Development of alginate granules for thiophenic derivative 5CN06 delivery by ionotropic gelation

Detalhes bibliográficos
Autor(a) principal: Medeiros, Kaline de Araújo
Data de Publicação: 2022
Outros Autores: Rolim, Michelle de Oliveira Pedrosa, Antonino , Rayane Santa Cruz Martins de Queiroz, Silva , Dayanne Tomaz Casimiro da, Mendonça Junior, Francisco Jaime Bezerra, Silva, José Alexsandro da, Damasceno , Bolívar Ponciano Goulart de Lima
Tipo de documento: Artigo
Idioma: por
Título da fonte: Research, Society and Development
Texto Completo: https://rsdjournal.org/index.php/rsd/article/view/35898
Resumo: The use of biodegradable polysaccharides with gel forming capacity to produce granules has been reported, but there are no reports in the literature associated with new 2-aminothiophene derivatives, which have demonstrated selective antifungal biological activity. Thus, the objective of this study was to evaluate the formation of alginate granules for the delivery of the thiophenic derivative and Active Pharmaceutical Ingredient (API) 5CN06 by ionotropic gelation. An emulsion of 0.1% 5CN06, a 3% sodium alginate solution and a 10% CaCl2 solution was produced. The emulsion and the alginate were mixed under different volumes and, under drip, in the CaCl2 solution, the granules were formed. Changing the proportion of polymer interferes with this yield, which is equal to and above 79.50% ± 0.03. In acid medium, pH 1.2, the granule does not have a significant swelling rate after 180 min. In a pH 7.4 medium it dissolves due to the presence of Na+. Using 10 ml of the emulsion mixtures containing the drug and 10 ml of 3% sodium alginate solution, granules were obtained with better encapsulation efficiency (65.7%). The higher mixing ratio interfered in the swelling capacity and in the thermal stabilization of the drug. Thus, the study of this system was promising, from the experimental conditions, for the understanding of the formation of granules to release the thiophenic derivative compound 5CN06, with antifungal action.
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spelling Development of alginate granules for thiophenic derivative 5CN06 delivery by ionotropic gelationDesarrollo de gránulos de alginato para la entrega del derivado tiofénico 5CN06 por gelificación ionotrópicaDesenvolvimento de grânulos de alginato para veiculação de derivado tiofênico 5CN06 por gelificação ionotrópica GrânulosDerivado TiofênicoGelificação IonotrópicaAlginato. GranulesThiophenic DerivativeIonotropic GelationAlginate.GránulosDerivado TiofénicoGelificación IonotrópicaAlginato.The use of biodegradable polysaccharides with gel forming capacity to produce granules has been reported, but there are no reports in the literature associated with new 2-aminothiophene derivatives, which have demonstrated selective antifungal biological activity. Thus, the objective of this study was to evaluate the formation of alginate granules for the delivery of the thiophenic derivative and Active Pharmaceutical Ingredient (API) 5CN06 by ionotropic gelation. An emulsion of 0.1% 5CN06, a 3% sodium alginate solution and a 10% CaCl2 solution was produced. The emulsion and the alginate were mixed under different volumes and, under drip, in the CaCl2 solution, the granules were formed. Changing the proportion of polymer interferes with this yield, which is equal to and above 79.50% ± 0.03. In acid medium, pH 1.2, the granule does not have a significant swelling rate after 180 min. In a pH 7.4 medium it dissolves due to the presence of Na+. Using 10 ml of the emulsion mixtures containing the drug and 10 ml of 3% sodium alginate solution, granules were obtained with better encapsulation efficiency (65.7%). The higher mixing ratio interfered in the swelling capacity and in the thermal stabilization of the drug. Thus, the study of this system was promising, from the experimental conditions, for the understanding of the formation of granules to release the thiophenic derivative compound 5CN06, with antifungal action.Se ha reportado el uso de polisacáridos biodegradables con capacidad gelificante para producir gránulos, pero no existen reportes en la literatura asociados a nuevos derivados del 2-aminotiofeno, que hayan demostrado actividad biológica antifúngica selectiva. Por lo tanto, el objetivo de este estudio fue evaluar la formación de gránulos de alginato para la entrega del derivado tiofénico e Ingrediente Farmacéutico Activo (IFA) 5CN06 por gelificación ionotrópica. Se produjo una emulsión de 5CN06 al 0,1%, una