Preparação de nanopartículas de quitosana para liberação de fármacos

Detalhes bibliográficos
Autor(a) principal: Barros, Ellen Luna de [UNIFESP]
Data de Publicação: 2018
Tipo de documento: Dissertação
Idioma: por
Título da fonte: Repositório Institucional da UNIFESP
Texto Completo: https://sucupira.capes.gov.br/sucupira/public/consultas/coleta/trabalhoConclusao/viewTrabalhoConclusao.jsf?popup=true&id_trabalho=6746807
https://repositorio.unifesp.br/handle/11600/52796
Resumo: Drug carriers provide a more efficient manner to administer drugs that have restrictions in the use. In this study, chitosan, which is a semi synthetic biopolymer produced from a renewable source, has been transformed into nanoparticles to act as carriers for drugs and other bioactive molecules. The preparation of the nanoparticles was carried out using the coacervation and ionotropic gelation methods. The formed nanoparticles in aqueous dispersion were analyzed by zeta potential and dynamic light scattering of measurements. Nanoparticles isolated by centrifugation were analyzed by X-ray diffractometry and Fourier transformed infrared absorption spectroscopy. Ibuprofen was the model drug used in this study. This drug was incorporated directly into the nanoparticles during the synthesis step. The drug release from the chitosan nanoparticles was evaluated in phosphate buffer with pH 6.0 and 8.0 and also in simulated body fluid (pH 7.2), which is a medium that mimics the physiological chemical conditions of intracellular fluid. Representative kinetic models of different pharmaceutical forms of drug release dosage were applied to the experimental curve of ibuprofen release in simulated body fluid. The synthetic method based on coacervation did not produce the nanoparticles with the desired characteristics of low index of polydispersity and high zeta potential, in none of the experimental conditions evaluated. The ionotropic gelation method produced the nanoparticles with the desired colloidal characteristics when a mass ratio of chitosan and sodium tripolyphosphate of 3 : 1 was used during the preparation of the nanoparticles. The ibuprofen incorporation by using direct synthesis was around 91%, resulting in a material containing 21% by mass of the drug incorporated into the polymer network as tiny crystals and adsorbed molecules. The amount of ibuprofen released after 240 min in acid medium (30 %) was higher than in basic medium (10 %), which is the condition where the drug is way more soluble. This result demonstrated the role of the chitosan nanoparticle in modifing the ibuprofen solubility, as expect for a drug carrier. In simulated body fluid, 32% of the ibuprofen incorporated into the nanoparticles was released after the 240 min of monitoring. The experimental release kinetics adjusted to the Korsmeyer-Peppas model, ascribed for polymer matrices, with the release mechanism dominated in the monitored period by the diffusion of the drug located closest to the surface of the particle.
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spelling Preparação de nanopartículas de quitosana para liberação de fármacosNanoparticlesChitosanIbuprofenControlled releaseIonotropic gelation methodNanopartículasQuitosanaIbuprofenoLiberação modificadaGelificação ionotrópicaDrug carriers provide a more efficient manner to administer drugs that have restrictions in the use. In this study, chitosan, which is a semi synthetic biopolymer produced from a renewable source, has been transformed into nanoparticles to act as carriers for drugs and other bioactive molecules. The preparation of the nanoparticles was carried out using the coacervation and ionotropic gelation methods. The formed nanoparticles in aqueous dispersion were analyzed by zeta potential and dynamic light scattering of measurements. Nanoparticles isolated by centrifugation were analyzed by X-ray diffractometry and Fourier transformed infrared absorption spectroscopy. Ibuprofen was the model drug used in this study. This drug was incorporated directly into the nanoparticles during the synthesis step. The drug release from the chitosan nanoparticles was evaluated in phosphate buffer with pH 6.0 and 8.0 and also in simulated body fluid (pH 7.2), which is a medium that mimics the physiological chemical conditions of intracellular fluid. Representative kinetic models of different pharmaceutical forms of drug release dosage were applied to the experimental curve of ibuprofen release in simulated body fluid. The synthetic method based on coacervation did not produce the nanoparticles with the desired characteristics of low index of polydispersity and high zeta potential, in none of the experimental conditions evaluated. The ionotropic gelation method produced the nanoparticles with the desired colloidal characteristics when a mass ratio of chitosan and sodium tripolyphosphate of 3 : 1 was used during the preparation of the nanoparticles. The ibuprofen