Zein nanoparticles for oral delivery of quercetin: Pharmacokinetic studies and preventive anti-inflammatory effects in a mouse model of endotoxemia

详细信息    查看全文

• 作者：Rebeca Penalva ; PhD^a ; Carlos J. Gonzá ; lez-Navarro ; PhD^b ; Carlos Gamazo ; PhD^c ; Irene Esparza ; PhD^a ; Juan M. Irache ; PhD^a ; ^{jmirache@unav.es}
• 关键词：Cyclodextrin ; Quercetin ; Nanoparticles ; Oral delivery ; Sepsis
• 刊名：Nanomedicine: Nanotechnology, Biology and Medicine
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：13
• 期：1
• 页码：103-110
• 全文大小：889 K
• 卷排序：13

文摘

Zein nanoparticles were evaluated as nanocarriers to promote the oral bioavailability of quercetin and, thus, improve its anti-inflammatory effect on a mouse model of induced endotoxemia. For this purpose, the flavonoid and 2-hydroxypropyl-β-cyclodextrin were encapsulated in zein nanoparticles. The resulting nanoparticles displayed a mean size of about 300 nm and the payload was calculated to be close to 70 μg/mg nanoparticle. The release of quercetin from zein nanoparticles followed a zero-order kinetic. After oral administration, nanoparticles provided high and sustained levels of quercetin in plasma and the relative oral bioavailability was calculated to be approx. 60%. Animals treated with quercetin-loaded nanoparticles (1 dose every two days; 1 week) presented endotoxic symptoms less severe than those observed in animals treated with the oral solution of the flavonoid (1 dose every day; 1 week). This was further corroborated by the significantly low circulating TNF-alpha in the quercetin-loaded nanoparticles treated mice.