scrophulariaceae). Os estudos mais consistentes envolvendo apocinina estão relacionados com seus efeitos sobre os mecanismos fisiopatológicos de inibição da enzima NADPH oxidase, o qual representa um alvo terapêutico atraente para várias doenças. Entretanto, a apocinina tem como característica fraca solubilidade em meio aquoso, estreita relação dose-dependente e janela terapêutica, que provavelmente influenciam sua baixa biodisponibilidade por via oral. O objetivo do presente estudo foi o desenvolvimento de nanopartículas poliméricas contendo apocinina a partir de polímeros PLA, PLA-PEG e albumina de soro bovino (BSA), com o intuito de melhorar suas características de biodisponibilidade oral. Para quantificação e determinação da eficiência de encapsulação (EE%) de apocinina em nanopartículas, foi desenvolvida e validada metodologia analítica por cromatografia líquida de alta eficiência (CLAE). Para a caracterização morfológica e físico-química das nanopartículas, foram realizadas análises de diâmetro médio da partícula e índice de polidispersão (IP), potencial zeta (PZ), espectroscopia na região do infravermelho (IV), difração de raios X (DRX) e calorimetria diferencial exploratória (DSC). Formulações de nanopartículas de BSA contendo apocinina foram as que apresentaram melhores resultados em relação à sua caracterização morfológica e físico-química, dos quais a composição ideal que apresentaram partículas com diâmetros reduzidos, inferiores à 300 nm, e índices de eficiências de encapsulação da droga ≥ 79,5%. De acordo com os testes de DRX e DSC, houve diminuição do grau de cristalinidade da apocinina após o processo de nanoencapsulação, gerando partículas de melhor dissolução em água. Portanto, pode-se concluir que as nanopartículas de BSA contendo apocinina desenvolvidas nesse estudo possuem características morfológicas e físico-químicas adequadas para sua finalidade como sistema de liberação controlada.Submitted by Fabiano Jucá (fjuca@unicentro.br) on 2017-06-05T16:38:50Z No. of bitstreams: 1 JULIANA KOVALCZUK DE OLIVEIRA.pdf: 1881449 bytes, checksum: f357dd85a0d16bd6c7a537355c618ac8 (MD5)Made available in DSpace on 2017-06-05T16:38:51Z (GMT). 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dc.title.por.fl_str_mv |
DESENVOLVIMENTO TECNOLÓGICO E CARACTERIZAÇÃO FÍSICO-QUÍMICA DE NANOPARTÍCULAS POLIMÉRICAS CONTENDO APOCININA |
title |
DESENVOLVIMENTO TECNOLÓGICO E CARACTERIZAÇÃO FÍSICO-QUÍMICA DE NANOPARTÍCULAS POLIMÉRICAS CONTENDO APOCININA |
spellingShingle |
DESENVOLVIMENTO TECNOLÓGICO E CARACTERIZAÇÃO FÍSICO-QUÍMICA DE NANOPARTÍCULAS POLIMÉRICAS CONTENDO APOCININA OLIVEIRA, JULIANA KOVALCZUK DE Apocinina Albumina Nanopartículas NADPH oxidase Apocynin Albumin Nanoparticle NADPH oxidase CIENCIAS DA SAUDE::FARMACIA |
title_short |
DESENVOLVIMENTO TECNOLÓGICO E CARACTERIZAÇÃO FÍSICO-QUÍMICA DE NANOPARTÍCULAS POLIMÉRICAS CONTENDO APOCININA |
title_full |
DESENVOLVIMENTO TECNOLÓGICO E CARACTERIZAÇÃO FÍSICO-QUÍMICA DE NANOPARTÍCULAS POLIMÉRICAS CONTENDO APOCININA |
title_fullStr |
DESENVOLVIMENTO TECNOLÓGICO E CARACTERIZAÇÃO FÍSICO-QUÍMICA DE NANOPARTÍCULAS POLIMÉRICAS CONTENDO APOCININA |
title_full_unstemmed |
DESENVOLVIMENTO TECNOLÓGICO E CARACTERIZAÇÃO FÍSICO-QUÍMICA DE NANOPARTÍCULAS POLIMÉRICAS CONTENDO APOCININA |
title_sort |
DESENVOLVIMENTO TECNOLÓGICO E CARACTERIZAÇÃO FÍSICO-QUÍMICA DE NANOPARTÍCULAS POLIMÉRICAS CONTENDO APOCININA |
author |
OLIVEIRA, JULIANA KOVALCZUK DE |
author_facet |
OLIVEIRA, JULIANA KOVALCZUK DE |
author_role |
author |
dc.contributor.advisor1.fl_str_mv |
Khalil, Najeh Maissar |
dc.contributor.advisor1Lattes.fl_str_mv |
http://lattes.cnpq.br/8578241611510102 |
dc.contributor.advisor-co1.fl_str_mv |
Mainardes, Rubiana Mara |
dc.contributor.advisor-co1Lattes.fl_str_mv |
http://lattes.cnpq.br/7632867790178003 |
dc.contributor.authorID.fl_str_mv |
066.385.149-11 |
dc.contributor.authorLattes.fl_str_mv |
http://lattes.cnpq.br/0561453634710061 |
dc.contributor.author.fl_str_mv |
OLIVEIRA, JULIANA KOVALCZUK DE |
contributor_str_mv |
Khalil, Najeh Maissar Mainardes, Rubiana Mara |
