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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| Format: | Article |
| Language: | English |
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Dove Medical Press
2019-12-01
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| Series: | International Journal of Nanomedicine |
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| Online Access: | https://www.dovepress.com/effects-of-surface-characteristics-of-polymeric-nanocapsules-on-the-ph-peer-reviewed-article-IJN |
| _version_ | 1818751129106776064 |
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| 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 |
| collection | DOAJ |
| 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
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| first_indexed | 2024-12-18T04:30:39Z |
| format | Article |
| id | doaj.art-5306bdae8f564ab58d0afdc20212400d |
| institution | Directory Open Access Journal |
| issn | 1178-2013 |
| language | English |
| last_indexed | 2024-12-18T04:30:39Z |
| publishDate | 2019-12-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | International Journal of Nanomedicine |
| spelling | doaj.art-5306bdae8f564ab58d0afdc20212400d2022-12-21T21:20:59ZengDove Medical PressInternational Journal of Nanomedicine1178-20132019-12-01Volume 14101651017850810Effects of Surface Characteristics of Polymeric Nanocapsules on the Pharmacokinetics and Efficacy of Antimalarial QuinineMichels LRMaciel TRNakama KATeixeira FEGCarvalho FBGundel AAraujo BVHaas SELuana 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 https://www.dovepress.com/effects-of-surface-characteristics-of-polymeric-nanocapsules-on-the-ph-peer-reviewed-article-IJNquininemalariananocapsulesnanospheresantimalarial efficacy. |
| spellingShingle | 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 International Journal of Nanomedicine quinine malaria nanocapsules nanospheres antimalarial efficacy. |
| title | 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_short | 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 |
| topic | quinine malaria nanocapsules nanospheres antimalarial efficacy. |
| url | https://www.dovepress.com/effects-of-surface-characteristics-of-polymeric-nanocapsules-on-the-ph-peer-reviewed-article-IJN |
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