Development of alginate granules for thiophenic derivative 5CN06 delivery by ionotropic gelation
Autor(a) principal: | |
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Data de Publicação: | 2022 |
Outros Autores: | , , , , , |
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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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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1797052725832187904 |