PVP solid dispersions containing Poloxamer 407 or TPGS for the improvement of ursolic acid release
Autor(a) principal: | |
---|---|
Data de Publicação: | 2023 |
Outros Autores: | , , , , |
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. |
id |
UNSP_83effa239b65e3a53d3578dfc2c05264 |
---|---|
oai_identifier_str |
oai:repositorio.unesp.br:11449/248795 |
network_acronym_str |
UNSP |
network_name_str |
Repositório Institucional da UNESP |
repository_id_str |
2946 |
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/openAccess2024-06-24T13:46:11Zoai:repositorio.unesp.br:11449/248795Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T21:03:00.332331Repositório 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 |
|
_version_ |
1808129278329487360 |