Desenvolvimento de nanoformulação de zeína para liberação controlada de apocinina
Autor(a) principal: | |
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Data de Publicação: | 2020 |
Tipo de documento: | Tese |
Idioma: | por |
Título da fonte: | Biblioteca Digital de Teses e Dissertações do UNICENTRO |
Texto Completo: | http://tede.unicentro.br:8080/jspui/handle/jspui/1835 |
Resumo: | Apocynin (APO) is a phenolic compound initially isolated from the species Picrorhiza kurroa. This compound has been extensively investigated for its ability to inhibit the nicotinamide adenine dinucleotide phosphate (NADPH) multi-enzymatic complex by interacting with the activating proteins necessary to assemble the enzyme units and, consequently, blocking its activity. This complex is the only endogenous system intended for superoxide anion production, a precursor of highly oxidizing substances. In this sense, a biological action of apocynin consists of modulating the action of NADPH oxidase and preventing the formation of oxidative species that, in excess, can modify the redox state of cells. As a result, APO has a positive effect on the prevention and remediation of a wide number of diseases including ischemic accidents, Alzheimer's, diabetes and others. However, APO presents some options for using it in terms of pharmacokinetic properties, mainly due to the oral route, which result in low absorption and rapid elimination of the compound. The nanostructured systems based on naturals polymers have been a promising way to improve the physicochemical characteristics of various compounds. In this context, the objective of the present study was to develop a zein, casein and lysine nanoparticle (NP-ZCL-APO) using the liquid-liquid dispersion method to enable APO by oral route. The nanoparticles obtained were characterized by particle size distribuition, mean particle size (𝑆̅), polydispersity index (PI), zeta potential (ZP), encapsulation efficiency (% EE), scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), thermal analysis (TA), simulated gastrointestinal release, stability assessment, hemolytic cytotoxicity and cytotoxicity against Vero, Caco-2, and HaCaT cells. The 𝑆̅value was 208.8 ± 12.3 nm, with PI of 0.134 ± 0.036, and ZP of -22.0 ± 2.3 mV. SEM images demonstrated regular and spherical shape. The % EE was optimized which resulted in 27.1 ± 3.5 % encapsulation, (1.91 ± 0.26 mg APO / mL).There was no evidence of chemical reactions and formation of new components in the matrix from FTIR. NP-ZCL-APO showed an increase in thermal stability, a reduction in blood cell toxicity that causes cell disruption and reduced inhibition of normal cell growth when compared to free APO. The APO cumulative gastrointestinal release was 31.2 ± 2.1 %. Regarding stability, NP-ZCL-APO maintained the physicochemical characteristics after the freeze-drying process with cryoprotectant and also when it was subject to storage at refrigerated temperature (4 °C) and room temperature (25 °C) for a period of ten months. In addition, there was a reduction in toxicity on blood cells and on normal cells when compared to free APO. In addition, NP-ZCL-APO showed interaction with mucin, the main glycoprotein in mucus, indicating mucoadhesion. Based on the characterizations set, combined with the low cost of formulation and low toxicity, the obtained system was consolidated for in vivo tests. The maintenance of the physicochemical characteristics after the freeze-drying process, in the presence of the selected cryoprotectant, is a result that favors this direction. Therefore, the study concluded the nanoparticle of NP-ZCL-APO developed is a potential alternative to optimize the pharmacokinetic properties and bioavailability of APO for the use of this compound orally. |
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Khalil, Najeh Maissarhttp://lattes.cnpq.br/8578241611510102Mainardes, Rubiana Marahttp://lattes.cnpq.br/7632867790178003046863449-56http://lattes.cnpq.br/9790824082917402Giongo, Camila Nascimento2022-02-22T15:10:49Z2020-06-29Giongo, Camila Nascimento. Desenvolvimento de nanoformulação de zeína para liberação controlada de apocinina. 2020. 