a School of Pharmacy, Faculty of Medicine and Health Sciences , Keele University , Keele , UK.
b Molecular and Clinical Pharmacology, Institute of Translational Medicine , University of Liverpool , Liverpool , UK.
Expert Rev Gastroenterol Hepatol. 2018 Mar;12(3):223-236. doi: 10.1080/17474124.2018.1399794. Epub 2017 Nov 8.
Nano-scale formulations are being developed to improve the delivery of orally administered medicines, and the interactions between nanoformulations and the gastrointestinal luminal, mucosal and epithelial environment is currently being investigated. The mucosal surface of the gastrointestinal tract is capable of trapping and eliminating large particles and pathogens as part of the natural defences of the body, it is becoming clearer that nanoformulation properties such as particle size, charge, and shape, as well as mucous properties such as viscoelasticity, thickness, density, and turn-over time are all relevant to these interactions. However, progress has been slow to utilise this information to produce effective mucous-penetrating particles. Areas covered: This review focuses on delivery method of nanomedicines both into and across the gastrointestinal mucosal surface, and aims to summarise the biological barriers that exist to successful oral nanomedicine delivery and how these barriers may be investigated and overcome. Expert commentary: Despite successes in the laboratory, no nanotechnology-enabled products are currently in clinical use which either specifically target the intestinal mucous surface or cross the epithelial barrier intact. New nanomedicine-based treatments of local diseases (intestinal cancer, inflammation, infection) and systemic diseases are advancing towards clinical use, and offer genuine opportunities to improve therapy.
正在开发纳米级制剂以改善口服药物的递送，目前正在研究纳米制剂与胃肠道腔、黏膜和上皮环境之间的相互作用。胃肠道的黏膜表面能够捕获和消除大颗粒和病原体，这是身体自然防御的一部分，现在越来越清楚的是，纳米制剂的性质，如粒径、电荷和形状，以及黏液的性质，如粘弹性、厚度、密度和更新时间，都与这些相互作用有关。然而，将这些信息用于生产有效的穿透黏液的颗粒的进展缓慢。涵盖领域：本综述重点介绍了纳米药物在胃肠道黏膜表面的输送方法，并旨在总结成功的口服纳米药物输送所存在的生物学障碍，以及如何研究和克服这些障碍。专家评论：尽管在实验室取得了成功，但目前没有任何基于纳米技术的产品专门针对肠道黏液表面或完整地穿过上皮屏障在临床中使用。基于新型纳米药物的局部疾病（肠道癌症、炎症、感染）和全身性疾病的治疗方法正在向临床应用推进，并为改善治疗提供了真正的机会。
