Trypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives
Autor(a) principal: | |
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Data de Publicação: | 2021 |
Outros Autores: | , , , , , , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da FIOCRUZ (ARCA) |
Texto Completo: | https://www.arca.fiocruz.br/handle/icict/51428 |
Resumo: | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, Brazil |
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Sousa, Lucas Resende DutraAzevedo, Maria Luíza SchaeferRocha, Dayana FerreiraAndrade, Ângela LeãoAmparo, Tatiane RoqueteSantos, Orlando David Henrique dosSeibert, Janaína BrandãoVieira, Paula Melo de AbreuCarneiro, Cláudia MartinsBarboza, Ana Paula MoreiraNeves, Bernardo Ruegger AlmeidaSales Junior, Policarpo AdemarMurta, Silvane Maria FonsecaNovack, Kátia MonteiroSantos, Viviane Martins Rebello dos2022-02-23T13:39:54Z2022-02-23T13:39:54Z2021SOUSA, Lucas Resende Dutra et al. Trypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives. J. Braz. Chem. Soc., v. 32, n. 6, p. 1162-1172, 2021. doi.org/10.21577/0103-5053.202100170103-5053https://www.arca.fiocruz.br/handle/icict/5142810.21577/0103-5053.20210017engSociedade Brasileira de QuímicaTrypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivativesinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleUniversidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, BrazilUniversidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, BrazilUniversidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, BrazilUniversidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, BrazilUniversidade Federal de Ouro Preto. Escola de Farmácia. Ouro Preto, MG, BrazilUniversidade Federal de Ouro Preto. Escola de Farmácia. Ouro Preto, MG, BrazilUniversidade Federal de São Carlos. Departamento de Química. São Carlos, SP, BrazilUniversidade Federal de São Carlos. Departamento de Química. São Carlos, SP, BrazilUniversidade Federal de Ouro Preto. Instituto Departamento de Ciências Biológicas. Ouro Preto, MG, BrazilUniversidade Federal de Ouro Preto. Escola de Farmácia. Ouro Preto, MG, BrazilUniversidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Física. Ouro Preto, MG, BrazilUniversidade Federal de Minas Gerais. Departamento de Física. Belo Horizonte, MG, BrazilFundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, BrazilFundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, BrazilUniversidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, BrazilUniversidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, BrazilSelecting a polymer depends on its characteristics, the properties of the drug and of the remaining ingredients in the formulation. The drug, when incorporated into a polymeric matrix, can show several advantages when compared with its conventional form. In this context, this work describes the preparation and characterization of polyethylene glycol (PEG 4000) and its derivative particles loaded with benznidazole, as well as evaluates their trypanocidal activity. In this work, reactions to modify the PEG 4000 polymer and the subsequent incorporation of the benznidazole were made. The nuclear magnetic resonance (NMR) analysis confirmed the efficiency in modifying the PEG chains. The morphology of polymeric films was observed by atomic force microscopy (AFM) and showed considerable changes on the film organization. The acetylation of PEG favored the stability of the system and an increase in the zeta potential from -14.83 to -25.54 mV was observed. Although encapsulation efficiency values between 30.14 and 39.48% were found, the enhanced benznidazole dissolution profile by microparticles enables the use of lower drug concentrations. This fact can be proven by the increased trypanocidal effect of benznidazole when encapsulated in BP3 microparticles. Finally, the high selectivity of the formulations for trypanocidal action guarantees their safety as an alternative for the treatment of the Chagas disease.benznidazoleChagas diseasecytotoxicitymicroparticlespolymerinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-83082https://www.arca.fiocruz.br/bitstream/icict/51428/1/license.txt9193a7c197bc67acd023525e72a03240MD51ORIGINALTrypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives.pdfTrypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives.pdfapplication/pdf4064387https://www.arca.fiocruz.br/bitstream/icict/51428/2/Trypanocidal%20Activity%20and%20Increased%20Solubility%20of%20Benznidazole%20Incorporated%20in%20PEG%204000%20and%20Its%20Derivatives.pdfae4ed1cfb5627475f566f5d9fc1af923MD52icict/514282022-02-23 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dc.title.pt_BR.fl_str_mv |
Trypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives |
title |
Trypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives |
spellingShingle |
Trypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives Sousa, Lucas Resende Dutra benznidazole Chagas disease cytotoxicity microparticles polymer |
title_short |
Trypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives |
title_full |
Trypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives |
title_fullStr |
Trypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives |
title_full_unstemmed |
Trypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives |
title_sort |
Trypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives |
author |
Sousa, Lucas Resende Dutra |
author_facet |
Sousa, Lucas Resende Dutra Azevedo, Maria Luíza Schaefer Rocha, Dayana Ferreira Andrade, Ângela Leão Amparo, Tatiane Roquete Santos, Orlando David Henrique dos Seibert, Janaína Brandão Vieira, Paula Melo de Abreu Carneiro, Cláudia Martins Barboza, Ana Paula Moreira Neves, Bernardo Ruegger Almeida Sales Junior, Policarpo Ademar Murta, Silvane Maria Fonseca Novack, Kátia Monteiro Santos, Viviane Martins Rebello dos |
author_role |
author |
author2 |
Azevedo, Maria Luíza Schaefer Rocha, Dayana Ferreira Andrade, Ângela Leão Amparo, Tatiane Roquete Santos, Orlando David Henrique dos Seibert, Janaína Brandão Vieira, Paula Melo de Abreu Carneiro, Cláudia Martins Barboza, Ana Paula Moreira Neves, Bernardo Ruegger Almeida Sales Junior, Policarpo Ademar Murta, Silvane Maria Fonseca Novack, Kátia Monteiro Santos, Viviane Martins Rebello dos |
author2_role |
author author author author author author author author author author author author author author |
dc.contributor.author.fl_str_mv |
Sousa, Lucas Resende Dutra Azevedo, Maria Luíza Schaefer Rocha, Dayana Ferreira Andrade, Ângela Leão Amparo, Tatiane Roquete Santos, Orlando David Henrique dos Seibert, Janaína Brandão Vieira, Paula Melo de Abreu Carneiro, Cláudia Martins Barboza, Ana Paula Moreira Neves, Bernardo Ruegger Almeida Sales Junior, Policarpo Ademar Murta, Silvane Maria Fonseca Novack, Kátia Monteiro Santos, Viviane Martins Rebello dos |
dc.subject.en.pt_BR.fl_str_mv |
benznidazole Chagas disease cytotoxicity microparticles polymer |
topic |
benznidazole Chagas disease cytotoxicity microparticles polymer |
description |
Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, Brazil |
publishDate |
2021 |
dc.date.issued.fl_str_mv |
2021 |
dc.date.accessioned.fl_str_mv |
2022-02-23T13:39:54Z |
dc.date.available.fl_str_mv |
2022-02-23T13:39:54Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.citation.fl_str_mv |
SOUSA, Lucas Resende Dutra et al. Trypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives. J. Braz. Chem. Soc., v. 32, n. 6, p. 1162-1172, 2021. doi.org/10.21577/0103-5053.20210017 |
dc.identifier.uri.fl_str_mv |
https://www.arca.fiocruz.br/handle/icict/51428 |
dc.identifier.issn.pt_BR.fl_str_mv |
0103-5053 |
dc.identifier.doi.none.fl_str_mv |
10.21577/0103-5053.20210017 |
identifier_str_mv |
SOUSA, Lucas Resende Dutra et al. Trypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives. J. Braz. Chem. Soc., v. 32, n. 6, p. 1162-1172, 2021. doi.org/10.21577/0103-5053.20210017 0103-5053 10.21577/0103-5053.20210017 |
url |
https://www.arca.fiocruz.br/handle/icict/51428 |
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eng |
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eng |
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info:eu-repo/semantics/openAccess |
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openAccess |
dc.publisher.none.fl_str_mv |
Sociedade Brasileira de Química |
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Sociedade Brasileira de Química |
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reponame:Repositório Institucional da FIOCRUZ (ARCA) instname:Fundação Oswaldo Cruz (FIOCRUZ) instacron:FIOCRUZ |
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Fundação Oswaldo Cruz (FIOCRUZ) |
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FIOCRUZ |
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Repositório Institucional da FIOCRUZ (ARCA) |
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