The role of stabilizers and mechanical processes on physico-chemical and anti-inflammatory properties of methotrexate nanosuspensions

Detalhes bibliográficos
Autor(a) principal: Santos, Aline Martins dos [UNESP]
Data de Publicação: 2020
Outros Autores: Meneguin, Andréia Bagliotti [UNESP], Fonseca-Santos, Bruno [UNESP], Chaves de Souza, Maurício Palmeira [UNESP], Barboza Ferreira, Leonardo Miziara [UNESP], Sábio, Rafael Miguel [UNESP], Chorilli, Marlus [UNESP], Daflon Gremião, Maria Palmira [UNESP]
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da UNESP
Texto Completo: http://dx.doi.org/10.1016/j.jddst.2020.101638
http://hdl.handle.net/11449/201629
Resumo: The aim of this study was to investigate two different mechanical processes (Ultra-turrax® and Sonication) and two stabilizers (Methyl cellulose (MC) and Poloxamer 407 (P407)) on the physico-chemical and anti-inflammatory properties of the MTX nanosuspensions. The mechanical process, presence and type of stabilizers showed a strong impact on the particle size, polydispersity index (PDI), zeta potential and morphology of MTX nanosuspensions. In particular, the surfactant property of P407 in combination sonication process reduced significantly the particle size of MTX to nano-range size. Short term stability evaluated by dynamic light scattering (DLS) technique proved that the addition of the stabilizers MC and P407 on the MTX nanosuspensions provided stability through of the steric hindrance. In vitro dissolution studies showed that MTX nanosuspensions enhanced the drug release rates, revealing the influence of the different particle size on the drug release profiles. In vivo inflammation study indicated that MTX nanosuspensions presented a greater effect on the anti-inflammatory activity, maintaining this effect for up to 6 h, being more effective than the positive control. It could be concluded that the combined usage of mechanical processes and stabilizers modified in vitro and in vivo performance of the MTX nanosuspensions. Therefore, these results confirm the potential of these nanosuspensions as a promising tool for enhancement of dissolution rate and oral bioavailability of poorly water-soluble drugs, such as MTX.
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spelling The role of stabilizers and mechanical processes on physico-chemical and anti-inflammatory properties of methotrexate nanosuspensionsAcid-base neutralizationAnti-inflammatory activityBottom-up processMethotrexateMethyl celluloseNanosuspensionPoloxamer 407The aim of this study was to investigate two different mechanical processes (Ultra-turrax® and Sonication) and two stabilizers (Methyl cellulose (MC) and Poloxamer 407 (P407)) on the physico-chemical and anti-inflammatory properties of the MTX nanosuspensions. The mechanical process, presence and type of stabilizers showed a strong impact on the particle size, polydispersity index (PDI), zeta potential and morphology of MTX nanosuspensions. In particular, the surfactant property of P407 in combination sonication process reduced significantly the particle size of MTX to nano-range size. Short term stability evaluated by dynamic light scattering (DLS) technique proved that the addition of the stabilizers MC and P407 on the MTX nanosuspensions provided stability through of the steric hindrance. In vitro dissolution studies showed that MTX nanosuspensions enhanced the drug release rates, revealing the influence of the different particle size on the drug release profiles. In vivo inflammation study indicated that MTX nanosuspensions presented a greater effect on the anti-inflammatory activity, maintaining this effect for up to 6 h, being more effective than the positive control. It could be concluded that the combined usage of mechanical processes and stabilizers modified in vitro and in vivo performance of the MTX nanosuspensions. Therefore, these results confirm the potential of these nanosuspensions as a promising tool for enhancement of dissolution rate and oral bioavailability of poorly water-soluble drugs, such as MTX.Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)São Paulo State University (UNESP) School of Pharmaceutical SciencesSão Paulo State University (UNESP) School of Pharmaceutical SciencesCAPES: 001FAPESP: 2016/01464-9Universidade Estadual Paulista (Unesp)Santos, Aline Martins dos [UNESP]Meneguin, Andréia Bagliotti [UNESP]Fonseca-Santos, Bruno [UNESP]Chaves de Souza, Maurício Palmeira [UNESP]Barboza Ferreira, Leonardo Miziara [UNESP]Sábio, Rafael Miguel [UNESP]Chorilli, Marlus [UNESP]Daflon Gremião, Maria Palmira [UNESP]2020-12-12T02:37:41Z2020-12-12T02:37:41Z2020-06-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://dx.doi.org/10.1016/j.jddst.2020.101638Journal of Drug Delivery Science and Technology, v. 57.1773-2247http://hdl.handle.net/11449/20162910.1016/j.jddst.2020.1016382-s2.0-85081885006Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengJournal of Drug Delivery Science and Technologyinfo:eu-repo/semantics/openAccess2024-06-24T13:45:39Zoai:repositorio.unesp.br:11449/201629Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T17:57:26.981448Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false
