基于Pickering乳剂原理的、以难溶性药物固体纳米粒子为唯一界面稳定剂的口服“前纳米乳”研究

项目名称： 基于Pickering乳剂原理的、以难溶性药物固体纳米粒子为唯一界面稳定剂的口服“前纳米乳”研究

项目编号： No.81202475

项目类型： 青年科学基金项目

立项/批准年度： 2013

项目学科： 药物学、药理学

项目作者： 魏晓慧

作者单位： 上海交通大学

项目金额： 23万元

中文摘要： 本课题提出了一种全新的难溶性药物口服纳米乳剂：用具有生物学活性的难溶性药物的固体纳米粒子，取代现有的"惰性"无机或有机纳米粒子，作为唯一的油水界面稳定剂，制备基于Pickering乳剂原理的"前纳米乳"，从而明显提高难溶性药物的载药量和乳剂的稳定性，并且消除表面活性剂所带来的刺激性和安全性问题，这种构想尚未见文献报道。同时，通过研究难溶性药物固体纳米粒子的界面稳定行为及其影响因素，以及这样的乳剂体系在细胞水平和动物体内的吸收过程和机制，理解药物固体纳米粒子的表面性质与其界面稳定效果和体内吸收的关系。从而从促进吸收的角度，针对性地对药物固体纳米颗粒进行有效的表面性质调控，改善药物的吸收。这将改变现有的乳剂的载药和输送思路（即药物需要溶解或分散于油相中，并主要以乳滴形式被吸收），发展为一种新型的完全不含表面活性剂，但具有高载药量，高稳定性和良好吸收效果的难溶性药物口服纳米乳给药系统。

中文关键词： Pickering乳剂；难溶性药物；纳米粒子；热力学；DSC

英文摘要： A novel surfactants free oral nanoemulsion delivery system of poorly soluble drugs through the preparation of Pickering emulsion was proposed. Different from the reported inactive inorganic or organic nanoparticles widely adopted as the stabilization agents for Pickering emulsion, in this study, the nanoparticles of poorly soluble drugs themselves with modified surface properties were introduced as the sole stabilization agent for the emulsion system. The loading capacity and the physical stability of the resulted emulsion system would be expected to be greatly improved due to the large oil water intafaces and the intrinsic good stability of Pickering emulsion. The surface properties of the drugs nanoparticles and the relationship to their interfacial behaviors as well as their stabilization effect would be emphasized as the first important point; the second important point would be the oral absorption mechanism for the novel nanoemulsion system. Based on the results of these two studies, we hope we could get a clear and deep understanding of the effect of the surface properties of the drugs nanoparticles on the stabilization of oil water interfaces and the resulted in vivo absorption behavior. Then, more efficient and more specific surface properties modification to the poorly soluble drugs nanoparticles would

英文关键词： Pickering emulsion；insoluble drug；nanoparticle；thermodynamics；DSC