solución de alginato de sodio al 3% y una solución de CaCl2 al 10%. La emulsión y el alginato se mezclaron a diferentes volúmenes y, por goteo, en la solución de CaCl2, se formaron los gránulos. Cambiar la proporción de polímero interfiere con este rendimiento, que es igual y superior a 79,50% ± 0,03. En medio ácido, pH 1,2, el gránulo no tiene una tasa de hinchamiento significativa después de 180 min. En un medio pH 7,4 se disuelve por la presencia de Na+. Usando 10 ml de las mezclas de emulsión que contenían el fármaco y 10 ml de solución de alginato de sodio al 3%, se obtuvieron gránulos con mejor eficiencia de encapsulación (65,7%). La mayor proporción de mezcla interfirió en la capacidad de hinchamiento y en la estabilización térmica del fármaco. Así, el estudio de este sistema resultó prometedor, a partir de las condiciones experimentales, para la comprensión de la formación de gránulos para la liberación del compuesto derivado tiofénico 5CN06, con acción antifúngica.O uso de polissacarídeos biodegradáveis com capacidade de formação de gel para produção de grânulos não tem sido relatado na literatura associados a novos derivados 2-aminotiofênicos, que tem demostrado atividade biológica antifúngica seletiva. Dessa forma o objetivo desse estudo foi avaliar a formação de grânulos de alginato para veiculação do derivado tiofênico e Insumo Farmacêutico Ativo (IFA) 5CN06 por gelificação ionotrópica. Foi produzido uma emulsão de 5CN06 a 0,1%, uma solução de alginato de sódio 3% e uma solução de CaCl2 a 10%. Sob distintos volumes a emulsão e o alginato foram misturadas e sob gotejamento, na solução CaCl2, os grânulos foram formados. A alteração da proporção de polímero interfere nesse rendimento, sendo esse igual e acima de 79,50 % ± 0,03. Em meio ácido, pH 1,2, o grânulo não possui significativa taxa de intumescimento, após 180 min. Em meio pH 7,4 ele se dissolve devido a presença de Na+. Utilizando 10mL das misturas de emulsão que contém o fármaco e 10 mL de solução de alginato de sódio a 3%, obteve-se grânulos, com melhor eficiência de encapsulação (65,7%). A maior razão da mistura interferiu na capacidade de intumescimento e na estabilização térmica do IFA. Dessa forma, o estudo desse sistema foi promissor, a partir das condições experimentais, para o entendimento da formação dos grânulos para liberação do composto derivado tiofênico 5CN06, com ação antifúngica.Research, Society and Development2022-10-18info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://rsdjournal.org/index.php/rsd/article/view/3589810.33448/rsd-v11i14.35898Research, Society and Development; Vol. 11 No. 14; e26111435898Research, Society and Development; Vol. 11 Núm. 14; e26111435898Research, Society and Development; v. 11 n. 14; e261114358982525-3409reponame:Research, Society and Developmentinstname:Universidade Federal de Itajubá (UNIFEI)instacron:UNIFEIporhttps://rsdjournal.org/index.php/rsd/article/view/35898/30093Copyright (c) 2022 Kaline de Araújo Medeiros; Michelle de Oliveira Pedrosa Rolim; Rayane Santa Cruz Martins de Queiroz Antonino ; Dayanne Tomaz Casimiro da Silva ; Francisco Jaime Bezerra Mendonça Junior; José Alexsandro da Silva; Bolívar Ponciano Goulart de Lima Damasceno https://creativecommons.org/licenses/by/4.0info:eu-repo/semantics/openAccessMedeiros, Kaline de AraújoRolim, Michelle de Oliveira PedrosaAntonino , Rayane Santa Cruz Martins de QueirozSilva , Dayanne Tomaz Casimiro da Mendonça Junior, Francisco Jaime Bezerra Silva, José Alexsandro daDamasceno , Bolívar Ponciano Goulart de Lima 2022-11-08T13:36:27Zoai:ojs.pkp.sfu.ca:article/35898Revistahttps://rsdjournal.org/index.php/rsd/indexPUBhttps://rsdjournal.org/index.php/rsd/oairsd.articles@gmail.com2525-34092525-3409opendoar:2024-01-17T09:50:38.657665Research, Society and Development - Universidade Federal de Itajubá (UNIFEI)false
dc.title.none.fl_str_mv Development of alginate granules for thiophenic derivative 5CN06 delivery by ionotropic gelation
Desarrollo de gránulos de alginato para la entrega del derivado tiofénico 5CN06 por gelificación ionotrópica
Desenvolvimento de grânulos de alginato para veiculação de derivado tiofênico 5CN06 por gelificação ionotrópica
title Development of alginate granules for thiophenic derivative 5CN06 delivery by ionotropic gelation
spellingShingle Development of alginate granules for thiophenic derivative 5CN06 delivery by ionotropic gelation
Medeiros, Kaline de Araújo
Grânulos
Derivado Tiofênico
Gelificação Ionotrópica
Alginato.
Granules
Thiophenic Derivative
Ionotropic Gelation
Alginate.