dc.title.none.fl_str_mv The role of stabilizers and mechanical processes on physico-chemical and anti-inflammatory properties of methotrexate nanosuspensions
title The role of stabilizers and mechanical processes on physico-chemical and anti-inflammatory properties of methotrexate nanosuspensions
spellingShingle The role of stabilizers and mechanical processes on physico-chemical and anti-inflammatory properties of methotrexate nanosuspensions
Santos, Aline Martins dos [UNESP]
Acid-base neutralization
Anti-inflammatory activity
Bottom-up process
Methotrexate
Methyl cellulose
Nanosuspension
Poloxamer 407
title_short The role of stabilizers and mechanical processes on physico-chemical and anti-inflammatory properties of methotrexate nanosuspensions
title_full The role of stabilizers and mechanical processes on physico-chemical and anti-inflammatory properties of methotrexate nanosuspensions
title_fullStr The role of stabilizers and mechanical processes on physico-chemical and anti-inflammatory properties of methotrexate nanosuspensions
title_full_unstemmed The role of stabilizers and mechanical processes on physico-chemical and anti-inflammatory properties of methotrexate nanosuspensions
title_sort The role of stabilizers and mechanical processes on physico-chemical and anti-inflammatory properties of methotrexate nanosuspensions
author Santos, Aline Martins dos [UNESP]
author_facet Santos, Aline Martins dos [UNESP]
Meneguin, Andréia Bagliotti [UNESP]
Fonseca-Santos, Bruno [UNESP]
Chaves de Souza, Maurício Palmeira [UNESP]
Barboza Ferreira, Leonardo Miziara [UNESP]
Sábio, Rafael Miguel [UNESP]
Chorilli, Marlus [UNESP]
Daflon Gremião, Maria Palmira [UNESP]
author_role author
author2 Meneguin, Andréia Bagliotti [UNESP]
Fonseca-Santos, Bruno [UNESP]
Chaves de Souza, Maurício Palmeira [UNESP]
Barboza Ferreira, Leonardo Miziara [UNESP]
Sábio, Rafael Miguel [UNESP]
Chorilli, Marlus [UNESP]
Daflon Gremião, Maria Palmira [UNESP]
author2_role author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Universidade Estadual Paulista (Unesp)
dc.contributor.author.fl_str_mv Santos, Aline Martins dos [UNESP]
Meneguin, Andréia Bagliotti [UNESP]
Fonseca-Santos, Bruno [UNESP]
Chaves de Souza, Maurício Palmeira [UNESP]
Barboza Ferreira, Leonardo Miziara [UNESP]
Sábio, Rafael Miguel [UNESP]
Chorilli, Marlus [UNESP]
Daflon Gremião, Maria Palmira [UNESP]
dc.subject.por.fl_str_mv Acid-base neutralization
Anti-inflammatory activity
Bottom-up process
Methotrexate
Methyl cellulose
Nanosuspension
Poloxamer 407
topic Acid-base neutralization
Anti-inflammatory activity
Bottom-up process
Methotrexate
Methyl cellulose
Nanosuspension
Poloxamer 407
description The aim of this study was to investigate two different mechanical processes (Ultra-turrax® and Sonication) and two stabilizers (Methyl cellulose (MC) and Poloxamer 407 (P407)) on the physico-chemical and anti-inflammatory properties of the MTX nanosuspensions. The mechanical process, presence and type of stabilizers showed a strong impact on the particle size, polydispersity index (PDI), zeta potential and morphology of MTX nanosuspensions. In particular, the surfactant property of P407 in combination sonication process reduced significantly the particle size of MTX to nano-range size. Short term stability evaluated by dynamic light scattering (DLS) technique proved that the addition of the stabilizers MC and P407 on the MTX nanosuspensions provided stability through of the steric hindrance. In vitro dissolution studies showed that MTX nanosuspensions enhanced the drug release rates, revealing the influence of the different particle size on the drug release profiles. In vivo inflammation study indicated that MTX nanosuspensions presented a greater effect on the anti-inflammatory activity, maintaining this effect for up to 6 h, being more effective than the positive control. It could be concluded that the combined usage of mechanical processes and stabilizers modified in vitro and in vivo performance of the MTX nanosuspensions. Therefore, these results confirm the potential of these nanosuspensions as a promising tool for enhancement of dissolution rate and oral bioavailability of poorly water-soluble drugs, such as MTX.
publishDate 2020
dc.date.none.fl_str_mv 2020-12-12T02:37:41Z
2020-12-12T02:37:41Z
2020-06-01
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/10.1016/j.jddst.2020.101638
Journal of Drug Delivery Science and Technology, v. 57.
1773-2247
http://hdl.handle.net/11449/201629
10.1016/j.jddst.2020.101638
2-s2.0-85081885006
url http://dx.doi.org/10.1016/j.jddst.2020.101638
http://hdl.handle.net/11449/201629
identifier_str_mv Journal of Drug Delivery Science and Technology, v. 57.
1773-2247
10.1016/j.jddst.2020.101638
2-s2.0-85081885006
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Journal of Drug Delivery Science and Technology
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
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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