Effects of Surface Characteristics of Polymeric Nanocapsules on the Pharmacokinetics and Efficacy of Antimalarial Quinine

Luana Roberta Michels,1 Tamara Ramos Maciel,1 Kelly Ayumi Nakama,1 Flavia Elizabete Guerra Teixeira,1 Felipe Barbosa de Carvalho,1 André Gundel,2 Bibiana Verlindo de Araujo,3 Sandra Elisa Haas1 1Pharmaceutical Sciences Post Graduate Program, Pharmacy Course, Federal University of Pampa, U...

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Autores principales:	Michels LR, Maciel TR, Nakama KA, Teixeira FEG, Carvalho FB, Gundel A, Araujo BV, Haas SE
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	quinine malaria nanocapsules nanospheres antimalarial efficacy. Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/5306bdae8f564ab58d0afdc20212400d
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spelling	oai:doaj.org-article:5306bdae8f564ab58d0afdc20212400d2021-12-02T00:43:44ZEffects of Surface Characteristics of Polymeric Nanocapsules on the Pharmacokinetics and Efficacy of Antimalarial Quinine1178-2013https://doaj.org/article/5306bdae8f564ab58d0afdc20212400d2019-12-01T00:00:00Zhttps://www.dovepress.com/effects-of-surface-characteristics-of-polymeric-nanocapsules-on-the-ph-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Luana Roberta Michels,1 Tamara Ramos Maciel,1 Kelly Ayumi Nakama,1 Flavia Elizabete Guerra Teixeira,1 Felipe Barbosa de Carvalho,1 André Gundel,2 Bibiana Verlindo de Araujo,3 Sandra Elisa Haas1 1Pharmaceutical Sciences Post Graduate Program, Pharmacy Course, Federal University of Pampa, UNIPAMPA, Uruguaiana, RS, Brazil; 2Campus Bagé, Federal University of Pampa, UNIPAMPA, Bagé, RS 1650, Brazil; 3Pharmaceutical Sciences Post Graduate Program, College of Pharmacy, Federal University of Rio Grande do Sul, Porto Alegre, RS 2752, BrazilCorrespondence: Sandra Elisa HaasCurso de Farmácia, Universidade Federal do Pampa, UNIPAMPA, Uruguaiana, BrazilTel +55 55 39110200Email sandrahaas@unipampa.edu.brIntroduction: 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.Keywords: quinine, malaria, nanocapsules, nanospheres, antimalarial efficacy  Michels LRMaciel TRNakama KATeixeira FEGCarvalho FBGundel AAraujo BVHaas SEDove Medical Pressarticlequininemalariananocapsulesnanospheresantimalarial efficacy.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 10165-10178 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	quinine malaria nanocapsules nanospheres antimalarial efficacy. Medicine (General) R5-920
spellingShingle	quinine malaria nanocapsules nanospheres antimalarial efficacy. Medicine (General) R5-920 Michels LR Maciel TR Nakama KA Teixeira FEG Carvalho FB Gundel A Araujo BV Haas SE Effects of Surface Characteristics of Polymeric Nanocapsules on the Pharmacokinetics and Efficacy of Antimalarial Quinine
description	Luana Roberta Michels,1 Tamara Ramos Maciel,1 Kelly Ayumi Nakama,1 Flavia Elizabete Guerra Teixeira,1 Felipe Barbosa de Carvalho,1 André Gundel,2 Bibiana Verlindo de Araujo,3 Sandra Elisa Haas1 1Pharmaceutical Sciences Post Graduate Program, Pharmacy Course, Federal University of Pampa, UNIPAMPA, Uruguaiana, RS, Brazil; 2Campus Bagé, Federal University of Pampa, UNIPAMPA, Bagé, RS 1650, Brazil; 3Pharmaceutical Sciences Post Graduate Program, College of Pharmacy, Federal University of Rio Grande do Sul, Porto Alegre, RS 2752, BrazilCorrespondence: Sandra Elisa HaasCurso de Farmácia, Universidade Federal do Pampa, UNIPAMPA, Uruguaiana, BrazilTel +55 55 39110200Email sandrahaas@unipampa.edu.brIntroduction: 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.Keywords: quinine, malaria, nanocapsules, nanospheres, antimalarial efficacy
format	article
author	Michels LR Maciel TR Nakama KA Teixeira FEG Carvalho FB Gundel A Araujo BV Haas SE
author_facet	Michels LR Maciel TR Nakama KA Teixeira FEG Carvalho FB Gundel A Araujo BV Haas SE
author_sort	Michels LR
title	Effects of Surface Characteristics of Polymeric Nanocapsules on the Pharmacokinetics and Efficacy of Antimalarial Quinine
title_short	Effects of Surface Characteristics of Polymeric Nanocapsules on the Pharmacokinetics and Efficacy of Antimalarial Quinine
title_full	Effects of Surface Characteristics of Polymeric Nanocapsules on the Pharmacokinetics and Efficacy of Antimalarial Quinine
title_fullStr	Effects of Surface Characteristics of Polymeric Nanocapsules on the Pharmacokinetics and Efficacy of Antimalarial Quinine
title_full_unstemmed	Effects of Surface Characteristics of Polymeric Nanocapsules on the Pharmacokinetics and Efficacy of Antimalarial Quinine
title_sort	effects of surface characteristics of polymeric nanocapsules on the pharmacokinetics and efficacy of antimalarial quinine
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/5306bdae8f564ab58d0afdc20212400d
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Effects of Surface Characteristics of Polymeric Nanocapsules on the Pharmacokinetics and Efficacy of Antimalarial Quinine

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