Solid dispersions of leaves Eugenia florida (Myrtaceae) extracts to optimize the solubility of the betulinic acid marker
Autor(a) principal: | |
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Data de Publicação: | 2021 |
Outros Autores: | , , , |
Tipo de documento: | Artigo |
Idioma: | por |
Título da fonte: | Revista Fitos |
Texto Completo: | https://revistafitos.far.fiocruz.br/index.php/revista-fitos/article/view/1070 |
Resumo: | Eugenia florida DC belongs to the family Myrtaceae. Previous phytochemical studies with extracts of E. florida leaves showed the occurrence of triterpenes and, among its constituents, the betulinic acid (BA), which presents a vast literature with different biological activities, such as anti-inflammatory, antimalarial, antimicrobial, antiviral and anticancer, however, its low aqueous solubility limits its bioavailability. In order to increase bioavailability, the use of solid dispersions is highlighted, where lipophilic drugs are dispersed in hydrophilic carriers, causing increase in solubility and dissolution profile. In this work, solid dispersions containing extracts of E. florida were prepared using the carrier Gelucire®50/13 as a polymeric agent and lactose monohydrate as a hydrophilic support using the fusion technique. The system that showed better BA solubility was characterized by Fourier Transform Infrared Spectroscopy (FTIR), Thermogravimetric Analysis (TGA), Differential Scanning Calorimetry (DSC) and X-Ray Diffractometry (DRX). The solid dispersion technique elevated the solubility of betulinic acid in Eugenia florida leaf extract eleven times, suggesting an increase in the bioavailability of the marker. |
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Solid dispersions of leaves Eugenia florida (Myrtaceae) extracts to optimize the solubility of the betulinic acid markerDispersões sólidas de extratos de folhas de Eugenia florida DC. (Myrtaceae) para otimização da solubilidade do marcador ácido betulínicoDispersões SólidasSolubilidadeÁcido BetulínicoEugenia floridaSolid DispersionsSolubilityBetulinic AcidEugenia floridaEugenia florida DC belongs to the family Myrtaceae. Previous phytochemical studies with extracts of E. florida leaves showed the occurrence of triterpenes and, among its constituents, the betulinic acid (BA), which presents a vast literature with different biological activities, such as anti-inflammatory, antimalarial, antimicrobial, antiviral and anticancer, however, its low aqueous solubility limits its bioavailability. In order to increase bioavailability, the use of solid dispersions is highlighted, where lipophilic drugs are dispersed in hydrophilic carriers, causing increase in solubility and dissolution profile. In this work, solid dispersions containing extracts of E. florida were prepared using the carrier Gelucire®50/13 as a polymeric agent and lactose monohydrate as a hydrophilic support using the fusion technique. The system that showed better BA solubility was characterized by Fourier Transform Infrared Spectroscopy (FTIR), Thermogravimetric Analysis (TGA), Differential Scanning Calorimetry (DSC) and X-Ray Diffractometry (DRX). The solid dispersion technique elevated the solubility of betulinic acid in Eugenia florida leaf extract eleven times, suggesting an increase in the bioavailability of the marker.Eugenia florida DC. pertence à família Myrtaceae. Estudos fitoquímicos anteriores com extratos de folhas de E. florida revelaram a ocorrência de triterpenos e, entre seus constituintes, o ácido betulínico (AB), que apresenta uma vasta literatura com diferentes atividades biológicas, como anti-inflamatório, antimalárico, antimicrobiano, antiviral e anticâncer, porém, sua baixa solubilidade aquosa limita a sua