incorporation by using direct synthesis was around 91%, resulting in a material containing 21% by mass of the drug incorporated into the polymer network as tiny crystals and adsorbed molecules. The amount of ibuprofen released after 240 min in acid medium (30 %) was higher than in basic medium (10 %), which is the condition where the drug is way more soluble. This result demonstrated the role of the chitosan nanoparticle in modifing the ibuprofen solubility, as expect for a drug carrier. In simulated body fluid, 32% of the ibuprofen incorporated into the nanoparticles was released after the 240 min of monitoring. The experimental release kinetics adjusted to the Korsmeyer-Peppas model, ascribed for polymer matrices, with the release mechanism dominated in the monitored period by the diffusion of the drug located closest to the surface of the particle.Carreadores de fármacos propiciam maneiras mais eficientes para a administração de princípios ativos que apresentem alguma restrição de uso. Neste estudo, a quitosana, que é um biopolímero semissintético de origem renovável, foi transformada em nanopartículas para carreamento de fármacos e outras moléculas bioativas. A preparação das nanopartículas de foi feita pelos métodos da coacervação e de gelificação ionotrópica. As nanopartículas formadas em dispersão aquosa foram analisadas por medidas de potencial ζ e de espalhamento dinâmico de luz. As nanopartículas isoladas por centrifugação foram analisadas por difratometria de raios X e espectroscopia vibracional de absorção no infravermelho por transformada de Fourier. O fármaco modelo utilizado neste estudo foi o ibuprofeno, o qual foi incorporado às nanopartículas pelo método de síntese direta. A posterior liberação foi avaliada em pH 6,0 e 8,0 e, também, em fluído corporal simulado (pH 7,2), que é um meio que mimetiza o fluído intracelular. Modelos cinéticos representativos de diferentes formas farmacêuticas de liberação modificada foram aplicados à curva experimental de liberação do ibuprofeno em fluído corporal simulado. Os resultados demonstraram que a síntese por coacervação não produziu as nanopartículas com as características desejadas (baixo índice de polidispersividade e potencial ζ elevado) em nenhuma das condições experimentais testadas. A síntese por gelificação produziu as nanopartículas com as características coloidais desejadas quando utilizada a proporção em massa de quitosana : tripolifosfato de sódio de 3 : 1 na preparação das nanopartículas. A eficiência de incorporação do ibuprofeno por síntese direta foi de aproximadamente 91 %, resultando em um material contendo 21 % em massa do fármaco incorporado na rede polimérica na forma de pequenos cristais e de moléculas adsorvidas. A quantidade de ibuprofeno liberada após 240 min em meio ácido (30 %) foi maior do que em básico (10 %), que é a condição na qual este fármaco é bem mais solúvel. Este resultado fato demonstrou a atuação da nanopartícula de quitosana na modificação da disponibilidade do fármaco, como esperado para um carreador. Em fluido corporal simulado foi liberado 32 % do ibuprofeno incorporado nas nanopartículas considerando ao longo dos 240 min de monitoramento. A cinética de liberação se ajustou ao modelo de KorsmeyerPeppas, aplicado às matrizes poliméricas, sendo o mecanismo de liberação no período avaliado dominado pela difusão do fármaco localizado mais próximo da superfície da partículaDados abertos - Sucupira - Teses e dissertações (2018)Universidade Federal de São PauloBizeto, Marcos Augusto [UNIFESP]Universidade Federal de São Paulo (UNIFESP)Barros, Ellen Luna de [UNIFESP]2020-03-25T12:10:32Z2020-03-25T12:10:32Z2018-11-29info:eu-repo/semantics/masterThesisinfo:eu-repo/semantics/publishedVersion56 p.application/pdfhttps://sucupira.capes.gov.br/sucupira/public/consultas/coleta/trabalhoConclusao/viewTrabalhoConclusao.jsf?popup=true&id_trabalho=67468072018-0739.pdfhttps://repositorio.unifesp.br/handle/11600/52796porinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da UNIFESPinstname:Universidade Federal de São Paulo (UNIFESP)instacron:UNIFESP2024-08-02T18:30:44Zoai:repositorio.unifesp.br/:11600/52796Repositório InstitucionalPUBhttp://www.repositorio.unifesp.br/oai/requestbiblioteca.csp@unifesp.bropendoar:34652024-08-02T18:30:44Repositório Institucional da UNIFESP - Universidade Federal de São Paulo (UNIFESP)false
dc.title.none.fl_str_mv Preparação de nanopartículas de quitosana para liberação de fármacos
title Preparação de nanopartículas de quitosana para liberação de fármacos
spellingShingle Preparação de nanopartículas de quitosana para liberação de fármacos
Barros, Ellen Luna de [UNIFESP]
Nanoparticles
Chitosan
Ibuprofen
Controlled release
Ionotropic gelation method
Nanopartículas
Quitosana
Ibuprofeno
Liberação modificada
Gelificação ionotrópica
title_short Preparação de nanopartículas de quitosana para liberação de fármacos
title_full Preparação de nanopartículas de quitosana para liberação de fármacos
