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

Autor(es)

Nicoleti, Luisa Ribeiro ; Di Filippo, Leonardo Delello ; Duarte, Jonatas Lobato ; Luiz, Marcela Tavares ; Sabio, Rafael Miguel ; Chorilli, Marlus

• Tipo de documento: Artigo Científico
• Fonte: COLLOIDS AND SURFACES B-BIOINTERFACES; v. 226, p. 7-pg., 2023-04-11.

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. (AU)

• Processo FAPESP: 19/25125-7 - Nanoemulsões contendo terpenos como potenciais larvicidas e repelentes contra Aedes aegypti (Linnaeus, 1762)
• Beneficiário: Jonatas Lobato Duarte
• Modalidade de apoio: Bolsas no Brasil - Doutorado
• Processo FAPESP: 19/17913-5 - Desenvolvimento farmacotécnico e atividade anti-Candida albicans in vitro e in vivo de carreadores lipídicos nanoestruturados dispersos em hidrogéis para administração vaginal de hipericina
• Beneficiário: Marlus Chorilli
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 20/12622-0 - Avaliação do potencial de carreadores lipídicos nanoestruturados funcionalizados com cetuximabe dispersos em hidrogéis termo-responsivos mucoadesivos para administração intranasal de temozolomida no tratamento do Glioblastoma Multiforme
• Beneficiário: Leonardo Delello Di Filippo
• Modalidade de apoio: Bolsas no Brasil - Doutorado