Effect of the oral administration of nanoencapsulated quercetin on a mouse model of Alzheimer’s disease

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• 作者：Lina Clara Gayoso e Ibiapina Moreno^a ; ^c ; Elena Puerta^b ; José ; Eduardo Suá ; rez-Santiago^b ; Nereide Stela Santos-Magalhã ; es^c ; Maria J. Ramirez^b ; Juan M. Irache^a ; ^{jmirache@unav.es} ; ^{juanmirache@gmail.com}
• 关键词：Quercetin (PubChem CID ; 5280343) ; Zein (PubChem SID ; 47208016) ; 2-hydroxypropyl-β-cyclodextrin (PubChem CID ; 44134771)
• 刊名：International Journal of Pharmaceutics
• 出版年：2017
• 出版时间：30 January 2017
• 年：2017
• 卷：517
• 期：1-2
• 页码：50-57
• 全文大小：753 K
• 卷排序：517

文摘

Quercetin has been identified as a promising compound with a neuroprotective potential against age-related neurodegenerative diseases such as Alzheimer's disease (AD). Nevertheless, the clinical application of quercetin is hampered by its low oral bioavailability. The aim of this work was to evaluate the capability of nanoencapsulated quercetin in zein nanoparticles (NPQ), that significantly improves the oral absorption and bioavailability of the flavonoid, as potential oral treatment for AD. For this purpose, SAMP8 mice were orally treated for two months with either NPQ (25 mg/kg every 48 h) or a solution of quercetin (Q; 25 mg/kg daily). NPQ displayed a size of 260 nm and a payload of about 70 μg/mg. For Q, no significant effects were observed in animals. On the contrary, the oral administration of NPQ improved the cognition and memory impairments characteristics of SAMP8 mice. These observations appeared to be related with a decreased expression of the hippocampal astrocyte marker GFAP. Furthermore, significant levels of quercetin were quantified in the brain of mice treated with nanoparticles. These findings highlight the potential of zein nanoparticles to promote the oral absorption of quercetin as well as the therapeutic potential of this flavonoid in AD pathogenesis.