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

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dc.contributor.authorZatta, Kelly Cristine
dc.contributor.authorFrank, Luiza A.
dc.contributor.authorReolon, Luciano Antonio
dc.contributor.authorAmaral-Machado, Lucas
dc.contributor.authorEgito, Eryvaldo S. T.
dc.contributor.authorGremião, Maria Palmira Daflon [UNESP]
dc.contributor.authorPohlmann, Adriana Raffin
dc.contributor.authorGuterres, Silvia S.
dc.contributor.institutionUniversidade Federal do Rio Grande do Sul (UFRGS)
dc.contributor.institutionCentro Universitário Ritter dos Reis–UniRitter
dc.contributor.institutionUniversidade Federal do Rio Grande do Norte (UFRN)
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.date.accessioned2018-12-11T17:35:43Z
dc.date.available2018-12-11T17:35:43Z
dc.date.issued2018-02-01
dc.description.abstractMelanoma 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.en
dc.description.affiliationUniversidade Federal do Rio Grande do Sul (UFRGS)
dc.description.affiliationEscola de Ciências da Saúde Centro Universitário Ritter dos Reis–UniRitter
dc.description.affiliationUniversidade Federal do Rio Grande do Norte (UFRN)
dc.description.affiliationUniversidade Estadual de São Paulo (UNESP)
dc.description.affiliationDepartamento de Química Orgânica Instituto de Química Universidade Federal do Rio Grande do Sul (UFRGS)
dc.description.affiliationUnespUniversidade Estadual de São Paulo (UNESP)
dc.identifierhttp://dx.doi.org/10.3390/nano8020075
dc.identifier.citationNanomaterials, v. 8, n. 2, 2018.
dc.identifier.doi10.3390/nano8020075
dc.identifier.file2-s2.0-85041724369.pdf
dc.identifier.issn2079-4991
dc.identifier.lattes9129780536724256
dc.identifier.scopus2-s2.0-85041724369
dc.identifier.urihttp://hdl.handle.net/11449/179573
dc.language.isoeng
dc.relation.ispartofNanomaterials
dc.rights.accessRightsAcesso aberto
dc.sourceScopus
dc.subject5-fluorouracil
dc.subjectBiopolymers
dc.subjectCytotoxicity
dc.subjectMetastatic melanoma
dc.subjectMicroparticles
dc.subjectNanoparticles
dc.subjectPulmonary delivery
dc.titleAn inhalable powder formulation based on micro-and nanoparticles containing 5-fluorouracil for the treatment of metastatic melanomaen
dc.typeArtigo
unesp.advisor.lattes9129780536724256

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Artigos - Fármacos e Medicamentos - FCFAR