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

2024-11-01Research article Open access
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dc.contributor.authorSilva, Ana Teresa
dc.contributor.authorPrudêncio, Miguel
dc.contributor.authorOliveira, Isabel S.
dc.contributor.authorNogueira, Fátima
dc.contributor.authorMorais, Inês
dc.contributor.authorSantana, Sofia
dc.contributor.authorFerraz, Ricardo
dc.contributor.authorWorkneh, Eyob A.
dc.contributor.authorGomes, Paula
dc.contributor.authorMarques, Eduardo F.
dc.contributor.authorFerraz, Ricardo
dc.date.accessioned2025-07-08T08:26:11Z
dc.date.available2025-07-08T08:26:11Z
dc.date.issued2024-11-01
dc.description.abstractColloidal 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.por
dc.identifier.citationSilva, A. T., Oliveira, I. S., Morais, I., Santana, S., Workneh, E. A., Prudêncio, M., Nogueira, F., Ferraz, R., Gomes, P., & Marques, E. F. (2024). High efficacy of chloroquine-derived bile salts in Pluronic F127 micelles against blood-stage Plasmodium falciparum. Journal of Molecular Liquids, 413, 125986. https://doi.org/10.1016/j.molliq.2024.125986
dc.identifier.doi10.1016/j.molliq.2024.125986
dc.identifier.eissn1873-3166
dc.identifier.issn0167-7322
dc.identifier.urihttp://hdl.handle.net/10400.22/30197
dc.language.isoeng
dc.peerreviewedyes
dc.publisherElsevier
dc.relationCIRCNA/BRB/0281/2019; 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); SFRH/BD/150649/2020 and 2023.03356.BD;
dc.relation.hasversionhttps://www.sciencedirect.com/science/article/pii/S0167732224020452?via%3Dihub
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/
dc.subjectAntimalarial drugs
dc.subjectSurface-active ionic liquids
dc.subjectChloroquine & bile salts
dc.subjectPolymeric and mixed micelles
dc.subjectDrug nanocarriers
dc.subjectAntiplasmodial activity
dc.titleHigh efficacy of chloroquine-derived bile salts in Pluronic F127 micelles against blood-stage Plasmodium falciparumpor
dc.typeresearch article
dspace.entity.typePublication
oaire.citation.titleJournal of Molecular Liquids
oaire.citation.volume413
oaire.versionhttp://purl.org/coar/version/c_970fb48d4fbd8a85
person.familyNameFerraz
person.givenNameRicardo
person.identifier.ciencia-id001E-71CE-F92D
person.identifier.orcid0000-0002-1761-117X
person.identifier.ridG-5639-2011
person.identifier.scopus-author-id24464208500
relation.isAuthorOfPublicationa5a8faa7-12a5-4b1c-bced-44c895677397
relation.isAuthorOfPublication.latestForDiscoverya5a8faa7-12a5-4b1c-bced-44c895677397

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