biodisponibilidade. Para o aumento da biodisponibilidade tem destaque o uso de disperões sólidas, onde fármacos lipofílicos são dispersos em carreadores hidrofílicos, acarretando um aumento da solubilidade e perfil de dissolução. Neste trabalho, dispersões sólidas contendo extratos de E. florida foram preparados utilizando o carreador Gelucire®50/13 como agente polímerérico e a lactose monohidratada como suporte hidrofílico empregando a técnica de fusão. O sistema que apresentou melhor solubilidade de AB foi caracterizado através das técnicas de espectroscopia do Infravermelho com Transformada de Fourier (FTIR), Análise de Termogravimetria (TGA), Calorimetria Exploratória Diferencial (DSC) e Difratometria de Raios-X (DRX). A técnica de dispersão sólida aumentou onze vezes a solubilidade do ácido betulínico presente no extrato de folhas de Eugenia florida DC. (Myrtaceae), sugerindo o aumento da biodisponibilidade do marcador.Centro de Inovação em Biodiversidade e Saúde - Farmanguinhos/Fiocruz2021-12-17info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdftext/htmltext/xmlhttps://revistafitos.far.fiocruz.br/index.php/revista-fitos/article/view/107010.32712/2446-4775.2021.1070Revista Fitos; Vol. 15 No. 4 (2021); 456-473Revista Fitos; Vol. 15 Núm. 4 (2021); 456-473Revista Fitos; v. 15 n. 4 (2021); 456-4732446-47751808-9569reponame:Revista Fitosinstname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZporhttps://revistafitos.far.fiocruz.br/index.php/revista-fitos/article/view/1070/911https://revistafitos.far.fiocruz.br/index.php/revista-fitos/article/view/1070/912https://revistafitos.far.fiocruz.br/index.php/revista-fitos/article/view/1070/983Copyright (c) 2021 Revista Fitosinfo:eu-repo/semantics/openAccessNóbrega, Andréa Bezerra daBizarri, Carlos Henrique BrasilPaz, Andressa SantanaSeiceira, Rafael CardosoConceição, Edemilson Cardoso da2022-02-01T15:03:21Zoai:ojs.revistafitos.far.fiocruz.br:article/1070Revistahttps://revistafitos.far.fiocruz.br/index.php/revista-fitos/PUBhttp://revistafitos.far.fiocruz.br/index.php/revista-fitos/oairevistafitos@far.fiocruz.br || eugenio.telles@far.fiocruz.br2446-47752446-4775opendoar:2022-02-01T15:03:21Revista Fitos - Fundação Oswaldo Cruz (FIOCRUZ)false |
dc.title.none.fl_str_mv |
Solid dispersions of leaves Eugenia florida (Myrtaceae) extracts to optimize the solubility of the betulinic acid marker Dispersões sólidas de extratos de folhas de Eugenia florida DC. (Myrtaceae) para otimização da solubilidade do marcador ácido betulínico |
title |
Solid dispersions of leaves Eugenia florida (Myrtaceae) extracts to optimize the solubility of the betulinic acid marker |
spellingShingle |
Solid dispersions of leaves Eugenia florida (Myrtaceae) extracts to optimize the solubility of the betulinic acid marker Nóbrega, Andréa Bezerra da Dispersões Sólidas Solubilidade Ácido Betulínico Eugenia florida Solid Dispersions Solubility Betulinic Acid Eugenia florida |
title_short |
Solid dispersions of leaves Eugenia florida (Myrtaceae) extracts to optimize the solubility of the betulinic acid marker |
title_full |
Solid dispersions of leaves Eugenia florida (Myrtaceae) extracts to optimize the solubility of the betulinic acid marker |
title_fullStr |
Solid dispersions of leaves Eugenia florida (Myrtaceae) extracts to optimize the solubility of the betulinic acid marker |
title_full_unstemmed |
Solid dispersions of leaves Eugenia florida (Myrtaceae) extracts to optimize the solubility of the betulinic acid marker |
title_sort |
Solid dispersions of leaves Eugenia florida (Myrtaceae) extracts to optimize the solubility of the betulinic acid marker |
author |
Nóbrega, Andréa Bezerra da |
author_facet |