100 f. Tese (Programa de Pós-Graduação em Química - Doutorado) - Universidade Estadual do Centro-Oeste, Guarapuava - PR.http://tede.unicentro.br:8080/jspui/handle/jspui/1835Apocynin (APO) is a phenolic compound initially isolated from the species Picrorhiza kurroa. This compound has been extensively investigated for its ability to inhibit the nicotinamide adenine dinucleotide phosphate (NADPH) multi-enzymatic complex by interacting with the activating proteins necessary to assemble the enzyme units and, consequently, blocking its activity. This complex is the only endogenous system intended for superoxide anion production, a precursor of highly oxidizing substances. In this sense, a biological action of apocynin consists of modulating the action of NADPH oxidase and preventing the formation of oxidative species that, in excess, can modify the redox state of cells. As a result, APO has a positive effect on the prevention and remediation of a wide number of diseases including ischemic accidents, Alzheimer's, diabetes and others. However, APO presents some options for using it in terms of pharmacokinetic properties, mainly due to the oral route, which result in low absorption and rapid elimination of the compound. The nanostructured systems based on naturals polymers have been a promising way to improve the physicochemical characteristics of various compounds. In this context, the objective of the present study was to develop a zein, casein and lysine nanoparticle (NP-ZCL-APO) using the liquid-liquid dispersion method to enable APO by oral route. The nanoparticles obtained were characterized by particle size distribuition, mean particle size (𝑆̅), polydispersity index (PI), zeta potential (ZP), encapsulation efficiency (% EE), scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), thermal analysis (TA), simulated gastrointestinal release, stability assessment, hemolytic cytotoxicity and cytotoxicity against Vero, Caco-2, and HaCaT cells. The 𝑆̅value was 208.8 ± 12.3 nm, with PI of 0.134 ± 0.036, and ZP of -22.0 ± 2.3 mV. SEM images demonstrated regular and spherical shape. The % EE was optimized which resulted in 27.1 ± 3.5 % encapsulation, (1.91 ± 0.26 mg APO / mL).There was no evidence of chemical reactions and formation of new components in the matrix from FTIR. NP-ZCL-APO showed an increase in thermal stability, a reduction in blood cell toxicity that causes cell disruption and reduced inhibition of normal cell growth when compared to free APO. The APO cumulative gastrointestinal release was 31.2 ± 2.1 %. Regarding stability, NP-ZCL-APO maintained the physicochemical characteristics after the freeze-drying process with cryoprotectant and also when it was subject to storage at refrigerated temperature (4 °C) and room temperature (25 °C) for a period of ten months. In addition, there was a reduction in toxicity on blood cells and on normal cells when compared to free APO. In addition, NP-ZCL-APO showed interaction with mucin, the main glycoprotein in mucus, indicating mucoadhesion. Based on the characterizations set, combined with the low cost of formulation and low toxicity, the obtained system was consolidated for in vivo tests. The maintenance of the physicochemical characteristics after the freeze-drying process, in the presence of the selected cryoprotectant, is a result that favors this direction. Therefore, the study concluded the nanoparticle of NP-ZCL-APO developed is a potential alternative to optimize the pharmacokinetic properties and bioavailability of APO for the use of this compound orally.Apocinina (APO) é um composto fenólico isolado da espécie Picrorhiza kurroa que tem sido investigado por sua capacidade de inibir o complexo multienzimático fosfato de dinucleotídeo nicotinamida adenina (NADPH) por interagir com as proteínas ativadoras necessárias à montagem das unidades enzimáticas e, consequentemente, bloquear sua atividade. Tal complexo é o único sistema endógeno destinado à produção do ânion superóxido, precursor de substâncias altamente oxidantes. Nesse sentido, a ação biológica da APO consiste em modular a ação da NADPH oxidase e impedir a formação dessas espécies oxidativas que, em excesso, podem atuar modificando o estado redox das células. Em consequência disso, a APO promove efeito na prevenção e remediação de um amplo número de doenças que incluem acidentes isquêmicos, Alzheimer, diabetes, entre outras. No entanto, a APO apresenta algumas limitações de uso quanto às propriedades farmacocinéticas, sobretudo por rota de administração gastrointestinal, que resultam na baixa absorção e rápida eliminação do composto. Os sistemas nanoestruturados baseados em polímeros naturais têm sido uma ferramenta promissora para ampliar características físico-químicas de vários compostos. Nesse contexto, o objetivo do presente trabalho consistiu em desenvolver nanopartículas de zeína, caseína e