Desenvolvimento e atividade antifúngica de nanopartículas de PLGA carregadas com o peptídeo crotalicidina [15-34]

Detalhes bibliográficos
Ano de defesa: 2019
Autor(a) principal: Santos, Ana Paula dos
Orientador(a): Baptista, Gandhi Rádis
Banca de defesa: Não Informado pela instituição
Tipo de documento: Dissertação
Tipo de acesso: Acesso aberto
Idioma: por
Instituição de defesa: Não Informado pela instituição
Programa de Pós-Graduação: Não Informado pela instituição
Departamento: Não Informado pela instituição
País: Não Informado pela instituição
Palavras-chave em Português:
Link de acesso: http://www.repositorio.ufc.br/handle/riufc/42068
Resumo: Human fungal infections, in the form of topical infections or as systemic infections, have become a significant cause of morbidity. In addition, the antifungal agents normally used to treat these infections have shown limited therapeutic results due to toxic side effects, low efficacy and the emergence of resistant pathogens, making the development of new antifungal agents in the pharmaceutical area of great interest. In this sense, the present study aimed to develop an optimized formulation of PLGA (poly (lactic acid-co-glycolic acid)) nanoparticles to load the Ctn[15-34] peptide, a promising antifungal agent derived from a cathelicidin of the venom gland of the snake Crotalus durissus terrificus. The nanoparticles were synthesized by the double emulsion/solvent evaporation method and had their physicochemical characteristics, stability, release and antifungal activity evaluated. The obtained nanosystem presented homogeneous particles, with a mean size of 213.2 ± 2.00 nm, polydispersity index of 0.044 ± 0.04 and zeta potential of -16.03 ± 1.20 mV, with perfect stability of these parameters by 30 days at 4 °C. An excellent entrapment efficiency was obtained, around 93.3 ± 0.10% and the release profile showed a rapid initial release of the peptide, approximately 27% in the first 24 hours, followed by sustained release for at least 16 days. Another relevant aspect is that the nanoparticles potentiated the antifungal activity of the peptide when compared to its free form, in equivalent concentration, representing a thriving therapeutic approach for the delivery of Ctn[15-34].
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spelling Santos, Ana Paula dosAraújo, Tamara Gonçalves deBaptista, Gandhi Rádis2019-05-28T10:27:40Z2019-05-28T10:27:40Z2019-04-23SANTOS, A. P. D. Desenvolvimento e atividade antifúngica de nanopartículas de PLGA carregadas com o peptídeo crotalicidina [15-34]. 2019. 61 f. Dissertação. (Mestrado em Ciências Farmacêuticas) - Faculdade de Farmácia, Odontologia e Enfermagem, Universidade Federal do Ceará, Fortaleza, 2019.http://www.repositorio.ufc.br/handle/riufc/42068Human fungal infections, in the form of topical infections or as systemic infections, have become a significant cause of morbidity. In addition, the antifungal agents normally used to treat these infections have shown limited therapeutic results due to toxic side effects, low efficacy and the emergence of resistant pathogens, making the development of new antifungal agents in the pharmaceutical area of great interest. In this sense, the present study aimed to develop an optimized formulation of PLGA (poly (lactic acid-co-glycolic acid)) nanoparticles to load the Ctn[15-34] peptide, a promising antifungal agent derived from a cathelicidin of the venom gland of the snake Crotalus durissus terrificus. The nanoparticles were synthesized by the double emulsion/solvent evaporation method and had their physicochemical characteristics, stability, release and antifungal activity evaluated. The obtained nanosystem presented homogeneous particles, with a mean size of 213.2 ± 2.00 nm, polydispersity index