Gránulos
Derivado Tiofénico
Gelificación Ionotrópica
Alginato.
title_short Development of alginate granules for thiophenic derivative 5CN06 delivery by ionotropic gelation
title_full Development of alginate granules for thiophenic derivative 5CN06 delivery by ionotropic gelation
title_fullStr Development of alginate granules for thiophenic derivative 5CN06 delivery by ionotropic gelation
title_full_unstemmed Development of alginate granules for thiophenic derivative 5CN06 delivery by ionotropic gelation
title_sort Development of alginate granules for thiophenic derivative 5CN06 delivery by ionotropic gelation
author Medeiros, Kaline de Araújo
author_facet Medeiros, Kaline de Araújo
Rolim, Michelle de Oliveira Pedrosa
Antonino , Rayane Santa Cruz Martins de Queiroz
Silva , Dayanne Tomaz Casimiro da
Mendonça Junior, Francisco Jaime Bezerra
Silva, José Alexsandro da
Damasceno , Bolívar Ponciano Goulart de Lima
author_role author
author2 Rolim, Michelle de Oliveira Pedrosa
Antonino , Rayane Santa Cruz Martins de Queiroz
Silva , Dayanne Tomaz Casimiro da
Mendonça Junior, Francisco Jaime Bezerra
Silva, José Alexsandro da
Damasceno , Bolívar Ponciano Goulart de Lima
author2_role author
author
author
author
author
author
dc.contributor.author.fl_str_mv Medeiros, Kaline de Araújo
Rolim, Michelle de Oliveira Pedrosa
Antonino , Rayane Santa Cruz Martins de Queiroz
Silva , Dayanne Tomaz Casimiro da
Mendonça Junior, Francisco Jaime Bezerra
Silva, José Alexsandro da
Damasceno , Bolívar Ponciano Goulart de Lima
dc.subject.por.fl_str_mv Grânulos
Derivado Tiofênico
Gelificação Ionotrópica
Alginato.
Granules
Thiophenic Derivative
Ionotropic Gelation
Alginate.
Gránulos
Derivado Tiofénico
Gelificación Ionotrópica
Alginato.
topic Grânulos
Derivado Tiofênico
Gelificação Ionotrópica
Alginato.
Granules
Thiophenic Derivative
Ionotropic Gelation
Alginate.
Gránulos
Derivado Tiofénico
Gelificación Ionotrópica
Alginato.
description The use of biodegradable polysaccharides with gel forming capacity to produce granules has been reported, but there are no reports in the literature associated with new 2-aminothiophene derivatives, which have demonstrated selective antifungal biological activity. Thus, the objective of this study was to evaluate the formation of alginate granules for the delivery of the thiophenic derivative and Active Pharmaceutical Ingredient (API) 5CN06 by ionotropic gelation. An emulsion of 0.1% 5CN06, a 3% sodium alginate solution and a 10% CaCl2 solution was produced. The emulsion and the alginate were mixed under different volumes and, under drip, in the CaCl2 solution, the granules were formed. Changing the proportion of polymer interferes with this yield, which is equal to and above 79.50% ± 0.03. In acid medium, pH 1.2, the granule does not have a significant swelling rate after 180 min. In a pH 7.4 medium it dissolves due to the presence of Na+. Using 10 ml of the emulsion mixtures containing the drug and 10 ml of 3% sodium alginate solution, granules were obtained with better encapsulation efficiency (65.7%). The higher mixing ratio interfered in the swelling capacity and in the thermal stabilization of the drug. Thus, the study of this system was promising, from the experimental conditions, for the understanding of the formation of granules to release the thiophenic derivative compound 5CN06, with antifungal action.
publishDate 2022
dc.date.none.fl_str_mv 2022-10-18
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv https://rsdjournal.org/index.php/rsd/article/view/35898
10.33448/rsd-v11i14.35898
url https://rsdjournal.org/index.php/rsd/article/view/35898
identifier_str_mv 10.33448/rsd-v11i14.35898
dc.language.iso.fl_str_mv por
language por
dc.relation.none.fl_str_mv https://rsdjournal.org/index.php/rsd/article/view/35898/30093
dc.rights.driver.fl_str_mv https://creativecommons.org/licenses/by/4.0
info:eu-repo/semantics/openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by/4.0
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Research, Society and Development
publisher.none.fl_str_mv Research, Society and Development
dc.source.none.fl_str_mv Research, Society and Development; Vol. 11 No. 14; e26111435898
Research, Society and Development; Vol. 11 Núm. 14; e26111435898
Research, Society and Development; v. 11 n. 14; e26111435898
2525-3409
reponame:Research, Society and Development
instname:Universidade Federal de Itajubá (UNIFEI)
instacron:UNIFEI
instname_str Universidade Federal de Itajubá (UNIFEI)
instacron_str UNIFEI
institution UNIFEI
reponame_str Research, Society and Development
collection Research, Society and Development
repository.name.fl_str_mv Research, Society and Development - Universidade Federal de Itajubá (UNIFEI)
repository.mail.fl_str_mv rsd.articles@gmail.com
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