Desenvolvimento de nanopartículas de quitosana contendo carvacrol frente a Leishmania infantum: estudo preliminar
Autor(a) principal: | |
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Data de Publicação: | 2022 |
Tipo de documento: | Dissertação |
Idioma: | por |
Título da fonte: | Biblioteca Digital de Teses e Dissertações da UFPB |
Texto Completo: | https://repositorio.ufpb.br/jspui/handle/123456789/26828 |
Resumo: | The Leishmaniases are neglected tropical infectious diseases caused by protozoa of the genus Leishmania and transmitted by sand flies (Lutzomyia). Visceral leishmaniasis (VL) is the most severe form of the disease. The treatment lines for VL include intravenously administered drugs that cause adverse effects in patients. Carvacrol (CAR), is a phenolic monoterpene that has shown strong activity against Leishmania spp. Chitosan (Chi) is a biopolymer with excellent chemical and biological properties, and acts as a component of several drug delivery systems in various therapies and in particular in anti-leishmania activity. Several studies have proposed the use of nanocarriers as delivery systems using polymeric chitosan nanoparticles, as a strategy to improve efficacy and safety in the treatment of leishmaniasis. The hypothesis of this study of CAR encapsulation in polymeric chitosan nanoparticles (NPChi) aims to answer whether its therapeutic effects can potentiate the treatment for leishmaniasis. Thus, the present work aimed to develop, characterize NPChi containing CAR (NPCar) and evaluate the anti-leishmania activity against L. infantum. The NPChi were prepared by the ionic gelation method varying the concentrations of Chi:TPP respectively between 0.05%, 0.1% and 0.2% and 0.05%, 0.1% and 0.5%, obtaining 9 samples. The in vitro activity assays were performed against promastigotes of L. infantum by the MTT test and the results were analyzed with the aid of GraphPad Prisma 5.0 software. Among the prepared formulations, sample A2 (0.1%Chi:0.05%TPP g/v), had the best results, with particle sizes at 89.43 ± 0.774 nm, polydispersity 0.168 and Zeta potential 12.8 mV. After encapsulation of the CAR (1mg/mL) in formulation A2, it showed a particle size of 245.9 nm, polydispersity 0.175 and the high zeta potential 15.4 mV. Preliminary analysis of in vitro antileishmania activity demonstrated strong inhibition of L. infantum promastigotes by NPCar with an IC50 of 2.659 μg/mL. The results of the present study demonstrate that the obtained NPCar maintain characteristics suitable for drug delivery systems with high homogeneity and stability, and preliminary studies in L. infantum demonstrated that NPCar may be promising candidates for visceral leishmaniasis. |
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Desenvolvimento de nanopartículas de quitosana contendo carvacrol frente a Leishmania infantum: estudo preliminarLeishmaniose VisceralMonoterpenosBiopolímerosNanobiotecnologiaNanocarreadoresVisceral LeishmaniasisMonoterpenesBiopolymersNanobiotechnologyNanocarriersCNPQ::CIENCIAS BIOLOGICAS::BIOLOGIA GERALThe Leishmaniases are neglected tropical infectious diseases caused by protozoa of the genus Leishmania and transmitted by sand flies (Lutzomyia). Visceral leishmaniasis (VL) is the most severe form of the disease. The treatment lines for VL include intravenously administered drugs that cause adverse effects in patients. Carvacrol (CAR), is a phenolic monoterpene that has shown strong activity against Leishmania spp. Chitosan (Chi) is a biopolymer with excellent chemical and biological properties, and acts as a component of several drug delivery systems in various therapies and in particular in anti-leishmania activity. Several studies have proposed the use of nanocarriers as delivery systems