受肠上皮细胞顶侧(AP)和基底侧(BL)双重脂膜屏障的限制作用，大量候选化合物的口服吸收较差，生物利用度低，导致在成药过程中被淘汰。为改善药物的跨上皮吸收效率，各种微纳米递药系统不断涌现，该些递药系统一定程度上改善了药物跨AP膜的摄取能力，却仍难以突破BL膜屏障，导致促吸收效果有限。因此，有必要开发一种更高效的新型递药技术，以进一步提高药物的跨上皮吸收效率。研究发现，机体对于甘油三酯的吸收拥有一套特有的自主选择性吸收机制，这使得甘油三酯可高效地跨越上皮细胞AP和BL膜的双重屏障而快速吸收，本文旨在设计一基于甘油三酯结构的智能化前体药物，以使难吸收药物分子主动参与到机体内甘油三酯的消化吸收途径，以其特有的选择性吸收机制，突破限制其吸收的AP和BL侧双重脂膜屏障。本项目开发的智能化前体药物技术，为难吸收候选药物的口服递送提供一种新的策略，有望更高效地提高药物的口服吸收。

The oral absorption of most drug candidates was hampered by the apical (AP) and basolateral (BL) lipid membrane barriers of gastrointestinal epithelium, which led to the final abandonment for these candidates before their clinical trial. In order to improve the drug transport efficacy across the epithelium, various of micro- or nanocarriers were developed overcoming the epithelial AP membrane barrier. However, limited drug absorption was achieved by these carriers due to their low efficiency to penetrate the BL barriers. Thus, it is necessary to develop a new oral delivery system to overcome these dual lipid barriers of epithelium efficiently. In this study, we designed a triglycerides-mimetic functional prodrug, which would effectively penetrate across the dual barriers of epithelial cells in the way of the absorption pathway for triglycerides. This delivery technology provides a new strategy for the oral delivery of poorly absorbed drug.