期刊
CURRENT DRUG DELIVERY
卷 17, 期 3, 页码 229-245出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1567201817666200210120950
关键词
Nanomicelles; flavonoids; biodistribution; anti-tumor efficiency; toxicity; glioma
资金
- Natural Science Foundation of Hubei Povince, China [2013CFC071]
Background: Owing to the rich anticancer properties of flavonoids, there is the need for their incorporation into delivery vehicles like nanomicelles for safe delivery of the drug into brain tumor microenvironment. Objective: This study therefore aimed to prepare the phospholipid-based Labrasol/Pluronic F68 modified nanomicelles loaded with flavonoids (Nano-flavonoids) for the delivery of the drug to target brain tumor. 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 nano-flavonoids, 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.
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