David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge MA 02139, United States.
Department of Anesthesiology, Perioperative and Pain Medicine, Boston Children's Hospital, Harvard Medical School, Boston, MA, United States.
Colloids Surf B Biointerfaces. 2020 Oct;194:111202. doi: 10.1016/j.colsurfb.2020.111202. Epub 2020 Jun 17.
Both whole and processed foods contain numerous bioactive substances that improve human health and performance, including macronutrients, micronutrients, and nutraceuticals. Many of these substances are strongly hydrophobic and chemically labile, which can diminish their beneficial health effects, since only a small fraction of the ingested amount is actually absorbed and utilized by the body. In the gastrointestinal tract, the overall bioavailability of a hydrophobic substance is determined by its bioaccessibility, transformation, and absorption. The design of functional foods with enhanced biological activity depends on identifying the relative importance of these three different processes for specific bioactive substances, and then using this knowledge to optimize the nature of food matrices to boost bioavailability. In this review, we focus on the utilization of oil-in-water nanoemulsions for this purpose because their compositions, structures, and properties can be easily manipulated. Nanoemulsions can be used as delivery systems where the hydrophobic bioactive substances are loaded into the oil phase either before or after homogenization. Alternatively, they can be utilized as excipient systems. In this case, the bioactive substances are located within an existing food product (such as a fruit or vegetable), which is then consumed with a specially-designed excipient nanoemulsion (such as a sauce, dressing, or cream). Research has shown that for both delivery and excipient systems, the oral bioavailability of hydrophobic bioactives can be enhanced considerably in the presence of a nanoemulsion, provided its properties have been carefully designed. This review article outlines the principles of the design of nanoemulsion-based delivery and excipient systems for boosting the bioavailability of hydrophobic bioactive substances.
完整的和加工的食品都含有许多有益于人类健康和表现的生物活性物质，包括宏量营养素、微量营养素和营养保健品。这些物质中有许多具有很强的疏水性和化学不稳定性，这可能会降低它们对健康的有益影响，因为只有一小部分摄入的量实际上被身体吸收和利用。在胃肠道中，疏水性物质的整体生物利用度取决于其生物可及性、转化和吸收。具有增强生物活性的功能性食品的设计取决于确定这三个不同过程对特定生物活性物质的相对重要性，然后利用这一知识优化食品基质的性质，以提高生物利用度。在这篇综述中，我们专注于利用水包油纳米乳液来达到这个目的，因为它们的组成、结构和性质可以很容易地被操纵。纳米乳液可以作为输送系统，其中疏水性生物活性物质可以在均质化之前或之后装载到油相中。或者，它们可以被用作赋形剂系统。在这种情况下，生物活性物质位于现有的食品产品（如水果或蔬菜）内，然后与专门设计的赋形纳米乳液（如酱汁、调味料或奶油）一起食用。研究表明，对于输送和赋形剂系统，在纳米乳液存在的情况下，疏水性生物活性物质的口服生物利用度可以大大提高，前提是其性质已经被仔细设计。这篇综述文章概述了基于纳米乳液的输送和赋形剂系统设计原则，以提高疏水性生物活性物质的生物利用度。
