口服给药方法由于其安全性、患者遵从性高、容易摄入且不引起不适以及对各种药物的耐受性而优于其他给药方法。然而，许多药物口服生物利用度较低，这是由于胃肠道中的极端条件和吸收挑战所引起的。本综述全面讨论了靶向药物运载至肠淋巴系统（ILS）的方法。它探讨了ILS的结构和生理屏障，突出了其在脂质和药物吸收和转运中的重要性。本综述介绍了利用空间精确的载体靶向ILS的各种方法，旨在提高生物利用度、实现靶向输送，并减少临床中的一通道代谢。此外，本综述还概述了利用这些载体开启ILS窗口的几种方法，为癌症治疗和口服疫苗输送的潜在临床应用铺平了道路。通过关注靶向ILS的药物载体，本文强调了这些策略在改善治疗效果和患者预后中的关键作用。总体而言，本文强调了靶向ILS的药物载体的关键作用，以及这些策略对改善治疗效果和患者预后的潜在影响。© 2023 BioMed Central Ltd.，属于Springer Nature。

Oral administration is preferred over other drug delivery methods due to its safety, high patient compliance, ease of ingestion without discomfort, and tolerance of a wide range of medications. However, oral drug delivery is limited by the poor oral bioavailability of many drugs, caused by extreme conditions and absorption challenges in the gastrointestinal tract. This review thoroughly discusses the targeted drug vehicles to the intestinal lymphatic system (ILS). It explores the structure and physiological barriers of the ILS, highlighting its significance in dietary lipid and medication absorption and transport. The review presents various approaches to targeting the ILS using spatially precise vehicles, aiming to enhance bioavailability, achieve targeted delivery, and reduce first-pass metabolism with serve in clinic. Furthermore, the review outlines several methods for leveraging these vehicles to open the ILS window, paving the way for potential clinical applications in cancer treatment and oral vaccine delivery. By focusing on targeted drug vehicles to the ILS, this article emphasizes the critical role of these strategies in improving therapeutic efficacy and patient outcomes. Overall, this article emphasizes the critical role of targeted drug vehicles to the ILS and the potential impact of these strategies on improving therapeutic efficacy and patient outcomes.© 2023. BioMed Central Ltd., part of Springer Nature.