Development, characterization and in vitro cytotoxicity of kaempferol-loaded nanostructured lipid carriers in glioblastoma multiforme cells
Autor(a) principal: | |
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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/10.1016/j.colsurfb.2023.113309 http://hdl.handle.net/11449/249846 |
Resumo: | Glioblastoma multiforme is the most common and most aggressive human brain cancer. GBM treatment is still a challenge because many drugs are not able to cross the blood-brain barrier, in addition to the increasing resistance to currently available chemotherapy. New therapeutic alternatives are emerging, and, in this context, we highlight kaempferol, a flavonoid with remarkable anti-tumor activity but with limited bioavailability due to its strong lipophilic property. A promising tool to improve the biopharmaceutical properties of molecules such as kaempferol is the use of drug-delivery nanosystems, such as nanostructured lipid carriers (NLC), which can facilitate the dispersion and delivery of highly lipophilic molecules. The present work aimed at the development and characterization of kaempferol-loaded NLC (K-NLC) and the evaluation of its biological properties using in vitro models. The K-NLC showed an average size of 120 nm, zeta potential of − 21 mV, and polydispersity index of 0.099. The K-NLC presented high kaempferol encapsulation efficiency (93%), a drug loading of 3.58%, and a sustained kaempferol release profile for up to 48 h. In addition to presenting a 7-fold increase in kaempferol cytotoxicity, its encapsulation in NLC promoted a cellular uptake of 75%, which corroborates with increased cytotoxicity in U-87MG cells, as observed. Together, these data reinforce the promising antineoplastic properties of kaempferol in addition to the key role of NLC as a platform for the efficient delivery of lipophilic drugs to neoplastic cells, which improved their uptake and therapeutic efficacy in glioblastoma multiforme cells. |
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Development, characterization and in vitro cytotoxicity of kaempferol-loaded nanostructured lipid carriers in glioblastoma multiforme cellsBrain cancerDrug deliveryFlavonoidsLipid nanoparticlesGlioblastoma multiforme is the most common and most aggressive human brain cancer. GBM treatment is still a challenge because many drugs are not able to cross the blood-brain barrier, in addition to the increasing resistance to currently available chemotherapy. New therapeutic alternatives are emerging, and, in this context, we highlight kaempferol, a flavonoid with remarkable anti-tumor activity but with limited bioavailability due to its strong lipophilic property. A promising tool to improve the biopharmaceutical properties of molecules such as kaempferol is the use of drug-delivery nanosystems, such as nanostructured lipid carriers (NLC), which can facilitate the dispersion and delivery of highly lipophilic molecules. The present work aimed at the development and characterization of kaempferol-loaded NLC (K-NLC) and the evaluation of its biological properties using in vitro models. The K-NLC showed an average size of 120 nm, zeta potential of − 21 mV, and polydispersity index of 0.099. The K-NLC presented high kaempferol encapsulation efficiency (93%), a drug loading of 3.58%, and a sustained kaempferol release profile for up to 48 h. In addition to presenting a 7-fold increase in kaempferol cytotoxicity, its encapsulation in NLC promoted a cellular uptake of 75%, which corroborates with increased cytotoxicity in U-87MG cells, as observed. Together, these data reinforce the promising antineoplastic properties of kaempferol in addition to the key role of NLC as a platform for the efficient delivery of lipophilic drugs to neoplastic cells, which improved their uptake and therapeutic efficacy in glioblastoma multiforme cells.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)São Paulo State University “Júlio de Mesquita Filho” School of Pharmaceutical Sciences, São PauloSão Paulo State University “Júlio de Mesquita Filho” School of Pharmaceutical Sciences, São PauloFAPESP: 19/17913–5FAPESP: 2019/25125–7FAPESP: 2020/12622–0Universidade Estadual Paulista (UNESP)Nicoleti, Luisa Ribeiro [UNESP]Di Filippo, Leonardo Delello [UNESP]Duarte, Jonatas Lobato [UNESP]Luiz, Marcela Tavares [UNESP]Sábio, Rafael Miguel [UNESP]Chorilli, Marlus [UNESP]2023-07-29T16:10:48Z2023-07-29T16:10:48Z2023-06-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://dx.doi.org/10.1016/j.colsurfb.2023.113309Colloids and Surfaces B: Biointerfaces, v. 226.1873-43670927-7765http://hdl.handle.net/11449/24984610.1016/j.colsurfb.2023.1133092-s2.0-85152110126Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengColloids and Surfaces B: Biointerfacesinfo:eu-repo/semantics/openAccess2024-06-24T13:46:12Zoai:repositorio.unesp.br:11449/249846Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T21:28:14.110695Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Development, characterization and in vitro cytotoxicity of kaempferol-loaded nanostructured lipid carriers in glioblastoma multiforme cells |
