Targeting Leishmania amazonensis amastigotes through macrophage internalisation of a hydroxymethylnitrofurazone nanostructured polymeric system

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dc.contributorSistema FMUSP-HC: Faculdade de Medicina da Universidade de São Paulo (FMUSP) e Hospital das Clínicas da FMUSP
dc.contributor.authorMONTEIRO, Lis Marie
dc.contributor.authorLOBENBERG, Raimar
dc.contributor.authorFERREIRA, Elizabeth Igne
dc.contributor.authorCOTRIM, Paulo Cesar
dc.contributor.authorKANASHIRO, Edite
dc.contributor.authorROCHA, Mussya
dc.contributor.authorCHUNG, Man Chin
dc.contributor.authorBOU-CHACRA, Nadia
dc.date.accessioned2017-10-24T13:18:19Z
dc.date.available2017-10-24T13:18:19Z
dc.date.issued2017
dc.description.abstractDextran-coated poly (n-butyl cyanoacrylate) nanoparticles (PBCA-NPs) were prepared and were evaluated for enhanced delivery of a promising anti-Leishmania drug candidate, hydroxymethylnitrofurazone (NFOH), to phagocytic cells. Currently available chemotherapy for leishmaniasis, such as pentavalent antimonials, presents low safety and efficacy. Furthermore, widespread drug resistance in leishmaniasis is rapidly emerging. To overcome these drawbacks, the use of nanosized delivery systems can reduce systemic drug toxicity and increase the drug concentration in infected macrophages, therefore improving treatment of leishmaniasis. PBCA-NPs containing NFOH (PBCA-NFOH-NPs) were prepared by an anionic emulsion polymerisation method. The z-average and polydispersity index (PDI) were determined by photon correlation spectroscopy, the zeta potential by microelectrophoresis and the entrapment efficiency by HPLC. Cytotoxicity was determined using macrophages from BALB/c mice. Efficacy tests were performed using Leishmania amazonensis promastigotes and amastigotes. The z-average of PBCA-NFOH-NPs was 151.5 +/- 61.97 nm, with a PDI of 0.104 +/- 0.01, a zeta potential of -10.1 +/- 6.49 mV and an entrapment efficiency of 64.47 +/- 0.43%. Efficacy in amastigotes revealed IC50 values of 0.33 mu M and 31.2 mu M for the nanostructured and free NFOH, respectively (95-fold increase). The cytotoxicity study indicated low toxicity of the PBCA-NFOH-NPs to macrophages. The selectivity index was 370.6, which is 49-fold higher than free NFOH (7.6). Such findings indicated that improved efficacy could be due to NP internalisation following site-specific drug delivery and reactivation of immune protective reactions by the NP components. Thus, PBCA-NFOH-NPs have the potential to significantly improve the treatment of leishmaniasis, with reduced systemic side effects.
dc.description.indexMEDLINE
dc.identifier.citationINTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS, v.50, n.1, p.88-92, 2017
dc.identifier.doi10.1016/j.ijantimicag.2017.01.033
dc.identifier.eissn1872-7913
dc.identifier.issn0924-8579
dc.identifier.urihttps://observatorio.fm.usp.br/handle/OPI/21920
dc.language.isoeng
dc.publisherELSEVIER SCIENCE BV
dc.relation.ispartofInternational Journal of Antimicrobial Agents
dc.rightsrestrictedAccess
dc.rights.holderCopyright ELSEVIER SCIENCE BV
dc.subjectHydroxymethylnitrofurazone
dc.subjectPoly (n-butyl cyanoacrylate)
dc.subjectLeishmaniasis
dc.subjectDrug delivery
dc.subjectPolymeric nanoparticles
dc.subjectDextran
dc.subject.othervisceral leishmaniasis
dc.subject.othernanoparticles
dc.subject.otherdelivery
dc.subject.otherdextran
dc.subject.otheracid
dc.subject.wosInfectious Diseases
dc.subject.wosMicrobiology
dc.subject.wosPharmacology & Pharmacy
dc.titleTargeting Leishmania amazonensis amastigotes through macrophage internalisation of a hydroxymethylnitrofurazone nanostructured polymeric system
dc.typearticle
dc.type.categoryoriginal article
dc.type.versionpublishedVersion
dspace.entity.typePublication
hcfmusp.affiliation.countryCanadá
hcfmusp.affiliation.countryisoca
hcfmusp.author.externalMONTEIRO, Lis Marie:Univ Sao Paulo, Fac Pharmaceut Sci, Pharm Dept, Sao Paulo, Brazil
hcfmusp.author.externalLOBENBERG, Raimar:Univ Alberta, Fac Pharm & Pharmaceut Sci, Edmonton, AB, Canada
hcfmusp.author.externalFERREIRA, Elizabeth Igne:Univ Sao Paulo, Fac Pharmaceut Sci, Pharm Dept, Sao Paulo, Brazil
hcfmusp.author.externalCHUNG, Man Chin:UNESP Araraquara, Fac Pharmaceut Sci, Sao Paulo, Brazil
hcfmusp.author.externalBOU-CHACRA, Nadia:Univ Sao Paulo, Fac Pharmaceut Sci, Pharm Dept, Sao Paulo, Brazil
hcfmusp.citation.scopus20
hcfmusp.contributor.author-fmusphcPAULO CESAR COTRIM
hcfmusp.contributor.author-fmusphcEDITE HATSUMI YAMASHIRO KANASHIRO
hcfmusp.contributor.author-fmusphcMUSSYA CISOTTO ROCHA
hcfmusp.description.beginpage88
hcfmusp.description.endpage92
hcfmusp.description.issue1
hcfmusp.description.volume50
hcfmusp.origemWOS
hcfmusp.origem.pubmed28454918
hcfmusp.origem.scopus2-s2.0-85019134582
hcfmusp.origem.wosWOS:000405983100014
hcfmusp.publisher.cityAMSTERDAM
hcfmusp.publisher.countryNETHERLANDS
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