PVP solid dispersions containing Poloxamer 407 or TPGS for the improvement of ursolic acid release

Detalhes bibliográficos
Autor(a) principal: Pironi, Andressa Maria [UNESP]
Data de Publicação: 2023
Outros Autores: Eloy, Josimar de Oliveira, Rodero, Camila Fernanda [UNESP], Antonio, Selma Gutierrez [UNESP], Alonso, Jovan Duran [UNESP], Chorilli, Marlus [UNESP]
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da UNESP
Texto Completo: http://dx.doi.org/10.1590/s2175-97902023e21217
http://hdl.handle.net/11449/248795
Resumo: Solid dispersions (SDs) of ursolic acid (UA) were developed using polyvinylpyrrolidone K30 (PVP K30) in combination with non-ionic surfactants, such as D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) or poloxamer 407 (P407) with the aim of enhancing solubility and in vitro release of the UA. SDs were investigated using a 24 full factorial design, subsequently the selected formulations were characterized for water solubility, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), particle diameter, scanning electron microscopy, drug content, physical-chemical stability and in vitro release profile. SDs showed higher UA water-solubility than physical mixtures (PMs), which was attributed by transition of the drug from crystalline to amorphous or molecular state in the SDs, as indicated by XRD and DSC analyses. SD1 (with P407) and SD2 (with TPGS) were chosen for further investigation because they had higher drug load. SD1 proved to be more stable than SD2, revealing that P407 contributed to ensure the stability of the UA. Furthermore, SD1 and SD2 increased UA release by diffusion and swelling-controlled transport, following the Weibull model. Thus, solid dispersions obtained with PVP k-30 and P407 proved to be advantageous to enhance aqueous solubility and stability of UA.
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spelling PVP solid dispersions containing Poloxamer 407 or TPGS for the improvement of ursolic acid releaseSolid dispersionsSolvent methodUrsolic acidWater-solubilitySolid dispersions (SDs) of ursolic acid (UA) were developed using polyvinylpyrrolidone K30 (PVP K30) in combination with non-ionic surfactants, such as D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) or poloxamer 407 (P407) with the aim of enhancing solubility and in vitro release of the UA. SDs were investigated using a 24 full factorial design, subsequently the selected formulations were characterized for water solubility, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), particle diameter, scanning electron microscopy, drug content, physical-chemical stability and in vitro release profile. SDs showed higher UA water-solubility than physical mixtures (PMs), which was attributed by transition of the drug from crystalline to amorphous or molecular state in the SDs, as indicated by XRD and DSC analyses. SD1 (with P407) and SD2 (with TPGS) were chosen for further investigation because they had higher drug load. SD1 proved to be more stable than SD2, revealing that P407 contributed to ensure the stability of the UA. Furthermore, SD1 and SD2 increased UA release by diffusion and swelling-controlled transport, following the Weibull model. Thus, solid dispersions obtained with PVP k-30 and P407 proved to be advantageous to enhance aqueous solubility and stability of UA.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Department of Drugs and Medicines São Paulo State University School of Pharmaceutical Sciences, São PauloDepartment of Pharmacy Federal University of Ceara, CearáDepartment of Chemistry São Paulo State University Chemistry Institute, São PauloDepartment of Drugs and Medicines São Paulo State University School of Pharmaceutical Sciences, São PauloDepartment of Chemistry São Paulo State University Chemistry Institute, São PauloFAPESP: 2016/22544-0Universidade Estadual Paulista (UNESP)Federal University of CearaPironi, Andressa Maria [UNESP]Eloy, Josimar de OliveiraRodero, Camila Fernanda [UNESP]Antonio, Selma Gutierrez [UNESP]Alonso, Jovan Duran [UNESP]Chorilli, Marlus [UNESP]2023-07-29T13:53:58Z2023-07-29T13:53:58Z2023-01-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://dx.doi.org/10.1590/s2175-97902023e21217Brazilian Journal of Pharmaceutical Sciences, v. 59.2175-97901984-8250http://hdl.handle.net/11449/24879510.1590/s2175-97902023e212172-s2.0-85158834223Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengBrazilian Journal of Pharmaceutical Sciencesinfo:eu-repo/semantics/openAccess2023-07-29T13:53:58Zoai:repositorio.unesp.br:11449/248795Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462023-07-29T13:53:58Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false
