Development, characterization and in vitro cytotoxicity of kaempferol-loaded nanostructured lipid carriers in glioblastoma multiforme cells

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dc.contributor.authorNicoleti, Luisa Ribeiro [UNESP]
dc.contributor.authorDi Filippo, Leonardo Delello [UNESP]
dc.contributor.authorDuarte, Jonatas Lobato [UNESP]
dc.contributor.authorLuiz, Marcela Tavares [UNESP]
dc.contributor.authorSábio, Rafael Miguel [UNESP]
dc.contributor.authorChorilli, Marlus [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (UNESP)
dc.date.accessioned2023-07-29T16:10:48Z
dc.date.available2023-07-29T16:10:48Z
dc.date.issued2023-06-01
dc.description.abstractGlioblastoma 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.en
dc.description.affiliationSão Paulo State University “Júlio de Mesquita Filho” School of Pharmaceutical Sciences, São Paulo
dc.description.affiliationUnespSão Paulo State University “Júlio de Mesquita Filho” School of Pharmaceutical Sciences, São Paulo
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipIdFAPESP: 19/17913–5
dc.description.sponsorshipIdFAPESP: 2019/25125–7
dc.description.sponsorshipIdFAPESP: 2020/12622–0
dc.identifierhttp://dx.doi.org/10.1016/j.colsurfb.2023.113309
dc.identifier.citationColloids and Surfaces B: Biointerfaces, v. 226.
dc.identifier.doi10.1016/j.colsurfb.2023.113309
dc.identifier.issn1873-4367
dc.identifier.issn0927-7765
dc.identifier.scopus2-s2.0-85152110126
dc.identifier.urihttp://hdl.handle.net/11449/249846
dc.language.isoeng
dc.relation.ispartofColloids and Surfaces B: Biointerfaces
dc.sourceScopus
dc.subjectBrain cancer
dc.subjectDrug delivery
dc.subjectFlavonoids
dc.subjectLipid nanoparticles
dc.titleDevelopment, characterization and in vitro cytotoxicity of kaempferol-loaded nanostructured lipid carriers in glioblastoma multiforme cellsen
dc.typeArtigo
unesp.departmentFármacos e Medicamentos - FCFpt

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Araraquara - FCF - Faculdade de Ciências Farmacêuticas