Zhou Huafeng, Liu Guoqing, Zhang Jing, Sun Ning, Duan Mingxing, Yan Zemin, Xia Qiang
State Key Laboratory of Bioelectronics, School of Biological Science and Medical Engineering, Southeast University, Nanjing 210096, China ; State Key Laboratory of Biomembrane and Membrane Biotechnology, School of Life Sciences, Tsinghua University, Beijing 100084, China ; Jiangsu Longliqi Bioscience Co., Ltd., Suzhou 215555, China.
State Key Laboratory of Bioelectronics, School of Biological Science and Medical Engineering, Southeast University, Nanjing 210096, China.
Biomed Res Int. 2014;2014:793879. doi: 10.1155/2014/793879. Epub 2014 Jun 5.
To improve the bioavailability of orally administered lipophilic coenzyme Q10 (CoQ10), we formulated a novel lipid-free nano-CoQ10 system stabilized by various surfactants. Nano-CoQ10s, composed of 2.5% (w/w) CoQ10, 1.67% (w/w) surfactant, and 41.67% (w/w) glycerol, were prepared by hot high-pressure homogenization. The resulting formulations were characterized by particle size, zeta potential, differential scanning calorimetry, and cryogenic transmission electron microscopy. We found that the mean particle size of all nano-CoQ10s ranged from 66.3 ± 1.5 nm to 92.7 ± 1.5 nm and the zeta potential ranged from -12.8 ± 1.4 mV to -41.6 ± 1.4 mV. The CoQ10 in nano-CoQ10s likely existed in a supercooled state, and nano-CoQ10s stored in a brown sealed bottle were stable for 180 days at 25 °C. The bioavailability of CoQ10 was evaluated following oral administration of CoQ10 formulations in Sprague-Dawley rats. Compared to the values observed following administration of CoQ10-Suspension, nano-CoQ10 modified with various surfactants significantly increased the maximum plasma concentration and the area under the plasma concentration-time curve. Thus, the lipid-free system of a nano-CoQ10 stabilized with a surfactant may be an effective vehicle for improving oral bioavailability of CoQ10.
为提高口服亲脂性辅酶Q10（CoQ10）的生物利用度，我们制备了一种由各种表面活性剂稳定的新型无脂质纳米CoQ10体系。通过热高压均质法制备了纳米CoQ10，其由2.5%（w/w）的CoQ10、1.67%（w/w）的表面活性剂和41.67%（w/w）的甘油组成。通过粒径、zeta电位、差示扫描量热法和低温透射电子显微镜对所得制剂进行了表征。我们发现，所有纳米CoQ10的平均粒径在66.3±1.5nm至92.7±1.5nm之间，zeta电位在-12.8±1.4mV至-41.6±1.4mV之间。纳米CoQ10中的CoQ10可能以过冷状态存在，储存在棕色密封瓶中的纳米CoQ10在25℃下可稳定180天。在Sprague-Dawley大鼠口服CoQ10制剂后评估了CoQ10的生物利用度。与给予CoQ10混悬液后观察到的值相比，用各种表面活性剂修饰的纳米CoQ10显著提高了最大血浆浓度和血浆浓度-时间曲线下面积。因此，用表面活性剂稳定的纳米CoQ10无脂质体系可能是提高CoQ10口服生物利用度的有效载体。
