Author | Sousa, Lucas Resende Dutra | |
Author | Azevedo, Maria Luíza Schaefer | |
Author | Rocha, Dayana Ferreira | |
Author | Andrade, Ângela Leão | |
Author | Amparo, Tatiane Roquete | |
Author | Santos, Orlando David Henrique dos | |
Author | Seibert, Janaína Brandão | |
Author | Vieira, Paula Melo de Abreu | |
Author | Carneiro, Cláudia Martins | |
Author | Barboza, Ana Paula Moreira | |
Author | Neves, Bernardo Ruegger Almeida | |
Author | Sales Junior, Policarpo Ademar | |
Author | Murta, Silvane Maria Fonseca | |
Author | Novack, Kátia Monteiro | |
Author | Santos, Viviane Martins Rebello dos | |
Access date | 2022-02-23T13:39:54Z | |
Available date | 2022-02-23T13:39:54Z | |
Document date | 2021 | |
Citation | 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 | pt_BR |
ISSN | 0103-5053 | pt_BR |
URI | https://www.arca.fiocruz.br/handle/icict/51428 | |
Language | eng | pt_BR |
Publisher | Sociedade Brasileira de Química | pt_BR |
Rights | open access | pt_BR |
Title | Trypanocidal Activity and Increased Solubility of Benznidazole Incorporated in PEG 4000 and Its Derivatives | pt_BR |
Type | Article | pt_BR |
DOI | 10.21577/0103-5053.20210017 | |
Abstract | Selecting 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. | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Escola de Farmácia. Ouro Preto, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Escola de Farmácia. Ouro Preto, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de São Carlos. Departamento de Química. São Carlos, SP, Brazil | pt_BR |
Affilliation | Universidade Federal de São Carlos. Departamento de Química. São Carlos, SP, Brazil | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Instituto Departamento de Ciências Biológicas. Ouro Preto, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Escola de Farmácia. Ouro Preto, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Física. Ouro Preto, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Minas Gerais. Departamento de Física. Belo Horizonte, MG, Brazil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brazil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, Brazil | pt_BR |
Affilliation | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, Brazil | pt_BR |
Subject | benznidazole | pt_BR |
Subject | Chagas disease | pt_BR |
Subject | cytotoxicity | pt_BR |
Subject | microparticles | pt_BR |
Subject | polymer | pt_BR |