Development, characterization and in vitro cytotoxicity of kaempferol-loaded nanostructured lipid carriers in glioblastoma multiforme cells
dc.contributor.author | Nicoleti, Luisa Ribeiro [UNESP] | |
dc.contributor.author | Di Filippo, Leonardo Delello [UNESP] | |
dc.contributor.author | Duarte, Jonatas Lobato [UNESP] | |
dc.contributor.author | Luiz, Marcela Tavares [UNESP] | |
dc.contributor.author | Sábio, Rafael Miguel [UNESP] | |
dc.contributor.author | Chorilli, Marlus [UNESP] | |
dc.contributor.institution | Universidade Estadual Paulista (UNESP) | |
dc.date.accessioned | 2023-07-29T16:10:48Z | |
dc.date.available | 2023-07-29T16:10:48Z | |
dc.date.issued | 2023-06-01 | |
dc.description.abstract | 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. | en |
dc.description.affiliation | São Paulo State University “Júlio de Mesquita Filho” School of Pharmaceutical Sciences, São Paulo | |
dc.description.affiliationUnesp | São Paulo State University “Júlio de Mesquita Filho” School of Pharmaceutical Sciences, São Paulo | |
dc.description.sponsorship | Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) | |
dc.description.sponsorshipId | FAPESP: 19/17913–5 | |
dc.description.sponsorshipId | FAPESP: 2019/25125–7 | |
dc.description.sponsorshipId | FAPESP: 2020/12622–0 | |
dc.identifier | http://dx.doi.org/10.1016/j.colsurfb.2023.113309 | |
dc.identifier.citation | Colloids and Surfaces B: Biointerfaces, v. 226. | |
dc.identifier.doi | 10.1016/j.colsurfb.2023.113309 | |
dc.identifier.issn | 1873-4367 | |
dc.identifier.issn | 0927-7765 | |
dc.identifier.scopus | 2-s2.0-85152110126 | |
dc.identifier.uri | http://hdl.handle.net/11449/249846 | |
dc.language.iso | eng | |
dc.relation.ispartof | Colloids and Surfaces B: Biointerfaces | |
dc.source | Scopus | |
dc.subject | Brain cancer | |
dc.subject | Drug delivery | |
dc.subject | Flavonoids | |
dc.subject | Lipid nanoparticles | |
dc.title | Development, characterization and in vitro cytotoxicity of kaempferol-loaded nanostructured lipid carriers in glioblastoma multiforme cells | en |
dc.type | Artigo | |
unesp.department | Fármacos e Medicamentos - FCF | pt |