Department of Nutrition and Food Hygiene, Hubei Key Laboratory of Food Nutrition and Safety, School of Public Health, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China; Ministry of Education Key Laboratory of Environment and Health, School of Public Health, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China; College of Food Science and Engineering, Wuhan Polytechnic University, Wuhan 430023, China.
Department of Nutrition and Food Hygiene, Hubei Key Laboratory of Food Nutrition and Safety, School of Public Health, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China; Ministry of Education Key Laboratory of Environment and Health, School of Public Health, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
Colloids Surf B Biointerfaces. 2014 Mar 1;115:125-31. doi: 10.1016/j.colsurfb.2013.11.029. Epub 2013 Nov 24.
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 Cmax 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.
纳米生物技术最近被视为一种通过促进疏水性生物活性化合物在组织中的积累来提高治疗效果的有前途的策略。本研究的目的是制备一种新型的载有槲皮素的阳离子纳米结构脂质载体 (QR-CNLC),并评估其经口服给药后的体内分布。QR-CNLC 通过在高温下乳化并用各种功能成分在低温下固化来制备,并对其特性,包括物理指数、体外释放曲线和体内组织分布进行了研究。结果表明,QR-CNLC 表现出平均粒径为 126.6nm、zeta 电位为 40.5mV 和 89.3%的包封效率。与体外的槲皮素溶液相比,QR-CNLC 表现出较慢的释放速度。与对照组相比,QR-CNLC 在肺、肝和肾中的 AUC(组织浓度-时间曲线下面积)值更高,Cmax 值更高。肺、肝和肾的相对摄取率 (re) 值分别为 1.57、1.51 和 1.68,这表明与槲皮素混悬液相比,经口服 QR-CNLC 后,槲皮素可显著在肺、肾和肝中积累。总之,阳离子纳米结构脂质载体可能是一种有吸引力的用于口服递疏水性功能成分的纳米载体系统。