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辅酶 Q₁₀ 多不饱和脂肪酸纳米乳的制剂、表征及药代动力学研究。

Formulation, characterization and pharmacokinetic studies of coenzyme Q₁₀ PUFA's nanoemulsions.

机构信息

Université de Lorraine, Laboratoire d'Ingénierie des Biomolécules, ENSAIA, 2 av. de Forêt de Haye, 54500 Vandœuvre-lès-Nancy, France.

出版信息

Eur J Pharm Sci. 2012 Sep 29;47(2):305-12. doi: 10.1016/j.ejps.2012.06.008. Epub 2012 Jun 23.

Abstract

Coenzyme Q(10) (CoQ(10)) is an insoluble antioxidant molecule with great biological value but exhibit poor bioavailability. To improve the bioavailability of CoQ(10), we have proposed to formulate a nanoemulsion consisting of salmon oil, salmon lecithin, CoQ(10) and water. A commercial oily mixture, based on soybean oil and CoQ(10), was used for comparison, as well as a second oily mixture, composed of salmon lecithin, salmon oil and CoQ(10). Salmon oil and salmon lecithin were used as sources of polyunsaturated fatty acids (PUFA). The maximum solubility of CoQ(10) in salmon oil was 81.30 ± 0.08 mg/mL at 37 °C. Mean droplets size of the control and CoQ(10) nanoemulsions was 164 and 167 nm, respectively. The nanoemulsion was stable during 30 days at 25 °C. Bioavailability was evaluated as the area under the curve of CoQ(10) plasma concentration in male Wistar rats following oral administration of the three formulations of CoQ(10). The nanoemulsion increases at twice the bioavailability of CoQ(10) than conventional oily formulations regardless the nature of used fatty acids (soybean and salmon oils). Prepared nanoemulsion represents a vectorization of both LC-PUFAs and CoQ(10). That could be an interesting way to increase the absorption of these two bioactive molecules with natural low availability.

摘要

辅酶 Q(10)(CoQ(10))是一种不溶性抗氧化分子,具有很高的生物学价值,但生物利用度较差。为了提高 CoQ(10)的生物利用度,我们提出了一种由鱼油、鱼卵磷脂、CoQ(10)和水组成的纳米乳剂配方。我们使用了一种基于大豆油和 CoQ(10)的商业油性混合物作为对照,以及另一种由鱼卵磷脂、鱼油和 CoQ(10)组成的油性混合物。鱼油和鱼卵磷脂被用作多不饱和脂肪酸(PUFA)的来源。在 37°C 下,CoQ(10)在鱼油中的最大溶解度为 81.30±0.08mg/mL。对照和 CoQ(10)纳米乳的平均液滴大小分别为 164nm 和 167nm。纳米乳在 25°C 下稳定 30 天。雄性 Wistar 大鼠口服三种 CoQ(10)制剂后,CoQ(10)血浆浓度曲线下面积评估了生物利用度。纳米乳的生物利用度是常规油性制剂的两倍,与所用脂肪酸(大豆油和鱼油)的性质无关。制备的纳米乳代表了 LC-PUFA 和 CoQ(10)的载体化。这可能是一种增加这两种天然低生物利用度生物活性分子吸收的有趣方法。

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