The role of stabilizers and mechanical processes on physico-chemical and anti-inflammatory properties of methotrexate nanosuspensions
Autor(a) principal: | |
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Data de Publicação: | 2020 |
Outros Autores: | , , , , , , |
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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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 |
|
_version_ |
1808128878841954304 |