title |
Development, characterization and in vitro cytotoxicity of kaempferol-loaded nanostructured lipid carriers in glioblastoma multiforme cells |
spellingShingle |
Development, characterization and in vitro cytotoxicity of kaempferol-loaded nanostructured lipid carriers in glioblastoma multiforme cells Nicoleti, Luisa Ribeiro [UNESP] Brain cancer Drug delivery Flavonoids Lipid nanoparticles |
title_short |
Development, characterization and in vitro cytotoxicity of kaempferol-loaded nanostructured lipid carriers in glioblastoma multiforme cells |
title_full |
Development, characterization and in vitro cytotoxicity of kaempferol-loaded nanostructured lipid carriers in glioblastoma multiforme cells |
title_fullStr |
Development, characterization and in vitro cytotoxicity of kaempferol-loaded nanostructured lipid carriers in glioblastoma multiforme cells |
title_full_unstemmed |
Development, characterization and in vitro cytotoxicity of kaempferol-loaded nanostructured lipid carriers in glioblastoma multiforme cells |
title_sort |
Development, characterization and in vitro cytotoxicity of kaempferol-loaded nanostructured lipid carriers in glioblastoma multiforme cells |
author |
Nicoleti, Luisa Ribeiro [UNESP] |
author_facet |
Nicoleti, Luisa Ribeiro [UNESP] Di Filippo, Leonardo Delello [UNESP] Duarte, Jonatas Lobato [UNESP] Luiz, Marcela Tavares [UNESP] Sábio, Rafael Miguel [UNESP] Chorilli, Marlus [UNESP] |
author_role |
author |
author2 |
Di Filippo, Leonardo Delello [UNESP] Duarte, Jonatas Lobato [UNESP] Luiz, Marcela Tavares [UNESP] Sábio, Rafael Miguel [UNESP] Chorilli, Marlus [UNESP] |
author2_role |
author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Estadual Paulista (UNESP) |
dc.contributor.author.fl_str_mv |
Nicoleti, Luisa Ribeiro [UNESP] Di Filippo, Leonardo Delello [UNESP] Duarte, Jonatas Lobato [UNESP] Luiz, Marcela Tavares [UNESP] Sábio, Rafael Miguel [UNESP] Chorilli, Marlus [UNESP] |
dc.subject.por.fl_str_mv |
Brain cancer Drug delivery Flavonoids Lipid nanoparticles |
topic |
Brain cancer Drug delivery Flavonoids Lipid nanoparticles |
description |
Glioblastoma multiforme is the most common and most aggressive human brain cancer. GBM treatment is still a challenge because many drugs are not able to cross the blood-brain barrier, in addition to the increasing resistance to currently available chemotherapy. New therapeutic alternatives are emerging, and, in this context, we highlight kaempferol, a flavonoid with remarkable anti-tumor activity but with limited bioavailability due to its strong lipophilic property. A promising tool to improve the biopharmaceutical properties of molecules such as kaempferol is the use of drug-delivery nanosystems, such as nanostructured lipid carriers (NLC), which can facilitate the dispersion and delivery of highly lipophilic molecules. The present work aimed at the development and characterization of kaempferol-loaded NLC (K-NLC) and the evaluation of its biological properties using in vitro models. The K-NLC showed an average size of 120 nm, zeta potential of − 21 mV, and polydispersity index of 0.099. The K-NLC presented high kaempferol encapsulation efficiency (93%), a drug loading of 3.58%, and a sustained kaempferol release profile for up to 48 h. In addition to presenting a 7-fold increase in kaempferol cytotoxicity, its encapsulation in NLC promoted a cellular uptake of 75%, which corroborates with increased cytotoxicity in U-87MG cells, as observed. Together, these data reinforce the promising antineoplastic properties of kaempferol in addition to the key role of NLC as a platform for the efficient delivery of lipophilic drugs to neoplastic cells, which improved their uptake and therapeutic efficacy in glioblastoma multiforme cells. |
publishDate |
2023 |
dc.date.none.fl_str_mv |
2023-07-29T16:10:48Z 2023-07-29T16:10:48Z 2023-06-01 |
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.colsurfb.2023.113309 Colloids and Surfaces B: Biointerfaces, v. 226. 1873-4367 0927-7765 http://hdl.handle.net/11449/249846 10.1016/j.colsurfb.2023.113309 2-s2.0-85152110126 |
url |
http://dx.doi.org/10.1016/j.colsurfb.2023.113309 http://hdl.handle.net/11449/249846 |
identifier_str_mv |
Colloids and Surfaces B: Biointerfaces, v. 226. 1873-4367 0927-7765 10.1016/j.colsurfb.2023.113309 2-s2.0-85152110126 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Colloids and Surfaces B: Biointerfaces |
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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1808129323627970560 |