An inhalable powder formulation based on micro-and nanoparticles containing 5-fluorouracil for the treatment of metastatic melanoma

Detalhes bibliográficos
Autor(a) principal: Zatta, Kelly Cristine
Data de Publicação: 2018
Outros Autores: Frank, Luiza A., Reolon, Luciano Antonio, Amaral-Machado, Lucas, Egito, Eryvaldo S. T., Gremião, Maria Palmira Daflon [UNESP], Pohlmann, Adriana Raffin, Guterres, Silvia S.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da UNESP
Texto Completo: http://dx.doi.org/10.3390/nano8020075
http://hdl.handle.net/11449/179573
Resumo: Melanoma is the most aggressive and lethal type of skin cancer, with a poor prognosis because of the potential for metastatic spread. The aim was to develop innovative powder formulations for the treatment of metastatic melanoma based on micro- and nanocarriers containing 5-fluorouracil (5FU) for pulmonary administration, aiming at local and systemic action. Therefore, two innovative inhalable powder formulations were produced by spray-drying using chondroitin sulfate as a structuring polymer: (a) 5FU nanoparticles obtained by piezoelectric atomization (5FU-NS) and (b) 5FU microparticles of the mucoadhesive agent Methocel™ F4M for sustained release produced by conventional spray drying (5FU-MS). The physicochemical and aerodynamic were evaluated in vitro for both systems, proving to be attractive for pulmonary delivery. The theoretical aerodynamic diameters obtained were 0.322 ± 0.07 µm (5FU-NS) and 1.138 ± 0.54 µm (5FU-MS). The fraction of respirable particles (FR%) were 76.84 ± 0.07% (5FU-NS) and 55.01 ± 2.91% (5FU-MS). The in vitro mucoadhesive properties exhibited significant adhesion efficiency in the presence of Methocel™ F4M. 5FU-MS and 5FU-NS were tested for their cytotoxic action on melanoma cancer cells (A2058 and A375) and both showed a cytotoxic effect similar to 5FU pure at concentrations of 4.3 and 1.7-fold lower, respectively.
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spelling An inhalable powder formulation based on micro-and nanoparticles containing 5-fluorouracil for the treatment of metastatic melanoma5-fluorouracilBiopolymersCytotoxicityMetastatic melanomaMicroparticlesNanoparticlesPulmonary deliveryMelanoma is the most aggressive and lethal type of skin cancer, with a poor prognosis because of the potential for metastatic spread. The aim was to develop innovative powder formulations for the treatment of metastatic melanoma based on micro- and nanocarriers containing 5-fluorouracil (5FU) for pulmonary administration, aiming at local and systemic action. Therefore, two innovative inhalable powder formulations were produced by spray-drying using chondroitin sulfate as a structuring polymer: (a) 5FU nanoparticles obtained by piezoelectric atomization (5FU-NS) and (b) 5FU microparticles of the mucoadhesive agent Methocel™ F4M for sustained release produced by conventional spray drying (5FU-MS). The physicochemical and aerodynamic were evaluated in vitro for both systems, proving to be attractive for pulmonary delivery. The theoretical aerodynamic diameters obtained were 0.322 ± 0.07 µm (5FU-NS) and 1.138 ± 0.54 µm (5FU-MS). The fraction of respirable particles (FR%) were 76.84 ± 0.07% (5FU-NS) and 55.01 ± 2.91% (5FU-MS). The in vitro mucoadhesive properties exhibited significant adhesion efficiency in the presence of Methocel™ F4M. 5FU-MS and 5FU-NS were tested for their cytotoxic action on melanoma cancer cells (A2058 and A375) and both showed a cytotoxic effect similar to 5FU pure at concentrations of 4.3 and 1.7-fold lower, respectively.Universidade Federal do Rio Grande do Sul (UFRGS)Escola de Ciências da Saúde Centro Universitário Ritter dos Reis–UniRitterUniversidade Federal do Rio Grande do Norte (UFRN)Universidade Estadual de São Paulo (UNESP)Departamento de Química Orgânica Instituto de Química Universidade Federal do Rio Grande do Sul (UFRGS)Universidade Estadual de São Paulo (UNESP)Universidade Federal do Rio Grande do Sul (UFRGS)Centro Universitário Ritter dos Reis–UniRitterUniversidade Federal do Rio Grande do Norte (UFRN)Universidade Estadual Paulista (Unesp)Zatta, Kelly CristineFrank, Luiza A.Reolon, Luciano AntonioAmaral-Machado, LucasEgito, Eryvaldo S. T.Gremião, Maria Palmira Daflon [UNESP]Pohlmann, Adriana RaffinGuterres, Silvia S.2018-12-11T17:35:43Z2018-12-11T17:35:43Z2018-02-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://dx.doi.org/10.3390/nano8020075Nanomaterials, v. 8, n. 2, 2018.2079-4991http://hdl.handle.net/11449/17957310.3390/nano80200752-s2.0-850417243692-s2.0-85041724369.pdf9129780536724256Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengNanomaterialsinfo:eu-repo/semantics/openAccess2024-06-24T13:44:54Zoai:repositorio.unesp.br:11449/179573Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T14:01:34.713552Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false
dc.title.none.fl_str_mv An inhalable powder formulation based on micro-and nanoparticles containing 5-fluorouracil for the treatment of metastatic melanoma
title An inhalable powder formulation based on micro-and nanoparticles containing 5-fluorouracil for the treatment of metastatic melanoma
spellingShingle An inhalable powder formulation based on micro-and nanoparticles containing 5-fluorouracil for the treatment of metastatic melanoma
Zatta, Kelly Cristine
5-fluorouracil
Biopolymers
Cytotoxicity
Metastatic melanoma
Microparticles
Nanoparticles
Pulmonary delivery
title_short An inhalable powder formulation based on micro-and nanoparticles containing 5-fluorouracil for the treatment of metastatic melanoma
title_full An inhalable powder formulation based on micro-and nanoparticles containing 5-fluorouracil for the treatment of metastatic melanoma
title_fullStr An inhalable powder formulation based on micro-and nanoparticles containing 5-fluorouracil for the treatment of metastatic melanoma
title_full_unstemmed An inhalable powder formulation based on micro-and nanoparticles containing 5-fluorouracil for the treatment of metastatic melanoma
title_sort An inhalable powder formulation based on micro-and nanoparticles containing 5-fluorouracil for the treatment of metastatic melanoma
author Zatta, Kelly Cristine
author_facet Zatta, Kelly Cristine
Frank, Luiza A.
