Background: Owing to the rich anticancer properties of flavonoids, there is a need for their
incorporation into drug delivery vehicles like nanomicelles for safe delivery of the drug into the brain
Objective: This study, therefore, aimed to prepare the phospholipid-based Labrasol/Pluronic F68 modified
nano micelles loaded with flavonoids (Nano-flavonoids) for the delivery of the drug to the target
Methods: Myricetin, quercetin and fisetin were selected as the initial drugs to evaluate the biodistribution
and acute toxicity of the drug delivery vehicles in rats with implanted C6 glioma tumors after oral administration,
while the uptake, retention, release in human intestinal Caco-2 cells and the effect on the brain
endothelial barrier were investigated in Human Brain Microvascular Endothelial Cells (HBMECs).
Results: The results demonstrated that nano-flavonoids loaded with myricetin showed more evenly
distributed targeting tissues and enhanced anti-tumor efficiency in vivo without significant cytotoxicity
to Caco-2 cells and alteration in the Trans Epithelial Electric Resistance (TEER). There was no pathological
evidence of renal, hepatic or other organs dysfunction after the administration of nanoflavonoids,
which showed no significant influence on cytotoxicity to Caco-2 cells.
Conclusion: In conclusion, Labrasol/F68-NMs loaded with MYR and quercetin could enhance antiglioma
effect in vitro and in vivo, which may be better tools for medical therapy, while the pharmacokinetics
and pharmacodynamics of nano-flavonoids may ensure optimal therapeutic benefits.