of 0.044 ± 0.04 and zeta potential of -16.03 ± 1.20 mV, with perfect stability of these parameters by 30 days at 4 °C. An excellent entrapment efficiency was obtained, around 93.3 ± 0.10% and the release profile showed a rapid initial release of the peptide, approximately 27% in the first 24 hours, followed by sustained release for at least 16 days. Another relevant aspect is that the nanoparticles potentiated the antifungal activity of the peptide when compared to its free form, in equivalent concentration, representing a thriving therapeutic approach for the delivery of Ctn[15-34].As infecções fúngicas que acometem o ser humano, na forma de infecções tópicas ou como infecções sistêmicas, vêm se tornando uma causa significativa de morbidade. Aliado a isso, os antifúngicos normalmente utilizados para tratar essas infecções têm apresentado resultados terapêuticos limitados devido a efeitos colaterais tóxicos, baixa eficácia e o aparecimento de patógenos resistentes, tornando de grande interesse o desenvolvimento de novos agentes antifúngicos na área farmacêutica. Neste sentido, o presente estudo objetivou desenvolver uma formulação otimizada de nanopartículas de PLGA (poli(ácido lático-co-ácido glicólico)) para veicular o peptídeo Crotalicidina [15-34], um promissor agente antifúngico derivado de uma catelicidina da glândula de veneno da serpente Crotalus durissus terrificus. As nanopartículas foram sintetizadas pelo método de dupla emulsificação/evaporação de solvente e tiveram suas características físico-químicas, estabilidade, liberação e atividade antifúngica avaliadas. O nanossistema obtido apresentou partículas homogêneas, com tamanho médio de 213,2 ± 2,00 nm, índice de polidispersividade de 0,044 ± 0,04 e potencial zeta de -16,03 ± 1,20 mV, com perfeita estabilidade desses parâmetros por 30 dias a 4 °C. Uma excelente eficiência de encapsulação foi obtida, em torno de 93,3 ± 0,10 % e o perfil de liberação apresentado contou com uma liberação inicial rápida do peptídeo, aproximadamente 27% nas primeiras 24 horas, seguido de uma liberação sustentada por pelo menos 16 dias. Outro aspecto relevante é que as nanopartículas potencializaram a atividade antifúngica do peptídeo quando comparado à sua forma livre, em concentração equivalente, representando uma próspera abordagem terapêutica para a veiculação do Crotalicidina [15-34].NanopartículasAntifúngicosMicosesDesenvolvimento e atividade antifúngica de nanopartículas de PLGA carregadas com o peptídeo crotalicidina [15-34]info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisporreponame:Repositório Institucional da Universidade Federal do Ceará (UFC)instname:Universidade Federal do Ceará (UFC)instacron:UFCinfo:eu-repo/semantics/openAccessLICENSElicense.txtlicense.txttext/plain; charset=utf-81748http://repositorio.ufc.br/bitstream/riufc/42068/2/license.txt8a4605be74aa9ea9d79846c1fba20a33MD52ORIGINAL2019_dis_apdsantos.pdf2019_dis_apdsantos.pdfapplication/pdf917691http://repositorio.ufc.br/bitstream/riufc/42068/1/2019_dis_apdsantos.pdf1d44f35a5d202546dd6abba347900c8dMD51riufc/420682022-12-12 14:53:54.645oai:repositorio.ufc.br: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Repositório InstitucionalPUBhttp://www.repositorio.ufc.br/ri-oai/requestbu@ufc.br || repositorio@ufc.bropendoar:2022-12-12T17:53:54Repositório Institucional da Universidade Federal do Ceará (UFC) - Universidade Federal do Ceará (UFC)false
dc.title.pt_BR.fl_str_mv Desenvolvimento e atividade antifúngica de nanopartículas de PLGA carregadas com o peptídeo crotalicidina [15-34]
title Desenvolvimento e atividade antifúngica de nanopartículas de PLGA carregadas com o peptídeo crotalicidina [15-34]
spellingShingle Desenvolvimento e atividade antifúngica de nanopartículas de PLGA carregadas com o peptídeo crotalicidina [15-34]
