High efficacy of chloroquine-derived bile salts in Pluronic F127 micelles against blood-stage Plasmodium falciparum

Detalhes bibliográficos
Autor(a) principal: Silva, Ana Teresa
Data de Publicação: 2024
Outros Autores: Oliveira, Isabel S., Morais, Inês, Santana, Sofia, Workneh, Eyob A., Prudêncio, Miguel, Nogueira, Fátima, Ferraz, Ricardo, Gomes, Paula, Marques, Eduardo F.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10362/172746
Resumo: Funding Information: The authors thank Funda\u00E7\u00E3o para a Ci\u00EAncia e Tecnologia/Minist\u00E9rio da Educa\u00E7\u00E3o e Ci\u00EAncia \u2013 FCT/MEC, for PT national funds through the project CIRCNA/BRB/0281/2019. FCT/MCE is further acknowledged for supporting the Research Units LAQV-REQUIMTE (LA/P/0008/2020, UIDP/50006/2020 and UIDB/50006/2020), CIQUP (UIDB/00081/2020), IMS (LA/P/0056/2020), and GHTM (UID/Multi/04413/2020) and LA-REAL (LA/P/0117/2020). MP further acknowledges the \u201Cla Caixa\u201D Foundation for Grant HR21-848. ATS and IM thank both FCT/MCTES and Sociedade Portuguesa de Qu\u00EDmica (SPQ, Portugal) for their doctoral grants SFRH/BD/150649/2020 and 2023.03356.BD, respectively. The following reagent was obtained through BEI Resources, NIAID, NIH: Plasmodium falciparum, Strain 3D7HT-GFP, MRA-1029, contributed by Andrew M. Talman and Robert E. Sinden. Publisher Copyright: © 2024 The Author(s)
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spelling High efficacy of chloroquine-derived bile salts in Pluronic F127 micelles against blood-stage Plasmodium falciparumAntimalarial drugsAntiplasmodial activityChloroquine & bile saltsDrug nanocarriersPolymeric and mixed micellesSurface-active ionic liquidsElectronic, Optical and Magnetic MaterialsAtomic and Molecular Physics, and OpticsCondensed Matter PhysicsSpectroscopyPhysical and Theoretical ChemistryMaterials ChemistryFunding Information: The authors thank Funda\u00E7\u00E3o para a Ci\u00EAncia e Tecnologia/Minist\u00E9rio da Educa\u00E7\u00E3o e Ci\u00EAncia \u2013 FCT/MEC, for PT national funds through the project CIRCNA/BRB/0281/2019. FCT/MCE is further acknowledged for supporting the Research Units LAQV-REQUIMTE (LA/P/0008/2020, UIDP/50006/2020 and UIDB/50006/2020), CIQUP (UIDB/00081/2020), IMS (LA/P/0056/2020), and GHTM (UID/Multi/04413/2020) and LA-REAL (LA/P/0117/2020). MP further acknowledges the \u201Cla Caixa\u201D Foundation for Grant HR21-848. ATS and IM thank both FCT/MCTES and Sociedade Portuguesa de Qu\u00EDmica (SPQ, Portugal) for their doctoral grants SFRH/BD/150649/2020 and 2023.03356.BD, respectively. The following reagent was obtained through BEI Resources, NIAID, NIH: Plasmodium falciparum, Strain 3D7HT-GFP, MRA-1029, contributed by Andrew M. Talman and Robert E. Sinden. Publisher Copyright: © 2024 The Author(s)Colloidal nanocarriers can play a key role in the efficacious delivery of drugs, including antimalarials. Here, we investigated the ability of polymeric micelles of the block copolymer F127 to act as nanovehicles for two organic salts derived from chloroquine and human bile acids, namely, chloroquinium cholate (iCQP1) and chloroquinium glycocholate (iCQP1g). We have previously reported the strong in vitro antiplasmodial activity of these salts, which displayed IC50 values of 13 and 15 nM against blood forms of Plasmodium falciparum, respectively. By deriving from amphiphilic lipids, iCQP1 and iCQP1g also enclose the ability to act as surface-active ionic liquids (SAILs). The micellization properties of neat F127 and of the F127/SAIL mixtures were initially investigated to gain physicochemical insight into the interaction between polymer and bioactive SAILs, resorting to differential scanning calorimetry, surface tension measurements and dynamic light scattering. Micelle formation by F127 is an endothermic process strongly temperature and concentration dependent. Interestingly, this process is significantly changed when the molar fraction of SAIL (xSAIL) in the F127/SAIL mixture is varied between 0.33 and 0.90. Both SAILs favor the formation of mixed micelles by decreasing the micellization temperature, and (observed only when for xSAIL = 0.33) by synergistically decreasing the cmc. Concomitantly, the micellar size is reduced from 18 to 13 nm as xSAIL is increased from 0.33 to 0.90. Crucially, in vitro assays show that when the SAILs are loaded into F127 polymeric micelles, their antiplasmodial efficacy is substantially enhanced, with a significant drop in IC50, especially for the iCQP1/F127 system. This opens new possibilities for the nanoformulations of antimalarial compounds.Global Health and Tropical Medicine (GHTM)Instituto de Higiene e Medicina Tropical (IHMT)Vector borne diseases and pathogens (VBD)RUNSilva, Ana TeresaOliveira, Isabel S.Morais, InêsSantana, SofiaWorkneh, Eyob A.Prudêncio, MiguelNogueira, FátimaFerraz, RicardoGomes, PaulaMarques, Eduardo F.2024-09-30T22:32:46Z2024-11-012024-11-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10362/172746eng0167-7322PURE: 99998047https://doi.org/10.1016/j.molliq.2024.125986info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2024-10-07T01:39:24Zoai:run.unl.pt:10362/172746Portal AgregadorONGhttps://www.rcaap.pt/oai/openairemluisa.alvim@gmail.comopendoar:71602024-10-07T01:39:24Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv High efficacy of chloroquine-derived bile salts in Pluronic F127 micelles against blood-stage Plasmodium falciparum
