基于酪蛋白磷酸肽/壳聚糖自组装构建月见草素纳米粒及其吸收机制研究

桉叶中富含的月见草素(OeB)是一种极具开发前景的抗氧化功能活性物，但较低的口服生物利用度限制其应用。项目基于乳源生物活性肽-酪蛋白磷酸肽与天然活性多糖-壳聚糖自组装，合理设计新型聚电解质纳米粒来输送OeB，以改善其吸收缺陷，两种原料针对OeB具有独特的承载和靶向传递效果。项目通过分析构建过程中影响因素与纳米粒生物表征指标之间的相关性，优化构建条件，建立构建模型组，包括构建条件模型和作用力模型两部分。模型组的构建有利于更好的理解自组装理论、预测输送系统的稳定性和优化纳米粒构建过程。在模型构建的基础上，项目借助体内外实验模型，重点研究OeB纳米粒口服释放、吸收、代谢机制及潜在毒性，系统讨论纳米尺度粒子在通过胃肠道时的生物学过程基本问题。最终阐释纳米技术如何提高OeB生物利用度这一科学问题。该研究结果为纳米尺度物质吸收机制的理论体系提供基础数据，为研究高效的抗氧化保健新产品提供理论依据。

Oenothein B (OeB) abundant in eucalyptus leaf is a kind of antioxidant phytochemicals with a brilliant commercial prospect. But its poor oral-bioavailability is often the main reason for limiting their application. To solve this problem, a novel polyelectrolyte nanoparticle (PNP) delivery carrier fabricated by self-assembly behavior of casein phosphopeptides and chitosan, was developed to deliver OeB in this project. And the two materials had unique encapsulation and targeting delivery effects on OeB. The model groups including build conditions model and interaction forces model between casein phosphopeptides and chitosan were built based on the analysis of specific nanoparticle characteristics on the biological fate of OeB encapsulated in PNP, which was helpful to further understand self-assembling theory, predict stability of PNP, and optimize fabrication process. In addition, the physical and chemical properties and the biological fate of PNP were systematically studied by using in vitro and in vivo models to determine OeB PNPs oral digestion, absorption, distribution, metabolism and potential toxicity. The overall objective of this project is to address the lack of knowledge why the bioavailability of OeB can be substantially increased by encapsulation in PNP. At the completion of this project, we will have gained detailed fundamental knowledge about the impact of specific characteristics of the OeB PNP on the mechanisms of digestion within the GI tract, and provided theoretical basis for developing high-efficiency antioxidant health products.