Desenvolvimento de nanopartículas de quitosana contendo carvacrol frente a Leishmania infantum: estudo preliminar

Detalhes bibliográficos
Autor(a) principal: Borges, Joyce Cordeiro
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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spelling 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
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