Santos, Ana Paula dos
Nanopartículas
Antifúngicos
Micoses
title_short Desenvolvimento e atividade antifúngica de nanopartículas de PLGA carregadas com o peptídeo crotalicidina [15-34]
title_full Desenvolvimento e atividade antifúngica de nanopartículas de PLGA carregadas com o peptídeo crotalicidina [15-34]
title_fullStr Desenvolvimento e atividade antifúngica de nanopartículas de PLGA carregadas com o peptídeo crotalicidina [15-34]
title_full_unstemmed Desenvolvimento e atividade antifúngica de nanopartículas de PLGA carregadas com o peptídeo crotalicidina [15-34]
title_sort Desenvolvimento e atividade antifúngica de nanopartículas de PLGA carregadas com o peptídeo crotalicidina [15-34]
author Santos, Ana Paula dos
author_facet Santos, Ana Paula dos
author_role author
dc.contributor.co-advisor.none.fl_str_mv Araújo, Tamara Gonçalves de
dc.contributor.author.fl_str_mv Santos, Ana Paula dos
dc.contributor.advisor1.fl_str_mv Baptista, Gandhi Rádis
contributor_str_mv Baptista, Gandhi Rádis
dc.subject.por.fl_str_mv Nanopartículas
Antifúngicos
Micoses
topic Nanopartículas
Antifúngicos
Micoses
description Human fungal infections, in the form of topical infections or as systemic infections, have become a significant cause of morbidity. In addition, the antifungal agents normally used to treat these infections have shown limited therapeutic results due to toxic side effects, low efficacy and the emergence of resistant pathogens, making the development of new antifungal agents in the pharmaceutical area of great interest. In this sense, the present study aimed to develop an optimized formulation of PLGA (poly (lactic acid-co-glycolic acid)) nanoparticles to load the Ctn[15-34] peptide, a promising antifungal agent derived from a cathelicidin of the venom gland of the snake Crotalus durissus terrificus. The nanoparticles were synthesized by the double emulsion/solvent evaporation method and had their physicochemical characteristics, stability, release and antifungal activity evaluated. The obtained nanosystem presented homogeneous particles, with a mean size of 213.2 ± 2.00 nm, polydispersity index of 0.044 ± 0.04 and zeta potential of -16.03 ± 1.20 mV, with perfect stability of these parameters by 30 days at 4 °C. An excellent entrapment efficiency was obtained, around 93.3 ± 0.10% and the release profile showed a rapid initial release of the peptide, approximately 27% in the first 24 hours, followed by sustained release for at least 16 days. Another relevant aspect is that the nanoparticles potentiated the antifungal activity of the peptide when compared to its free form, in equivalent concentration, representing a thriving therapeutic approach for the delivery of Ctn[15-34].
publishDate 2019
dc.date.accessioned.fl_str_mv 2019-05-28T10:27:40Z
dc.date.available.fl_str_mv 2019-05-28T10:27:40Z
dc.date.issued.fl_str_mv 2019-04-23
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/masterThesis
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dc.identifier.citation.fl_str_mv SANTOS, A. P. D. Desenvolvimento e atividade antifúngica de nanopartículas de PLGA carregadas com o peptídeo crotalicidina [15-34]. 2019. 61 f. Dissertação. (Mestrado em Ciências Farmacêuticas) - Faculdade de Farmácia, Odontologia e Enfermagem, Universidade Federal do Ceará, Fortaleza, 2019.
dc.identifier.uri.fl_str_mv http://www.repositorio.ufc.br/handle/riufc/42068
identifier_str_mv SANTOS, A. P. D. Desenvolvimento e atividade antifúngica de nanopartículas de PLGA carregadas com o peptídeo crotalicidina [15-34]. 2019. 61 f. Dissertação. (Mestrado em Ciências Farmacêuticas) - Faculdade de Farmácia, Odontologia e Enfermagem, Universidade Federal do Ceará, Fortaleza, 2019.
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