title High efficacy of chloroquine-derived bile salts in Pluronic F127 micelles against blood-stage Plasmodium falciparum
spellingShingle High efficacy of chloroquine-derived bile salts in Pluronic F127 micelles against blood-stage Plasmodium falciparum
Silva, Ana Teresa
Antimalarial drugs
Antiplasmodial activity
Chloroquine & bile salts
Drug nanocarriers
Polymeric and mixed micelles
Surface-active ionic liquids
Electronic, Optical and Magnetic Materials
Atomic and Molecular Physics, and Optics
Condensed Matter Physics
Spectroscopy
Physical and Theoretical Chemistry
Materials Chemistry
title_short High efficacy of chloroquine-derived bile salts in Pluronic F127 micelles against blood-stage Plasmodium falciparum
title_full High efficacy of chloroquine-derived bile salts in Pluronic F127 micelles against blood-stage Plasmodium falciparum
title_fullStr High efficacy of chloroquine-derived bile salts in Pluronic F127 micelles against blood-stage Plasmodium falciparum
title_full_unstemmed High efficacy of chloroquine-derived bile salts in Pluronic F127 micelles against blood-stage Plasmodium falciparum
title_sort High efficacy of chloroquine-derived bile salts in Pluronic F127 micelles against blood-stage Plasmodium falciparum
author Silva, Ana Teresa
author_facet Silva, Ana Teresa
Oliveira, Isabel S.
Morais, Inês
Santana, Sofia
Workneh, Eyob A.
Prudêncio, Miguel
Nogueira, Fátima
Ferraz, Ricardo
Gomes, Paula
Marques, Eduardo F.
author_role author
author2 Oliveira, Isabel S.
Morais, Inês
Santana, Sofia
Workneh, Eyob A.
Prudêncio, Miguel
Nogueira, Fátima
Ferraz, Ricardo
Gomes, Paula
Marques, Eduardo F.
author2_role author
author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Global Health and Tropical Medicine (GHTM)
Instituto de Higiene e Medicina Tropical (IHMT)
Vector borne diseases and pathogens (VBD)
RUN
dc.contributor.author.fl_str_mv Silva, Ana Teresa
Oliveira, Isabel S.
Morais, Inês
Santana, Sofia
Workneh, Eyob A.
Prudêncio, Miguel
Nogueira, Fátima
Ferraz, Ricardo
Gomes, Paula
Marques, Eduardo F.
dc.subject.por.fl_str_mv Antimalarial drugs
Antiplasmodial activity
Chloroquine & bile salts
Drug nanocarriers
Polymeric and mixed micelles
Surface-active ionic liquids
Electronic, Optical and Magnetic Materials
Atomic and Molecular Physics, and Optics
Condensed Matter Physics
Spectroscopy
Physical and Theoretical Chemistry
Materials Chemistry
topic Antimalarial drugs
Antiplasmodial activity
Chloroquine & bile salts
Drug nanocarriers
Polymeric and mixed micelles
Surface-active ionic liquids
Electronic, Optical and Magnetic Materials
Atomic and Molecular Physics, and Optics
Condensed Matter Physics
Spectroscopy
Physical and Theoretical Chemistry
Materials Chemistry
description Funding Information: The authors thank Funda\u00E7\u00E3o para a Ci\u00EAncia e Tecnologia/Minist\u00E9rio da Educa\u00E7\u00E3o e Ci\u00EAncia \u2013 FCT/MEC, for PT national funds through the project CIRCNA/BRB/0281/2019. FCT/MCE is further acknowledged for supporting the Research Units LAQV-REQUIMTE (LA/P/0008/2020, UIDP/50006/2020 and UIDB/50006/2020), CIQUP (UIDB/00081/2020), IMS (LA/P/0056/2020), and GHTM (UID/Multi/04413/2020) and LA-REAL (LA/P/0117/2020). MP further acknowledges the \u201Cla Caixa\u201D Foundation for Grant HR21-848. ATS and IM thank both FCT/MCTES and Sociedade Portuguesa de Qu\u00EDmica (SPQ, Portugal) for their doctoral grants SFRH/BD/150649/2020 and 2023.03356.BD, respectively. The following reagent was obtained through BEI Resources, NIAID, NIH: Plasmodium falciparum, Strain 3D7HT-GFP, MRA-1029, contributed by Andrew M. Talman and Robert E. Sinden. Publisher Copyright: © 2024 The Author(s)
publishDate 2024
dc.date.none.fl_str_mv 2024-09-30T22:32:46Z
2024-11-01
2024-11-01T00:00:00Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10362/172746
url http://hdl.handle.net/10362/172746
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 0167-7322
PURE: 99998047
https://doi.org/10.1016/j.molliq.2024.125986
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.source.none.fl_str_mv reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron:RCAAP
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron_str RCAAP
institution RCAAP
reponame_str Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
collection Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository.name.fl_str_mv Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
repository.mail.fl_str_mv mluisa.alvim@gmail.com
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