Nóbrega, Andréa Bezerra da Bizarri, Carlos Henrique Brasil Paz, Andressa Santana Seiceira, Rafael Cardoso Conceição, Edemilson Cardoso da |
author_role |
author |
author2 |
Bizarri, Carlos Henrique Brasil Paz, Andressa Santana Seiceira, Rafael Cardoso Conceição, Edemilson Cardoso da |
author2_role |
author author author author |
dc.contributor.author.fl_str_mv |
Nóbrega, Andréa Bezerra da Bizarri, Carlos Henrique Brasil Paz, Andressa Santana Seiceira, Rafael Cardoso Conceição, Edemilson Cardoso da |
dc.subject.por.fl_str_mv |
Dispersões Sólidas Solubilidade Ácido Betulínico Eugenia florida Solid Dispersions Solubility Betulinic Acid Eugenia florida |
topic |
Dispersões Sólidas Solubilidade Ácido Betulínico Eugenia florida Solid Dispersions Solubility Betulinic Acid Eugenia florida |
description |
Eugenia florida DC belongs to the family Myrtaceae. Previous phytochemical studies with extracts of E. florida leaves showed the occurrence of triterpenes and, among its constituents, the betulinic acid (BA), which presents a vast literature with different biological activities, such as anti-inflammatory, antimalarial, antimicrobial, antiviral and anticancer, however, its low aqueous solubility limits its bioavailability. In order to increase bioavailability, the use of solid dispersions is highlighted, where lipophilic drugs are dispersed in hydrophilic carriers, causing increase in solubility and dissolution profile. In this work, solid dispersions containing extracts of E. florida were prepared using the carrier Gelucire®50/13 as a polymeric agent and lactose monohydrate as a hydrophilic support using the fusion technique. The system that showed better BA solubility was characterized by Fourier Transform Infrared Spectroscopy (FTIR), Thermogravimetric Analysis (TGA), Differential Scanning Calorimetry (DSC) and X-Ray Diffractometry (DRX). The solid dispersion technique elevated the solubility of betulinic acid in Eugenia florida leaf extract eleven times, suggesting an increase in the bioavailability of the marker. |
publishDate |
2021 |
dc.date.none.fl_str_mv |
2021-12-17 |
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://revistafitos.far.fiocruz.br/index.php/revista-fitos/article/view/1070 10.32712/2446-4775.2021.1070 |
url |
https://revistafitos.far.fiocruz.br/index.php/revista-fitos/article/view/1070 |
identifier_str_mv |
10.32712/2446-4775.2021.1070 |
dc.language.iso.fl_str_mv |
por |
language |
por |
dc.relation.none.fl_str_mv |
https://revistafitos.far.fiocruz.br/index.php/revista-fitos/article/view/1070/911 https://revistafitos.far.fiocruz.br/index.php/revista-fitos/article/view/1070/912 https://revistafitos.far.fiocruz.br/index.php/revista-fitos/article/view/1070/983 |
dc.rights.driver.fl_str_mv |
Copyright (c) 2021 Revista Fitos info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
Copyright (c) 2021 Revista Fitos |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf text/html text/xml |
dc.publisher.none.fl_str_mv |
Centro de Inovação em Biodiversidade e Saúde - Farmanguinhos/Fiocruz |
publisher.none.fl_str_mv |
Centro de Inovação em Biodiversidade e Saúde - Farmanguinhos/Fiocruz |
dc.source.none.fl_str_mv |
Revista Fitos; Vol. 15 No. 4 (2021); 456-473 Revista Fitos; Vol. 15 Núm. 4 (2021); 456-473 Revista Fitos; v. 15 n. 4 (2021); 456-473 2446-4775 1808-9569 reponame:Revista Fitos instname:Fundação Oswaldo Cruz (FIOCRUZ) instacron:FIOCRUZ |
instname_str |
Fundação Oswaldo Cruz (FIOCRUZ) |
instacron_str |
FIOCRUZ |
institution |
FIOCRUZ |
reponame_str |
Revista Fitos |
collection |
Revista Fitos |
repository.name.fl_str_mv |
Revista Fitos - Fundação Oswaldo Cruz (FIOCRUZ) |
repository.mail.fl_str_mv |
revistafitos@far.fiocruz.br || eugenio.telles@far.fiocruz.br |
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1798313475504603136 |