Liao Wenzhen, Liu Zhijun, Zhang Tiantian, Sun Suxia, Ye Jufeng, Li Ziyin, Mao Lianzhi, Ren Jiaoyan
Department of Nutrition and Food Hygiene, Guangdong Provincial Key Laboratory of Tropical Disease Research, School of Public Health, Southern Medical University , No.1023 South Shatai Road, Guangzhou 510515, China.
Guangdong Polytechnic of Science and Trade , Guangzhou 510430, China.
J Agric Food Chem. 2018 Jan 10;66(1):91-98. doi: 10.1021/acs.jafc.7b03953. Epub 2017 Dec 26.
Lots of active substances are hydrophobic materials at ambient and body temperatures, decreasing their bioavailability and posing great challenges to successful incorporation into medication and functional foods. The goal of this research was to develop a nanoemulsion delivery system containing a hydrophobic crystalline bioactive component (nobiletin) to improve the anti-inflammatory activity. Nobiletin was incorporated into the oily phase, and the nanoemulsions were fabricated using high-speed and high-pressure homogenization. Particle size, polydispersity index (PDI), and zeta potential were evaluated by a commercial laser light scattering instrument. The anti-inflammatory activities were performed in LPS-stimulated RAW 264.7 cells. The developed nobiletin nanoemulsion had an average droplet size of 168.6 ± 3.8 nm and a PDI of 0.168, while the average diameter of the blank nanoemulsion was 157.3 ± 1.9 nm and its PDI was 0.161. The zeta potential values of nobiletin nanoemulsion and blank nanoemulsion were -68.45 ± 0.64 and -62.75 ± 0.21 mV, respectively. All obtained nanoemulsions kept physically stable during storage at 4, 25, and 37 °C. A nobiletin-loaded nanoemulsion showed an enhanced anti-inflammatory activity in LPS-induced macrophages, with a decrease in pro-inflammatory mediators and cytokines. The findings suggested that the nanoemulsion would be used as an effective delivery system for nobiletin to improve its anti-inflammatory activity.
许多活性物质在环境温度和体温下都是疏水材料，这降低了它们的生物利用度，并给成功纳入药物和功能性食品带来了巨大挑战。本研究的目的是开发一种包含疏水性结晶生物活性成分（川陈皮素）的纳米乳液递送系统，以提高其抗炎活性。将川陈皮素掺入油相中，并使用高速和高压均质法制备纳米乳液。通过商用激光散射仪评估粒径、多分散指数（PDI）和zeta电位。在脂多糖刺激的RAW 264.7细胞中进行抗炎活性测试。所制备的川陈皮素纳米乳液的平均液滴尺寸为168.6±3.8nm，PDI为0.168，而空白纳米乳液的平均直径为157.3±1.9nm，其PDI为0.161。川陈皮素纳米乳液和空白纳米乳液的zeta电位值分别为-68.45±0.64和-62.75±0.21mV。所有获得的纳米乳液在4、25和37℃储存期间保持物理稳定。负载川陈皮素的纳米乳液在脂多糖诱导的巨噬细胞中显示出增强的抗炎活性，促炎介质和细胞因子减少。研究结果表明，纳米乳液将作为川陈皮素的有效递送系统，以提高其抗炎活性。
