表面活性剂是一类多样化的化合物，具有在不同物态之间吸附的能力。它们被用作制药辅料、食品添加剂、化妆品乳化剂，并作为家庭/工业清洁剂。本综述概述了口服药物剂型中存在的表面活性剂型辅料与胃肠道（GI）的肠上皮的相互作用。许多被允许人体消费的口服产品中的表面活性剂可以在体外实验中降低肠上皮细胞的存活率，并改变上皮细胞单层、分离的GI组织黏膜以及动物模型中的屏障完整性。这表明从这些模型预测在人体中的安全问题存在一定的不匹配。最近有争议的临床前研究还暗示一些广泛使用的口服产品中使用的乳化剂可能与溃疡性结肠炎、某些代谢紊乱和癌症有关。我们对口服剂型中各种表面活性剂辅料与胃肠道的相互作用进行了综述。安全数据从体外、离体、临床前动物和人体研究进行了审查。总结了在临床前研究中观察到的表面活性剂对GI上皮产生一些潜在的刺激性效应的因素。最后，我们对口服药物剂型中表面活性剂的整体安全性进行了展望，这对于输送系统的开发具有重要意义。版权所有 © 2023. Elsevier B.V. 发布。

Surfactants are a diverse group of compounds that share the capacity to adsorb at the boundary between distinct phases of matter. They are used as pharmaceutical excipients, food additives, emulsifiers in cosmetics, and as household/industrial detergents. This review outlines the interaction of surfactant-type excipients present in oral pharmaceutical dosage forms with the intestinal epithelium of the gastrointestinal (GI) tract. Many surfactants permitted for human consumption in oral products reduce intestinal epithelial cell viability in vitro and alter barrier integrity in epithelial cell monolayers, isolated GI tissue mucosae, and in animal models. This suggests a degree of mis-match for predicting safety issues in humans from such models. Recent controversial preclinical research also infers that some widely used emulsifiers used in oral products may be linked to ulcerative colitis, some metabolic disorders, and cancers. We review a wide range of surfactant excipients in oral dosage forms regarding their interactions with the GI tract. Safety data is reviewed across in vitro, ex vivo, pre-clinical animal, and human studies. The factors that may mitigate against some of the potentially abrasive effects of surfactants on GI epithelia observed in pre-clinical studies are summarised. We conclude with a perspective on the overall safety of surfactants in oral pharmaceutical dosage forms, which has relevance for delivery system development.Copyright © 2023. Published by Elsevier B.V.