dc.title.none.fl_str_mv PVP solid dispersions containing Poloxamer 407 or TPGS for the improvement of ursolic acid release
title PVP solid dispersions containing Poloxamer 407 or TPGS for the improvement of ursolic acid release
spellingShingle PVP solid dispersions containing Poloxamer 407 or TPGS for the improvement of ursolic acid release
Pironi, Andressa Maria [UNESP]
Solid dispersions
Solvent method
Ursolic acid
Water-solubility
title_short PVP solid dispersions containing Poloxamer 407 or TPGS for the improvement of ursolic acid release
title_full PVP solid dispersions containing Poloxamer 407 or TPGS for the improvement of ursolic acid release
title_fullStr PVP solid dispersions containing Poloxamer 407 or TPGS for the improvement of ursolic acid release
title_full_unstemmed PVP solid dispersions containing Poloxamer 407 or TPGS for the improvement of ursolic acid release
title_sort PVP solid dispersions containing Poloxamer 407 or TPGS for the improvement of ursolic acid release
author Pironi, Andressa Maria [UNESP]
author_facet Pironi, Andressa Maria [UNESP]
Eloy, Josimar de Oliveira
Rodero, Camila Fernanda [UNESP]
Antonio, Selma Gutierrez [UNESP]
Alonso, Jovan Duran [UNESP]
Chorilli, Marlus [UNESP]
author_role author
author2 Eloy, Josimar de Oliveira
Rodero, Camila Fernanda [UNESP]
Antonio, Selma Gutierrez [UNESP]
Alonso, Jovan Duran [UNESP]
Chorilli, Marlus [UNESP]
author2_role author
author
author
author
author
dc.contributor.none.fl_str_mv Universidade Estadual Paulista (UNESP)
Federal University of Ceara
dc.contributor.author.fl_str_mv Pironi, Andressa Maria [UNESP]
Eloy, Josimar de Oliveira
Rodero, Camila Fernanda [UNESP]
Antonio, Selma Gutierrez [UNESP]
Alonso, Jovan Duran [UNESP]
Chorilli, Marlus [UNESP]
dc.subject.por.fl_str_mv Solid dispersions
Solvent method
Ursolic acid
Water-solubility
topic Solid dispersions
Solvent method
Ursolic acid
Water-solubility
description Solid dispersions (SDs) of ursolic acid (UA) were developed using polyvinylpyrrolidone K30 (PVP K30) in combination with non-ionic surfactants, such as D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) or poloxamer 407 (P407) with the aim of enhancing solubility and in vitro release of the UA. SDs were investigated using a 24 full factorial design, subsequently the selected formulations were characterized for water solubility, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), particle diameter, scanning electron microscopy, drug content, physical-chemical stability and in vitro release profile. SDs showed higher UA water-solubility than physical mixtures (PMs), which was attributed by transition of the drug from crystalline to amorphous or molecular state in the SDs, as indicated by XRD and DSC analyses. SD1 (with P407) and SD2 (with TPGS) were chosen for further investigation because they had higher drug load. SD1 proved to be more stable than SD2, revealing that P407 contributed to ensure the stability of the UA. Furthermore, SD1 and SD2 increased UA release by diffusion and swelling-controlled transport, following the Weibull model. Thus, solid dispersions obtained with PVP k-30 and P407 proved to be advantageous to enhance aqueous solubility and stability of UA.
publishDate 2023
dc.date.none.fl_str_mv 2023-07-29T13:53:58Z
2023-07-29T13:53:58Z
2023-01-01
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/10.1590/s2175-97902023e21217
Brazilian Journal of Pharmaceutical Sciences, v. 59.
2175-9790
1984-8250
http://hdl.handle.net/11449/248795
10.1590/s2175-97902023e21217
2-s2.0-85158834223
url http://dx.doi.org/10.1590/s2175-97902023e21217
http://hdl.handle.net/11449/248795
identifier_str_mv Brazilian Journal of Pharmaceutical Sciences, v. 59.
2175-9790
1984-8250
10.1590/s2175-97902023e21217
2-s2.0-85158834223
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Brazilian Journal of Pharmaceutical Sciences
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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