using polymeric chitosan nanoparticles, as a strategy to improve efficacy and safety in the treatment of leishmaniasis. The hypothesis of this study of CAR encapsulation in polymeric chitosan nanoparticles (NPChi) aims to answer whether its therapeutic effects can potentiate the treatment for leishmaniasis. Thus, the present work aimed to develop, characterize NPChi containing CAR (NPCar) and evaluate the anti-leishmania activity against L. infantum. The NPChi were prepared by the ionic gelation method varying the concentrations of Chi:TPP respectively between 0.05%, 0.1% and 0.2% and 0.05%, 0.1% and 0.5%, obtaining 9 samples. The in vitro activity assays were performed against promastigotes of L. infantum by the MTT test and the results were analyzed with the aid of GraphPad Prisma 5.0 software. Among the prepared formulations, sample A2 (0.1%Chi:0.05%TPP g/v), had the best results, with particle sizes at 89.43 ± 0.774 nm, polydispersity 0.168 and Zeta potential 12.8 mV. After encapsulation of the CAR (1mg/mL) in formulation A2, it showed a particle size of 245.9 nm, polydispersity 0.175 and the high zeta potential 15.4 mV. Preliminary analysis of in vitro antileishmania activity demonstrated strong inhibition of L. infantum promastigotes by NPCar with an IC50 of 2.659 μg/mL. The results of the present study demonstrate that the obtained NPCar maintain characteristics suitable for drug delivery systems with high homogeneity and stability, and preliminary studies in L. infantum demonstrated that NPCar may be promising candidates for visceral leishmaniasis.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPESAs Leishmanioses são doenças infeciosas tropicais negligenciadas causadas por protozoários do gênero Leishmania e transmito por flebotomíneos (Lutzomyia). A leishmaniose visceral (LV) é a forma mais grave da doença. As linhas de tratamento para a LV incluem fármacos administrados pela via intravenosa e que causam efeitos adversos nos pacientes. O carvacrol (CAR), é um monoterpeno fenólico que tem mostrado forte atividade frente à Leishmania spp. A quitosana (Qui) é um biopolímero com excelentes propriedades químicas e biológicas, e atua como componente de diversos sistemas de liberação de fármacos em diversas terapias e em especial na atividade anti-leishmania. Vários estudos têm como propostas a utilização de nanocarreadores como sistemas de liberação utilizando nanopartículas poliméricas de quitosana, como estratégia para a melhoria da eficácia e segurança no tratamento da leishmaniose. A hipótese desse estudo de encapsulação do CAR em nanoparticulas poliméricas de quitosana (NPQui) objetiva responder se os seus efeitos terapêuticos podem potencializar o tratamento para leishmaniose. Dessa forma, o presente trabalho teve como objetivo desenvolver, caracterizar NPQui contendo o CAR (NPCar) e avaliar a atividade in vitro frente a L. infantum. As NPQui foram preparadas pelo método da gelificação iônica variando as concentrações de Qui e tripolifosfato (TPP) respectivamente entre 0,05%, 0,1% e 0,2% e 0,05%, 0,1% e 0,5%, obtendo 9 amostras. Posteriormente, as amostras foram caracterizadas pelo tamanho de partículas, índice de polidispersão (Pdi) e potencial Zeta, com o objetivo de avaliação das características desejáveis para sistemas de liberação de fármacos. Os ensaios de atividade in vitro, foram realizados frente a formas promastigotas de L. infantum pelo teste de MTT e os resultados foram analisados com o auxílio Software GraphPad Prisma 5.0. Entre as formulações preparadas, a amostra A2 (0,1%Qui:0,05%TPP g/v), teve melhores resultados, com tamanhos de partículas em 89,43 ± 0,774 nm, índice de polidispersibilidade 0,168 e potencial Zeta 12,8 mV. Após a encapsulação do CAR (1mg/mL) na formulação A2, a