Solid dispersions of leaves Eugenia florida (Myrtaceae) extracts to optimize the solubility of the betulinic acid marker

Detalhes bibliográficos
Autor(a) principal: Nóbrega, Andréa Bezerra da
Data de Publicação: 2021
Outros Autores: Bizarri, Carlos Henrique Brasil, Paz, Andressa Santana, Seiceira, Rafael Cardoso, Conceição, Edemilson Cardoso da
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.
id FIOCRUZ-1_2e784864b9c5b4724c440a91e624beb1
oai_identifier_str oai:ojs.revistafitos.far.fiocruz.br:article/1070
network_acronym_str FIOCRUZ-1
network_name_str Revista Fitos
repository_id_str
spelling 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
_version_ 1798313475504603136