过饱和多甲氧基黄酮纳米乳构建及其亚稳态调控研究

The bioavailability of polymethoxyflavones (PMFs) and such lipophilic bioactive components is seriously limited due to their crystalline and low water-solubility, which might cause local toxicity as for the excess ingestion. To fabricate high-loading delivery systems of functional ingredients and maintain the their stability under digestion tract, is the important scientific issue in the field of food nutrition and food ingredients. In this project, polymethoxyflavones (PMFs) with crystallinity and poor water-solubility are chosen as typical lipophilic components. The PMFs supersaturated dissolution systems will be created by investigating the difference of molecular structure and solubility, and studying the interaction with biopolymers. Then the influence factors and maintenance strategies are exploited. Subsequently, the supersaturated PMFs emulsions are prepared and their stability and encapsulation efficiency are characterized. Finally, the in vitro and in vivo bioavailability and safety are evaluated. This research can not only provide direct theoretical and data support for the food application of important physiological active components PMFs, but also offer referential methods and ideas for effective deliver of crystalline and lipophilic functional components.

多甲氧基黄酮(PMFs)等一大类脂溶性活性组分因其易结晶、水溶性低的限制，严重制约了其生物可利用性，甚至导致超量食用而产生局部毒性。构建高荷载功能性组分递送体系并保持其在消化环境下稳定，是食品营养与食品配料领域重要科学问题。本课题拟以具结晶性和低水溶性的PMFs为代表性脂溶性组分，从其分子结构及溶解性差异出发、利用与生物大分子的组分相互作用，创建PMFs过饱和溶解体系，探究其影响因素与维持方法，在此基础上制备过饱和PMFs乳液，表征其稳定性及负载率，评估其体内外的生物可利用性及安全性。课题研究可为重要生理活性物质 PMFs 的食品应用提供直接的理论和数据支持，更可为一大类兼具结晶性和脂溶性的功能组分的有效输送提供方法的借鉴和研究思路的参考。

多甲氧基黄酮（PMFs）是一类生物活性高的功能组分，但其低水溶性、高结晶性大大限制其在食品中的应用，并降低其生物可利用度。如何提高PMFs的包载量及稳定性，提升其生物效价是本项目开展的目的。项目从三个方面开展研究：1）PMFs在油水体系中的溶解行为，结果表明PMFs具有高油水分配系数，其结晶行为与贮藏温度相关联；2）负载PMFs的乳液及结构化乳液递送体系构建，结果表明水相中沉淀抑制剂（羟丙基甲基纤维素、浓缩乳清分离蛋白）的存在可以大大提升PMFs在乳液体系中的稳定性，界面上羟丙基甲基纤维素不仅能维持PMFs的稳定性，且能进一步提升PMFs在乳液中的包载量。单月桂酸甘油酯的油相修饰通过调控乳液的粘度，改变PMFs的结晶过程，并将晶体包裹在乳液网络结构中。浓缩乳清蛋白的水相修饰通过形成复凝聚体系控制PMFs晶体的生长过程，大大提升PMFs在乳液中的稳定性及包载量。3）PMFs体外生物可给性评价，结果表明PMFs生物可给性取决于PMFs在乳液体系中的包载量及乳液体系的结构。乳液凝胶体系对PMFs的物理稳定性有很好的提升作用，此外由于其缓释效应，负载的PMFs具有低生物可给性，但能避免PMFs在胃肠道消化过程中的沉淀析出现象。