lisina com o composto APO (NP-ZCL-APO) pelo método de dispersão líquido-líquido para viabilizar a administração de APO por via gastrointestinal. As NP-ZCL-APO obtidas foram caracterizadas por diâmetro médio de partícula (𝑆̅), índice de polidispersão (IPD), potencial zeta (PZ), eficiência de encapsulação (% EE), microscopia eletrônica de varredura (MEV), difração de raio X (DRX), espectroscopia de infravermelho com transformada de Fourier (FTIR), análise térmica (TA), liberação gastrointestinal simulada, avaliação de estabilidade, citotoxicidade hemolítica e citotoxicidade sobre células Vero, Caco-2 e HaCaT e teste de mucoadesão. O valor 𝑆̅foi de 208,8 ± 12,3 nm, com IPD de 0,134 ± 0,036 e PZ de -22,0 ± 2,3 mV. A % EE resultou em 27,1 ± 3,5% de encapsulação (1,91 ± 0,26 mg APO / mL). As imagens de MEV demonstraram forma regular e esférica. Não houve evidências de reações químicas e de formação de novos componentes na matriz identificados com FTIR. As NP-ZCL-APO mostraram um aumento na estabilidade térmica avaliada por TA. A liberação gastrointestinal cumulativa da APO foi de 31,2 ± 2,1%. Em relação a estabilidade, as NP-ZCL-APO mantiveram as características físico-químicas após o processo de liofilização com crioprotetor e também quando submetidas ao armazenamento em temperatura refrigerada (4 °C) e ambiente (25 °C) por um período de dez meses. Além disso, houve uma redução na toxicidade sobre células sanguíneas e sobre células normais quando comparadas à APO livre e interação de NP-ZCL-APO com a mucina, a principal glicoproteína do muco, indicando mucoadesão. Com base no conjunto de caracterizações, aliado ao baixo custo de formulação e baixa toxicidade, o sistema obtido está consolidado para ser direcionado a testes in vivo. A manutenção das características físico-químicas após o processo de liofilização, na presença do crioprotetor selecionado, é um resultado que favorece esse direcionamento. Assim, conclui-se que as NP-ZCL-APO desenvolvidas neste estudo é uma alternativa potencial para otimizar as propriedades farmacocinéticas e a biodisponibilidade da APO para administração deste composto por via oral.Submitted by Fabiano Jucá (fjuca@unicentro.br) on 2022-02-22T15:10:49Z No. of bitstreams: 1 tese - Camila Nascimento Giongo.pdf: 6025906 bytes, checksum: f02a31c4d66416295bde9a6ecca9b006 (MD5)Made available in DSpace on 2022-02-22T15:10:49Z (GMT). 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dc.title.por.fl_str_mv |
Desenvolvimento de nanoformulação de zeína para liberação controlada de apocinina |
dc.title.alternative.eng.fl_str_mv |
Development of zein nanoformulation for controlled release of apocynin |
title |
Desenvolvimento de nanoformulação de zeína para liberação controlada de apocinina |
spellingShingle |
Desenvolvimento de nanoformulação de zeína para liberação controlada de apocinina Giongo, Camila Nascimento Antioxidante Neutrófilos Mieloperoxidase Anti-inflamatório Acetovanilona Antioxidant Neutrophils Myeloperoxidase Anti-inflammatory Acetovanillone CIENCIAS EXATAS E DA TERRA::QUIMICA |
title_short |
Desenvolvimento de nanoformulação de zeína para liberação controlada de apocinina |
title_full |
Desenvolvimento de nanoformulação de zeína para liberação controlada de apocinina |
title_fullStr |
Desenvolvimento de nanoformulação de zeína para liberação controlada de apocinina |
title_full_unstemmed |
Desenvolvimento de nanoformulação de zeína para liberação controlada de apocinina |
title_sort |
Desenvolvimento de nanoformulação de zeína para liberação controlada de apocinina |
author |
Giongo, Camila Nascimento |
author_facet |
Giongo, Camila Nascimento |
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 |
046863449-56 |
dc.contributor.authorLattes.fl_str_mv |
http://lattes.cnpq.br/9790824082917402 |
dc.contributor.author.fl_str_mv |
Giongo, Camila Nascimento |
contributor_str_mv |
Khalil, Najeh Maissar Mainardes, Rubiana Mara |
dc.subject.por.fl_str_mv |
Antioxidante Neutrófilos Mieloperoxidase Anti-inflamatório Acetovanilona |
topic |
Antioxidante Neutrófilos Mieloperoxidase Anti-inflamatório Acetovanilona Antioxidant Neutrophils Myeloperoxidase Anti-inflammatory Acetovanillone CIENCIAS EXATAS E DA TERRA::QUIMICA |
dc.subject.eng.fl_str_mv |
Antioxidant Neutrophils Myeloperoxidase Anti-inflammatory Acetovanillone |
dc.subject.cnpq.fl_str_mv |
CIENCIAS EXATAS E DA TERRA::QUIMICA |
description |
