Riddet Institute, Massey University, Private Bag 11222, Palmerston North 4442, New Zealand.
Riddet Institute, Massey University, Private Bag 11222, Palmerston North 4442, New Zealand.
J Control Release. 2020 Nov 10;327:444-455. doi: 10.1016/j.jconrel.2020.08.025. Epub 2020 Aug 25.
In this work, we sought to incorporate coenzyme Q10-loaded nanoemulsions into a food system and to understand the impact of food digestion on the in vivo bioavailability of this bioactive compound. We selected octenyl succinic anhydride modified starch as emulsifier to prepare the nanoemulsions (with approximately 200 nm droplet diameter) after comparing with two other food-grade surfactants (whey protein isolate and lecithin) in terms of their colloidal stability during simulated gastrointestinal digestion. The change in ζ-potential revealed that the initial emulsifier might be partially replaced by bile salts under intestinal conditions, and the mixed micelles formed after digestion showed an apparent permeability coefficient of 4.79 × 10 cm/s in a rat intestinal epithelial cell line, without compromising the trans-epithelial electrical resistance. In a second step, a high protein beverage that incorporated the coenzyme Q10-loaded nanoemulsion was developed in a food pilot plant. The beverage had a particle size of D = 18 μm and D = 2.5 μm, corresponding to its different components. The changes in particle morphology and size distribution were analysed to understand the behaviour of this beverage during simulated gastrointestinal digestion. When coenzyme Q10 was encapsulated into the nanoemulsions and the beverage, its bioavailability in vivo increased 1.8- and 2.8-fold respectively, compared with coenzyme Q10 dissolved in oil. The higher coenzyme Q10 bioavailability in the beverage was probably because of a significantly higher level of lipolytic activity found for beverage than for nanoemulsions during gastrointestinal digestion. These results show the potential of using natural food materials to generate formulations to improve the bioavailability of bioactive compounds. More importantly, we highlight the influence of food digestion (i.e. lipolysis) on the absorption of hydrophobic bioactive components and suggest that food systems can be utilised as a dosage form to further enhance oral bioavailability.
在这项工作中,我们试图将辅酶 Q10 负载的纳米乳液纳入食品系统,并了解食品消化对这种生物活性化合物体内生物利用度的影响。我们选择辛烯基琥珀酸酐改性淀粉作为乳化剂,在模拟胃肠道消化过程中,通过与另外两种食品级表面活性剂(乳清蛋白分离物和卵磷脂)进行比较,制备了纳米乳液(粒径约为 200nm)。ζ-电位的变化表明,在肠道条件下,初始乳化剂可能部分被胆盐取代,消化后形成的混合胶束在大鼠肠上皮细胞系中的表观渗透系数为 4.79×10cm/s,而不会影响跨上皮电阻。在第二步中,在食品中试工厂中开发了一种含有负载辅酶 Q10 的纳米乳液的高蛋白饮料。该饮料的粒径为 D=18μm 和 D=2.5μm,分别对应于其不同的成分。分析颗粒形态和粒径分布的变化,以了解该饮料在模拟胃肠道消化过程中的行为。当辅酶 Q10 被包封在纳米乳液和饮料中时,与溶解在油中的辅酶 Q10 相比,其体内生物利用度分别提高了 1.8 倍和 2.8 倍。在胃肠道消化过程中,饮料的脂肪酶活性明显高于纳米乳液,这可能是饮料中辅酶 Q10 生物利用度更高的原因。这些结果表明,使用天然食品材料来生成配方可以提高生物活性化合物的生物利用度。更重要的是,我们强调了食品消化(即脂肪分解)对疏水性生物活性成分吸收的影响,并提出可以利用食品系统作为一种剂型来进一步提高口服生物利用度。