Characterization and biodistribution in vivo of quercetin-loaded cationic nanostructured lipid carriers
Characterization and biodistribution in vivo of quercetin-loaded cationic nanostructured lipid carriers
复制标题
负载槲皮素的阳离子纳米结构脂质载体的表征和体内生物分布。
DOI：
10.1016/j.colsurfb.2013.11.029
复制
发表时间：
2014-03-01
影响因子：
5.8
通讯作者：
Yao, Ping
中科院分区：
文献类型：
--
作者：
Liu, Liang;Tang, Yuhan;Yao, Ping
纳米生物技术最近被认为是一种很有前途的策略，以提高治疗效果，通过促进疏水生物活性化合物在组织中的积累。本研究的目的是制备一种新型的槲皮素阳离子纳米结构脂质载体（QR-CNLC），并评价其口服后的体内生物分布。采用高温乳化、低温固化的方法制备QR-CNLC，并对其物理指标、体外释药特性和体内组织分布进行了研究。结果表明，QR-CNLC的平均粒径为126.6 nm，Zeta电位为40.5 mV，包封率为89.3%。与槲皮素溶液相比，QR-CNLC在体外释放较慢。与对照组相比，QR-CNLC显示肺、肝和肾的AUC（组织浓度-时间曲线下面积）值和C-max值较高。肺、肝、肾的相对摄取率（re）值分别为1.57、1.51和1.68，表明口服QR-CNLC后，与槲皮素混悬液相比，槲皮素可在肺、肾、肝中显著蓄积。总之，阳离子纳米结构脂质载体可能是一个有吸引力的纳米载体系统，用于疏水性功能成分的口服递送。(C)2013爱思唯尔有限公司版权所有。
Nanobiotechnology has been recently viewed as a promising strategy to improve therapy efficacy by promoting the accumulation of hydrophobic bioactive compounds in tissues. The aim of present study was to formulate a novel quercetin-loaded cationic nanostructured lipid carriers (QR-CNLC) and to evaluate its biodistribution in vivo after oral administration. QR-CNLC were prepared by emulsifying at high temperature and subsequent solidifying at low temperature using various functional ingredients, and its characteristics, including physical index, release profile in vitro, and tissue distribution in vivo, were investigated. The results demonstrated that QR-CNLC exhibited an average particle size 126.6 nm, a zeta potential of 40.5 mV and 89.3% entrapment efficiency. QR-CNLC performed slower release compared with quercetin solution in vitro. QR-CNLC showed higher AUC (area under tissue concentration time curve) value and higher C-max value in lung, liver and kidney compared with control group. The value of relative intake rate (re) for lung, liver and kidney was 1.57, 1.51 and 1.68, respectively, which revealed that quercetin can be significantly accumulated in lung, kidney and liver after oral administration of QR-CNLC compared with quercetin suspension. In conclusion, cationic nanostructured lipid carriers may be an attractive nanocarrier system for oral delivery of hydrophobic functional components. (C) 2013 Elsevier B.V. All rights reserved.