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中国精品科技期刊2020
王忠娟,李紫菡,张秀娟,等. 基于红松籽油辅酶Q10纳米乳的制备、表征和药代动力学研究[J]. 食品工业科技,2022,43(21):225−234. doi: 10.13386/j.issn1002-0306.2022020080.
引用本文: 王忠娟,李紫菡,张秀娟,等. 基于红松籽油辅酶Q10纳米乳的制备、表征和药代动力学研究[J]. 食品工业科技,2022,43(21):225−234. doi: 10.13386/j.issn1002-0306.2022020080.
WANG Zhongjuan, LI Zihan, ZHANG Xiujuan, et al. Formulation, Characterization and Pharmacokinetic Studies of Pinus koraiensis Nuts Oil Based Coenzyme Q10 Loaded Nanoemulsion[J]. Science and Technology of Food Industry, 2022, 43(21): 225−234. (in Chinese with English abstract). doi: 10.13386/j.issn1002-0306.2022020080.
Citation: WANG Zhongjuan, LI Zihan, ZHANG Xiujuan, et al. Formulation, Characterization and Pharmacokinetic Studies of Pinus koraiensis Nuts Oil Based Coenzyme Q10 Loaded Nanoemulsion[J]. Science and Technology of Food Industry, 2022, 43(21): 225−234. (in Chinese with English abstract). doi: 10.13386/j.issn1002-0306.2022020080.

基于红松籽油辅酶Q10纳米乳的制备、表征和药代动力学研究

Formulation, Characterization and Pharmacokinetic Studies of Pinus koraiensis Nuts Oil Based Coenzyme Q10 Loaded Nanoemulsion

  • 摘要: 本文以红松籽油为油相,大豆卵磷脂为表面活性剂,无水乙醇为助表面活性剂,优化了辅酶Q10纳米乳(Coenzyme Q10 nanoemulsion,CoQ10-NE)制备工艺。研究了不同因素对CoQ10-NE平均粒径和多分散系数的影响,通过激光粒度仪,透射电镜,傅立叶红外光谱,稳定性,体外释放行为及大鼠体内药代动力学等进行表征。结果表明,当CoQ10与混合表面活性剂的质量比为3:40,CoQ10与红松籽油质量比为1:4,均质压力为800 bar,循环次数为6次时,得到平均粒径为150.30±1.43 nm、多分散系数为0.234±0.012的CoQ10-NE。透射电镜形貌微观结构表明,在1 µm和500 nm尺寸下,CoQ10-NE呈圆形,无粘连,成型性好;傅立叶红外光谱实验表明,CoQ10被完全包裹在纳米乳液中;稳定性实验结果表明,平均粒径和多分散系数整体无显著性差异(P>0.05),CoQ10-NE稳定性良好;体外释放实验结果表明,在120 min时,CoQ10-NE累积溶释放量是CoQ10混悬液的4.7倍,体外释放量显著提高。大鼠体内药代动力学实验结果表明,CoQ10-NE的最大血药浓度Cmax是CoQ10混悬液的2.80倍,CoQ10-NE在大鼠体内的药物浓度显著提高,CoQ10-NE的药时曲线下面积\rmAUC_0\text -\infty 是CoQ10混悬液的3.25倍,表明CoQ10-NE生物利用度明显提高,吸收更好。本研究所获CoQ10-NE为探索CoQ10新剂型的研发以及作为一种潜在的功能性成分应用到食品领域提供了理论基础。

     

    Abstract: Coenzyme Q10 nanoemulsion (CoQ10-NE) was improved and made utilizing Pinus koraiensis nuts oil as the oil phase, soybean lecithin as the surfactant, and ethanol as the cosurfactant in this study. The effects of different factors on the mean particle size and polydispersity index (PDI) of CoQ10-NE were studied, and the quality was evaluated by DLS, TEM, FT-IR, stability, in vitro release behavior and in vivo pharmacokinetic experiments in rats.The results showed that when the mass ratio of CoQ10 to mixed surfactant was 3:40, the mass ratio of CoQ10 to Pinus koraiensis nuts oil was 1:4, the homogenizing pressure was 800 bar, and the number of cycles was 6 times, the CoQ10-NE of mean particle size of 150.30±1.43 nm and PDI of 0.234±0.012 was obtained. The morphology and microstructure showed that the CoQ10-NE was round and non-adhesive at the size of 500 nm and 1 µm. FT-IR results showed that CoQ10 was completely encapsulated in nanoemulsion. The stability experiment showed that there was no significant difference in the mean particle size and PDI (P>0.05). CoQ10-NE had good stability. In vitro release experiments showed that the cumulative dissolution rate of CoQ10-NE was 4.7-fold that of the CoQ10 suspension at 120 min. The dissolution rate was significantly improved. According to the results of pharmacokinetic investigations in rats, the maximum plasma concentration Cmax of CoQ10-NE was 2.80-fold that of CoQ10 suspension, the drug concentration of CoQ10-NE in rats was greatly enhanced. The area \rmAUC_0\text -\infty was 3.25-fold that of the CoQ10 suspension, demonstrating that CoQ10-NE bioavailability and absorption were greatly increased. The CoQ10-NE developed in this study provides a theoretical foundation for investigating the creation of new CoQ10 formulations and their potential application as a functional ingredient in food.

     

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