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Title: Trypanocidal activity and increased solubility of benznidazole incorporated in PEG 4000 and its derivatives.
Authors: Sousa, Lucas Resende Dutra
Azevedo, Maria Luíza Schaefer
Rocha, Dayana F.
Andrade, Ângela Leão
Amparo, Tatiane Roquete
Santos, Orlando David Henrique dos
Seibert, Janaína Brandão
Pereira, Luciano Rodrigues
Vieira, Paula Melo de Abreu
Carneiro, Cláudia Martins
Barboza, Ana Paula Moreira
Neves, Bernardo Ruegger Almeida
Sales Junior, Policarpo Ademar Molina
Murta, Silvane Maria Fonseca
Novack, Kátia Monteiro
Santos, Viviane Martins Rebello dos
Keywords: Chagas disease
Issue Date: 2021
Citation: SOUSA, L. R. D. et al. Trypanocidal activity and increased solubility of benznidazole incorporated in PEG 4000 and its derivatives. Journal of Brazilian Chemistry Society, v. 32, n. 6, p. 1162-1172, 2021. Disponível em: <>. Acesso em: 10 jun. 2021.
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.
ISSN: 1678-4790
metadata.dc.rights.license: This is an open-access article distributed under the terms of the Creative Commons Attribution License. Fonte: o PDF do artigo.
Appears in Collections:DEACL - Artigos publicados em periódicos

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