RCSI School of Pharmacy, Royal College of Surgeons in Ireland, St Stephen's Green, Dublin 2, Ireland.
Department of Pharmacy and Pharmacology, University of Bath, UK.
Adv Drug Deliv Rev. 2016 Nov 15;106(Pt B):277-319. doi: 10.1016/j.addr.2016.06.005. Epub 2016 Jun 16.
Intestinal permeation enhancers (PEs) are one of the most widely tested strategies to improve oral delivery of therapeutic peptides. This article assesses the intestinal permeation enhancement action of over 250 PEs that have been tested in intestinal delivery models. In depth analysis of pre-clinical data is presented for PEs as components of proprietary delivery systems that have progressed to clinical trials. Given the importance of co-presentation of sufficiently high concentrations of PE and peptide at the small intestinal epithelium, there is an emphasis on studies where PEs have been formulated with poorly permeable molecules in solid dosage forms and lipoidal dispersions.
肠渗透增强剂 (PEs) 是提高治疗性肽口服递送最广泛测试的策略之一。本文评估了在肠道递送模型中测试的超过 250 种 PEs 的肠渗透增强作用。对于已进入临床试验的专有递送系统的组成部分的 PEs，本文提供了深入的临床前数据分析。鉴于足够高浓度的 PE 和肽在小肠上皮细胞共呈现的重要性，本文重点介绍了将 PEs 与固体剂型和类脂分散体中渗透性差的分子联合应用的研究。
