An inhalable powder formulation based on micro-and nanoparticles containing 5-fluorouracil for the treatment of metastatic melanoma
Autor(a) principal: | |
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Data de Publicação: | 2018 |
Outros Autores: | , , , , , , |
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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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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1808128306135957504 |