title_fullStr Preparação de nanopartículas de quitosana para liberação de fármacos
title_full_unstemmed Preparação de nanopartículas de quitosana para liberação de fármacos
title_sort Preparação de nanopartículas de quitosana para liberação de fármacos
author Barros, Ellen Luna de [UNIFESP]
author_facet Barros, Ellen Luna de [UNIFESP]
author_role author
dc.contributor.none.fl_str_mv Bizeto, Marcos Augusto [UNIFESP]
Universidade Federal de São Paulo (UNIFESP)
dc.contributor.author.fl_str_mv Barros, Ellen Luna de [UNIFESP]
dc.subject.por.fl_str_mv Nanoparticles
Chitosan
Ibuprofen
Controlled release
Ionotropic gelation method
Nanopartículas
Quitosana
Ibuprofeno
Liberação modificada
Gelificação ionotrópica
topic Nanoparticles
Chitosan
Ibuprofen
Controlled release
Ionotropic gelation method
Nanopartículas
Quitosana
Ibuprofeno
Liberação modificada
Gelificação ionotrópica
description Drug carriers provide a more efficient manner to administer drugs that have restrictions in the use. In this study, chitosan, which is a semi synthetic biopolymer produced from a renewable source, has been transformed into nanoparticles to act as carriers for drugs and other bioactive molecules. The preparation of the nanoparticles was carried out using the coacervation and ionotropic gelation methods. The formed nanoparticles in aqueous dispersion were analyzed by zeta potential and dynamic light scattering of measurements. Nanoparticles isolated by centrifugation were analyzed by X-ray diffractometry and Fourier transformed infrared absorption spectroscopy. Ibuprofen was the model drug used in this study. This drug was incorporated directly into the nanoparticles during the synthesis step. The drug release from the chitosan nanoparticles was evaluated in phosphate buffer with pH 6.0 and 8.0 and also in simulated body fluid (pH 7.2), which is a medium that mimics the physiological chemical conditions of intracellular fluid. Representative kinetic models of different pharmaceutical forms of drug release dosage were applied to the experimental curve of ibuprofen release in simulated body fluid. The synthetic method based on coacervation did not produce the nanoparticles with the desired characteristics of low index of polydispersity and high zeta potential, in none of the experimental conditions evaluated. The ionotropic gelation method produced the nanoparticles with the desired colloidal characteristics when a mass ratio of chitosan and sodium tripolyphosphate of 3 : 1 was used during the preparation of the nanoparticles. The ibuprofen incorporation by using direct synthesis was around 91%, resulting in a material containing 21% by mass of the drug incorporated into the polymer network as tiny crystals and adsorbed molecules. The amount of ibuprofen released after 240 min in acid medium (30 %) was higher than in basic medium (10 %), which is the condition where the drug is way more soluble. This result demonstrated the role of the chitosan nanoparticle in modifing the ibuprofen solubility, as expect for a drug carrier. In simulated body fluid, 32% of the ibuprofen incorporated into the nanoparticles was released after the 240 min of monitoring. The experimental release kinetics adjusted to the Korsmeyer-Peppas model, ascribed for polymer matrices, with the release mechanism dominated in the monitored period by the diffusion of the drug located closest to the surface of the particle.
publishDate 2018
dc.date.none.fl_str_mv 2018-11-29
2020-03-25T12:10:32Z
2020-03-25T12:10:32Z
dc.type.driver.fl_str_mv info:eu-repo/semantics/masterThesis
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
format masterThesis
status_str publishedVersion
dc.identifier.uri.fl_str_mv https://sucupira.capes.gov.br/sucupira/public/consultas/coleta/trabalhoConclusao/viewTrabalhoConclusao.jsf?popup=true&id_trabalho=6746807
2018-0739.pdf
https://repositorio.unifesp.br/handle/11600/52796
url https://sucupira.capes.gov.br/sucupira/public/consultas/coleta/trabalhoConclusao/viewTrabalhoConclusao.jsf?popup=true&id_trabalho=6746807
https://repositorio.unifesp.br/handle/11600/52796
identifier_str_mv 2018-0739.pdf
dc.language.iso.fl_str_mv por
language por
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv 56 p.
application/pdf
dc.publisher.none.fl_str_mv Universidade Federal de São Paulo
publisher.none.fl_str_mv Universidade Federal de São Paulo
dc.source.none.fl_str_mv reponame:Repositório Institucional da UNIFESP
instname:Universidade Federal de São Paulo (UNIFESP)
instacron:UNIFESP
instname_str Universidade Federal de São Paulo (UNIFESP)
instacron_str UNIFESP
institution UNIFESP
reponame_str Repositório Institucional da UNIFESP
collection Repositório Institucional da UNIFESP
repository.name.fl_str_mv Repositório Institucional da UNIFESP - Universidade Federal de São Paulo (UNIFESP)
repository.mail.fl_str_mv biblioteca.csp@unifesp.br
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