mesma apresentou tamanho de partícula de 245,9 nm, índice de polidispersibilidade 0,175 e o potencial zeta alto 15,4 mV. A análise preliminar da atividade in vitro anti-leishmania demostrou uma forte inibição das formas promastigotas de L. infantum das NPCar com uma IC50 de 2,659 μg/mL. Os resultados do presente estudo demonstram que as NPCar obtidas mantêm as características adequadas para sistemas de liberação de fármacos com homogeneidade e estabilidade, e os estudos preliminares em formas promastigotas de L. infantum demonstraram que as NPCar podem ser candidatos promissores para a leishmaniose visceral.Universidade Federal da ParaíbaBrasilBiologia Celular e MolecularPrograma de Pós-Graduação em Biologia Celular e MolecularUFPBKretzschmar, Elisângela Afonso de Mourahttp://lattes.cnpq.br/8717450801163791Borges, Joyce Cordeiro2023-04-27T13:01:57Z2022-10-312023-04-27T13:01:57Z2022-03-09info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesishttps://repositorio.ufpb.br/jspui/handle/123456789/26828porAttribution-NoDerivs 3.0 Brazilhttp://creativecommons.org/licenses/by-nd/3.0/br/info:eu-repo/semantics/embargoedAccessreponame:Biblioteca Digital de Teses e Dissertações da UFPBinstname:Universidade Federal da Paraíba (UFPB)instacron:UFPB2023-05-11T06:04:24Zoai:repositorio.ufpb.br:123456789/26828Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufpb.br/PUBhttp://tede.biblioteca.ufpb.br:8080/oai/requestdiretoria@ufpb.br|| diretoria@ufpb.bropendoar:2023-05-11T06:04:24Biblioteca Digital de Teses e Dissertações da UFPB - Universidade Federal da Paraíba (UFPB)false |
dc.title.none.fl_str_mv |
Desenvolvimento de nanopartículas de quitosana contendo carvacrol frente a Leishmania infantum: estudo preliminar |
title |
Desenvolvimento de nanopartículas de quitosana contendo carvacrol frente a Leishmania infantum: estudo preliminar |
spellingShingle |
Desenvolvimento de nanopartículas de quitosana contendo carvacrol frente a Leishmania infantum: estudo preliminar Borges, Joyce Cordeiro Leishmaniose Visceral Monoterpenos Biopolímeros Nanobiotecnologia Nanocarreadores Visceral Leishmaniasis Monoterpenes Biopolymers Nanobiotechnology Nanocarriers CNPQ::CIENCIAS BIOLOGICAS::BIOLOGIA GERAL |
title_short |
Desenvolvimento de nanopartículas de quitosana contendo carvacrol frente a Leishmania infantum: estudo preliminar |
title_full |
Desenvolvimento de nanopartículas de quitosana contendo carvacrol frente a Leishmania infantum: estudo preliminar |
title_fullStr |
Desenvolvimento de nanopartículas de quitosana contendo carvacrol frente a Leishmania infantum: estudo preliminar |
title_full_unstemmed |
Desenvolvimento de nanopartículas de quitosana contendo carvacrol frente a Leishmania infantum: estudo preliminar |
title_sort |
Desenvolvimento de nanopartículas de quitosana contendo carvacrol frente a Leishmania infantum: estudo preliminar |
author |
Borges, Joyce Cordeiro |
author_facet |
Borges, Joyce Cordeiro |
author_role |
author |
dc.contributor.none.fl_str_mv |
Kretzschmar, Elisângela Afonso de Moura http://lattes.cnpq.br/8717450801163791 |
dc.contributor.author.fl_str_mv |
Borges, Joyce Cordeiro |
dc.subject.por.fl_str_mv |
Leishmaniose Visceral Monoterpenos Biopolímeros Nanobiotecnologia Nanocarreadores Visceral Leishmaniasis Monoterpenes Biopolymers Nanobiotechnology Nanocarriers CNPQ::CIENCIAS BIOLOGICAS::BIOLOGIA GERAL |
topic |
Leishmaniose Visceral Monoterpenos Biopolímeros Nanobiotecnologia Nanocarreadores Visceral Leishmaniasis Monoterpenes Biopolymers Nanobiotechnology Nanocarriers CNPQ::CIENCIAS BIOLOGICAS::BIOLOGIA GERAL |
description |