dc.subject.por.fl_str_mv |
Apocinina Albumina Nanopartículas NADPH oxidase |
topic |
Apocinina Albumina Nanopartículas NADPH oxidase Apocynin Albumin Nanoparticle NADPH oxidase CIENCIAS DA SAUDE::FARMACIA |
dc.subject.eng.fl_str_mv |
Apocynin Albumin Nanoparticle NADPH oxidase |
dc.subject.cnpq.fl_str_mv |
CIENCIAS DA SAUDE::FARMACIA |
description |
Apocynin, also known as acetovanillone, is a methoxy-catechol described as a product originally extracted from the roots of Picrorhiza kurroa Royle (Scrophulariaceae). The most consistent studies involving apocynin are related to their effect on the pathophysiological mechanisms of NADPH oxidase inhibition, which represents an attractive therapeutic target for many diseases. However, apocynin has low solubility in water, and small dose-dependent therapeutic window, which are likely to influence their low bioavailability by oral route. The aim of this study was the development of polymeric nanoparticles containing apocynin from polymers PLA, PLA - PEG and bovine serum albumin (BSA), in order to improve their oral bioavailability characteristics. For quantification and determination of apocynin on nanoparticles encapsulation efficiency (EE%), it was developed and validated an analytical methodology in high performance liquid chromatography (HPLC). For morphological and physicochemical characterization of the nanoparticles, analysis of particle diameter and polydispersity index (PI), zeta potential (ZP), infrared spectroscopy (IR), X-ray diffraction (XRD), and differential scanning calorimetry (DSC) were performed. BSA nanoparticle containing apocynin showed the best results in relation to their morphological and physico-chemical characterization, especially in formulations with pH modification, in which the optimal composition had particles with reduced diameters, which were smaller than 300 nm, and rates of drug encapsulation efficiency ≥ 79.5 %. According to XRD and DSC, there was a decrease of crystallinity of apocynin after the nanoencapsulation process, thereby generating particles with better dissolution in water. Therefore, it can be concluded that BSA nanoparticles containing apocynin developed in this study have suitable morphological and physicochemical characteristics, which make them a potential drug delivery system. |
publishDate |
2014 |
dc.date.issued.fl_str_mv |
2014-05-05 |
dc.date.accessioned.fl_str_mv |
2017-06-05T16:38:51Z |
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info:eu-repo/semantics/publishedVersion |
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publishedVersion |
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OLIVEIRA, JULIANA KOVALCZUK DE. JULIANA KOVALCZUK DE OLIVEIRA. 2014. 79 f. Dissertação (Programa de Pós-Graduação em Ciências Farmacêuticas - Mestrado / Associação Ampla com UEPG) - Universidade Estadual do Centro-Oeste, Guarapuava - PR. |
dc.identifier.uri.fl_str_mv |
http://tede.unicentro.br:8080/jspui/handle/jspui/662 |
identifier_str_mv |
OLIVEIRA, JULIANA KOVALCZUK DE. JULIANA KOVALCZUK DE OLIVEIRA. 2014. 79 f. Dissertação (Programa de Pós-Graduação em Ciências Farmacêuticas - Mestrado / Associação Ampla com UEPG) - Universidade Estadual do Centro-Oeste, Guarapuava - PR. |
url |
http://tede.unicentro.br:8080/jspui/handle/jspui/662 |
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por |
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por |
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6997636413449754996 |
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openAccess |
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Universidade Estadual do Centro-Oeste |
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Programa de Pós-Graduação em Ciências Farmacêuticas (Mestrado / Associação Ampla com UEPG) |
dc.publisher.initials.fl_str_mv |
UNICENTRO |
dc.publisher.country.fl_str_mv |
Brasil |
dc.publisher.department.fl_str_mv |
Unicentro::Departamento de Farmácia |
publisher.none.fl_str_mv |
Universidade Estadual do Centro-Oeste |
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