Apocynin (APO) is a phenolic compound initially isolated from the species Picrorhiza kurroa. This compound has been extensively investigated for its ability to inhibit the nicotinamide adenine dinucleotide phosphate (NADPH) multi-enzymatic complex by interacting with the activating proteins necessary to assemble the enzyme units and, consequently, blocking its activity. This complex is the only endogenous system intended for superoxide anion production, a precursor of highly oxidizing substances. In this sense, a biological action of apocynin consists of modulating the action of NADPH oxidase and preventing the formation of oxidative species that, in excess, can modify the redox state of cells. As a result, APO has a positive effect on the prevention and remediation of a wide number of diseases including ischemic accidents, Alzheimer's, diabetes and others. However, APO presents some options for using it in terms of pharmacokinetic properties, mainly due to the oral route, which result in low absorption and rapid elimination of the compound. The nanostructured systems based on naturals polymers have been a promising way to improve the physicochemical characteristics of various compounds. In this context, the objective of the present study was to develop a zein, casein and lysine nanoparticle (NP-ZCL-APO) using the liquid-liquid dispersion method to enable APO by oral route. The nanoparticles obtained were characterized by particle size distribuition, mean particle size (𝑆̅), polydispersity index (PI), zeta potential (ZP), encapsulation efficiency (% EE), scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), thermal analysis (TA), simulated gastrointestinal release, stability assessment, hemolytic cytotoxicity and cytotoxicity against Vero, Caco-2, and HaCaT cells. The 𝑆̅value was 208.8 ± 12.3 nm, with PI of 0.134 ± 0.036, and ZP of -22.0 ± 2.3 mV. SEM images demonstrated regular and spherical shape. The % EE was optimized which resulted in 27.1 ± 3.5 % encapsulation, (1.91 ± 0.26 mg APO / mL).There was no evidence of chemical reactions and formation of new components in the matrix from FTIR. NP-ZCL-APO showed an increase in thermal stability, a reduction in blood cell toxicity that causes cell disruption and reduced inhibition of normal cell growth when compared to free APO. The APO cumulative gastrointestinal release was 31.2 ± 2.1 %. Regarding stability, NP-ZCL-APO maintained the physicochemical characteristics after the freeze-drying process with cryoprotectant and also when it was subject to storage at refrigerated temperature (4 °C) and room temperature (25 °C) for a period of ten months. In addition, there was a reduction in toxicity on blood cells and on normal cells when compared to free APO. In addition, NP-ZCL-APO showed interaction with mucin, the main glycoprotein in mucus, indicating mucoadhesion. Based on the characterizations set, combined with the low cost of formulation and low toxicity, the obtained system was consolidated for in vivo tests. The maintenance of the physicochemical characteristics after the freeze-drying process, in the presence of the selected cryoprotectant, is a result that favors this direction. Therefore, the study concluded the nanoparticle of NP-ZCL-APO developed is a potential alternative to optimize the pharmacokinetic properties and bioavailability of APO for the use of this compound orally. |
publishDate |
2020 |
dc.date.issued.fl_str_mv |
2020-06-29 |
dc.date.accessioned.fl_str_mv |
2022-02-22T15:10:49Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/doctoralThesis |
format |
doctoralThesis |
status_str |
publishedVersion |
dc.identifier.citation.fl_str_mv |
Giongo, Camila Nascimento. Desenvolvimento de nanoformulação de zeína para liberação controlada de apocinina. 2020. 100 f. Tese (Programa de Pós-Graduação em Química - Doutorado) - Universidade Estadual do Centro-Oeste, Guarapuava - PR. |
dc.identifier.uri.fl_str_mv |
http://tede.unicentro.br:8080/jspui/handle/jspui/1835 |
identifier_str_mv |
Giongo, Camila Nascimento. Desenvolvimento de nanoformulação de zeína para liberação controlada de apocinina. 2020. 100 f. Tese (Programa de Pós-Graduação em Química - Doutorado) - Universidade Estadual do Centro-Oeste, Guarapuava - PR. |
url |
http://tede.unicentro.br:8080/jspui/handle/jspui/1835 |
dc.language.iso.fl_str_mv |
por |
language |
por |
dc.relation.program.fl_str_mv |
3800526532796635565 |
dc.relation.confidence.fl_str_mv |
600 600 600 600 |
dc.relation.department.fl_str_mv |
-4338065490277529033 |
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Universidade Estadual do Centro-Oeste |
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