The Leishmaniases are neglected tropical infectious diseases caused by protozoa of the genus Leishmania and transmitted by sand flies (Lutzomyia). Visceral leishmaniasis (VL) is the most severe form of the disease. The treatment lines for VL include intravenously administered drugs that cause adverse effects in patients. Carvacrol (CAR), is a phenolic monoterpene that has shown strong activity against Leishmania spp. Chitosan (Chi) is a biopolymer with excellent chemical and biological properties, and acts as a component of several drug delivery systems in various therapies and in particular in anti-leishmania activity. Several studies have proposed the use of nanocarriers as delivery systems using polymeric chitosan nanoparticles, as a strategy to improve efficacy and safety in the treatment of leishmaniasis. The hypothesis of this study of CAR encapsulation in polymeric chitosan nanoparticles (NPChi) aims to answer whether its therapeutic effects can potentiate the treatment for leishmaniasis. Thus, the present work aimed to develop, characterize NPChi containing CAR (NPCar) and evaluate the anti-leishmania activity against L. infantum. The NPChi were prepared by the ionic gelation method varying the concentrations of Chi:TPP respectively between 0.05%, 0.1% and 0.2% and 0.05%, 0.1% and 0.5%, obtaining 9 samples. The in vitro activity assays were performed against promastigotes of L. infantum by the MTT test and the results were analyzed with the aid of GraphPad Prisma 5.0 software. Among the prepared formulations, sample A2 (0.1%Chi:0.05%TPP g/v), had the best results, with particle sizes at 89.43 ± 0.774 nm, polydispersity 0.168 and Zeta potential 12.8 mV. After encapsulation of the CAR (1mg/mL) in formulation A2, it showed a particle size of 245.9 nm, polydispersity 0.175 and the high zeta potential 15.4 mV. Preliminary analysis of in vitro antileishmania activity demonstrated strong inhibition of L. infantum promastigotes by NPCar with an IC50 of 2.659 μg/mL. The results of the present study demonstrate that the obtained NPCar maintain characteristics suitable for drug delivery systems with high homogeneity and stability, and preliminary studies in L. infantum demonstrated that NPCar may be promising candidates for visceral leishmaniasis. |
publishDate |
2022 |
dc.date.none.fl_str_mv |
2022-10-31 2022-03-09 2023-04-27T13:01:57Z 2023-04-27T13:01:57Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/masterThesis |
format |
masterThesis |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
https://repositorio.ufpb.br/jspui/handle/123456789/26828 |
url |
https://repositorio.ufpb.br/jspui/handle/123456789/26828 |
dc.language.iso.fl_str_mv |
por |
language |
por |
dc.rights.driver.fl_str_mv |
Attribution-NoDerivs 3.0 Brazil http://creativecommons.org/licenses/by-nd/3.0/br/ info:eu-repo/semantics/embargoedAccess |
rights_invalid_str_mv |
Attribution-NoDerivs 3.0 Brazil http://creativecommons.org/licenses/by-nd/3.0/br/ |
eu_rights_str_mv |
embargoedAccess |
dc.publisher.none.fl_str_mv |
Universidade Federal da Paraíba Brasil Biologia Celular e Molecular Programa de Pós-Graduação em Biologia Celular e Molecular UFPB |
publisher.none.fl_str_mv |
Universidade Federal da Paraíba Brasil Biologia Celular e Molecular Programa de Pós-Graduação em Biologia Celular e Molecular UFPB |
dc.source.none.fl_str_mv |
reponame:Biblioteca Digital de Teses e Dissertações da UFPB instname:Universidade Federal da Paraíba (UFPB) instacron:UFPB |
instname_str |
Universidade Federal da Paraíba (UFPB) |
instacron_str |
UFPB |
institution |
UFPB |
reponame_str |
Biblioteca Digital de Teses e Dissertações da UFPB |
collection |
Biblioteca Digital de Teses e Dissertações da UFPB |
repository.name.fl_str_mv |
Biblioteca Digital de Teses e Dissertações da UFPB - Universidade Federal da Paraíba (UFPB) |
repository.mail.fl_str_mv |
diretoria@ufpb.br|| diretoria@ufpb.br |
_version_ |
1801843008883130368 |