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Synthesis and biological evaluation of Amphotericin B formulations based on organic salts and ionic liquids against Leishmania infantum

2022-12-19Journal article Open access
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dc.contributor.authorFerraz, Ricardo
dc.contributor.authorSantarém, Nuno
dc.contributor.authorSantos, Andreia F. M.
dc.contributor.authorJacinto, Manuel L.
dc.contributor.authorCordeiro-da-Silva, Anabela
dc.contributor.authorPrudêncio, Cristina
dc.contributor.authorNoronha, João Paulo
dc.contributor.authorBranco, Luis C.
dc.contributor.authorPetrovski, Željko
dc.date.accessioned2023-02-01T15:01:30Z
dc.date.available2023-02-01T15:01:30Z
dc.date.issued2022-12-19
dc.description.abstractNowadays, organic salts and ionic liquids (OSILs) containing active pharmaceutical ingredients (APIs) are being explored as drug delivery systems in modern therapies (OSILs-API). In that sense, this work is focused on the development of novel OSILs-API based on amphotericin B through an innovative procedure and the evaluation of the respective biological activity against Leishmania infantum. Several ammonium, methylimidazolium, pyridinium and phosphonium organic cations combined with amphotericin B as anion were synthesized in moderate to high yields and high purities by the water-reduced buffer neutralization method. All prepared compounds were characterized to confirm the desired chemical structure and the specific optical rotation ([α]D25) was also determined. The biological assays performed on L. infantum promastigotes showed increased activity against this parasitic disease when compared with the starting chloride forms and amphotericin B alone, highlighting [P6,6,6,14][AmB] as the most promising formulation. Possible synergism in the antiprotozoal activity was also evaluated for [P6,6,6,14][AmB], since it was proven to be the compound with the highest toxicity. This work reported a simple synthetic method, which can be applied to prepare other organic salts based on molecules containing fragile chemical groups, demonstrating the potential of these OSILs-AmB as possible agents against leishmaniasis.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationFerraz, R., Santarém, N., Santos, A. F. M., Jacinto, M. L., Cordeiro-da-Silva, A., Prudêncio, C., Noronha, J. P., Branco, L. C., & Petrovski, Ž. (2022). Synthesis and Biological Evaluation of Amphotericin B Formulations Based on Organic Salts and Ionic Liquids against Leishmania infantum. Antibiotics, 11(12), 1841. https://doi.org/10.3390/antibiotics11121841pt_PT
dc.identifier.doi10.3390/antibiotics11121841pt_PT
dc.identifier.eissn2079-6382
dc.identifier.urihttp://hdl.handle.net/10400.22/22069
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherMDPIpt_PT
dc.relation.publisherversionhttps://www.mdpi.com/2079-6382/11/12/1841pt_PT
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/pt_PT
dc.subjectOrganic salts and ionic liquidspt_PT
dc.subjectAmphotericin Bpt_PT
dc.subjectActive pharmaceutical ingredientspt_PT
dc.subjectLeishmania infantumpt_PT
dc.subjectLeishmaniasispt_PT
dc.titleSynthesis and biological evaluation of Amphotericin B formulations based on organic salts and ionic liquids against Leishmania infantumpt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.citation.endPage12pt_PT
oaire.citation.startPage1pt_PT
oaire.citation.titleAntibioticspt_PT
oaire.citation.volume11(12)pt_PT
person.familyNameFerraz
person.familyNamePrudêncio
person.givenNameRicardo
person.givenNameCristina
person.identifier1200571
person.identifier.ciencia-id001E-71CE-F92D
person.identifier.ciencia-idC81E-F4EE-FADE
person.identifier.orcid0000-0002-1761-117X
person.identifier.orcid0000-0002-9920-936X
person.identifier.ridG-5639-2011
person.identifier.scopus-author-id24464208500
person.identifier.scopus-author-id6508057930
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
relation.isAuthorOfPublicationa5a8faa7-12a5-4b1c-bced-44c895677397
relation.isAuthorOfPublication881a8ad5-ab13-4e49-89f4-08ca61cc81e3
relation.isAuthorOfPublication.latestForDiscoverya5a8faa7-12a5-4b1c-bced-44c895677397

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