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dc.contributor.authorMichels, Luana Robertapt_BR
dc.contributor.authorMaciel, Tamara Ramospt_BR
dc.contributor.authorNakama, Kelly Ayumipt_BR
dc.contributor.authorTeixeira, Flávia Elizabete Guerrapt_BR
dc.contributor.authorCarvalho, Felipe Barbosa dept_BR
dc.contributor.authorGündel, Andrépt_BR
dc.contributor.authorAraújo, Bibiana Verlindo dept_BR
dc.contributor.authorHaas, Sandra Elisapt_BR
dc.date.accessioned2022-10-03T04:49:14Zpt_BR
dc.date.issued2019pt_BR
dc.identifier.issn1178-2013pt_BR
dc.identifier.urihttp://hdl.handle.net/10183/249651pt_BR
dc.description.abstractIntroduction: The surface charge of nanoparticles, such as nanospheres (NS) and nanocapsules (NC), has been studied with the purpose of improving the in vivo performance of drugs. The aim of this study was to develop, characterize, and evaluate the in vitro antimalarial efficacy of NCP80 and NSP80 (polysorbate coated) or NCEUD and NSEUD (prepared with Eudragit RS 100) loading quinine (QN). Methods: Formulations were prepared by the nanoprecipitation method, followed by wide physicochemical characterization. Antimalarial activity in Plasmodium berghei-infected mice and populational pharmacokinetics (PopPK) in rats were evaluated. Results: The formulations showed a nanometric range (between 138 ± 3.8 to 201 ± 23.0 nm), zeta potential (mV) of −33.1 ± 0.7 (NCP80), −30.5 ± 1 (UNCP80), −25.5 ± 1 (NSP80), −20 ± 0.3 (UNSP80), 4.61 ± 1 (NCEUD), 14.1 ± 0.9 (UNCEUD), 2.86 ± 0.3 (NSEUD) and 2.84 ± 0.6 (UNSEUD), content close to 100%, and good QN protection against UVA light. There was a twofold increase in the penetration of QN into infected erythrocytes with NC compared to that with NS. There was a significant increase in t1/2 for all NC evaluated compared to that of Free-QN, due to changes in Vdss. PopPK analysis showed that NCP80 acted as a covariate to Q (intercompartmental clearance) and V2 (volume of distribution in the peripheral compartment). For NCEUD, V1 and Q were modified after QN nanoencapsulation. Regarding in vivo efficacy, NCEUD increased the survival of mice unlike Free-QN. Conclusion: Cationic nanocapsules modified the pharmacology of QN, presenting a potential alternative for malaria treatment.en
dc.format.mimetypeapplication/pdfpt_BR
dc.language.isoengpt_BR
dc.relation.ispartofInternational journal of nanomedicine. Manchester. Vol. 14 (2019), p. 10165–10178pt_BR
dc.rightsOpen Accessen
dc.subjectQuinineen
dc.subjectQuininapt_BR
dc.subjectNanocapsulesen
dc.subjectMaláriapt_BR
dc.subjectNanospheresen
dc.subjectNanocápsulaspt_BR
dc.subjectNanosferaspt_BR
dc.subjectAntimalarial efficacyen
dc.subjectAntimaláricospt_BR
dc.titleEffects of surface characteristics of polymeric nanocapsules on the pharmacokinetics and efficacy of antimalarial quininept_BR
dc.typeArtigo de periódicopt_BR
dc.identifier.nrb001149058pt_BR
dc.type.originEstrangeiropt_BR


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