Reolon, Luciano Antonio
Amaral-Machado, Lucas
Egito, Eryvaldo S. T.
Gremião, Maria Palmira Daflon [UNESP]
Pohlmann, Adriana Raffin
Guterres, Silvia S.
author_role author
author2 Frank, Luiza A.
Reolon, Luciano Antonio
Amaral-Machado, Lucas
Egito, Eryvaldo S. T.
Gremião, Maria Palmira Daflon [UNESP]
Pohlmann, Adriana Raffin
Guterres, Silvia S.
author2_role author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Universidade Federal do Rio Grande do Sul (UFRGS)
Centro Universitário Ritter dos Reis–UniRitter
Universidade Federal do Rio Grande do Norte (UFRN)
Universidade Estadual Paulista (Unesp)
dc.contributor.author.fl_str_mv Zatta, Kelly Cristine
Frank, Luiza A.
Reolon, Luciano Antonio
Amaral-Machado, Lucas
Egito, Eryvaldo S. T.
Gremião, Maria Palmira Daflon [UNESP]
Pohlmann, Adriana Raffin
Guterres, Silvia S.
dc.subject.por.fl_str_mv 5-fluorouracil
Biopolymers
Cytotoxicity
Metastatic melanoma
Microparticles
Nanoparticles
Pulmonary delivery
topic 5-fluorouracil
Biopolymers
Cytotoxicity
Metastatic melanoma
Microparticles
Nanoparticles
Pulmonary delivery
description Melanoma is the most aggressive and lethal type of skin cancer, with a poor prognosis because of the potential for metastatic spread. The aim was to develop innovative powder formulations for the treatment of metastatic melanoma based on micro- and nanocarriers containing 5-fluorouracil (5FU) for pulmonary administration, aiming at local and systemic action. Therefore, two innovative inhalable powder formulations were produced by spray-drying using chondroitin sulfate as a structuring polymer: (a) 5FU nanoparticles obtained by piezoelectric atomization (5FU-NS) and (b) 5FU microparticles of the mucoadhesive agent Methocel™ F4M for sustained release produced by conventional spray drying (5FU-MS). The physicochemical and aerodynamic were evaluated in vitro for both systems, proving to be attractive for pulmonary delivery. The theoretical aerodynamic diameters obtained were 0.322 ± 0.07 µm (5FU-NS) and 1.138 ± 0.54 µm (5FU-MS). The fraction of respirable particles (FR%) were 76.84 ± 0.07% (5FU-NS) and 55.01 ± 2.91% (5FU-MS). The in vitro mucoadhesive properties exhibited significant adhesion efficiency in the presence of Methocel™ F4M. 5FU-MS and 5FU-NS were tested for their cytotoxic action on melanoma cancer cells (A2058 and A375) and both showed a cytotoxic effect similar to 5FU pure at concentrations of 4.3 and 1.7-fold lower, respectively.
publishDate 2018
dc.date.none.fl_str_mv 2018-12-11T17:35:43Z
2018-12-11T17:35:43Z
2018-02-01
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://dx.doi.org/10.3390/nano8020075
Nanomaterials, v. 8, n. 2, 2018.
2079-4991
http://hdl.handle.net/11449/179573
10.3390/nano8020075
2-s2.0-85041724369
2-s2.0-85041724369.pdf
9129780536724256
url http://dx.doi.org/10.3390/nano8020075
http://hdl.handle.net/11449/179573
identifier_str_mv Nanomaterials, v. 8, n. 2, 2018.
2079-4991
10.3390/nano8020075
2-s2.0-85041724369
2-s2.0-85041724369.pdf
9129780536724256
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Nanomaterials
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.source.none.fl_str_mv Scopus
reponame:Repositório Institucional da UNESP
instname:Universidade Estadual Paulista (UNESP)
instacron:UNESP
instname_str Universidade Estadual Paulista (UNESP)
instacron_str UNESP
institution UNESP
reponame_str Repositório Institucional da UNESP
collection Repositório Institucional da UNESP
repository.name.fl_str_mv Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)
repository.mail.fl_str_mv
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