Liu Lin, Yao WenDong, Rao YueFeng, Lu XiaoYang, Gao JianQing
a The First Affiliated Hospital, College of Medicine, Zhejiang University , Hangzhou , PR China.
b Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University , Hangzhou , PR China , and.
Drug Deliv. 2017 Nov;24(1):569-581. doi: 10.1080/10717544.2017.1279238.
Oral administration is a desirable alternative of parenteral administration due to the convenience and increased compliance to patients, especially for chronic diseases that require frequent administration. The oral drug delivery is a dynamic research field despite the numerous challenges limiting their effective delivery, such as enzyme degradation, hydrolysis and low permeability of intestinal epithelium in the gastrointestinal (GI) tract. pH-Responsive carriers offer excellent potential as oral therapeutic systems due to enhancing the stability of drug delivery in stomach and achieving controlled release in intestines. This review provides a wide perspective on current status of pH-responsive oral drug delivery systems prepared mainly with organic polymers or inorganic materials, including the strategies used to overcome GI barriers, the challenges in their development and future prospects, with focus on technology trends to improve the bioavailability of orally delivered drugs, the mechanisms of drug release from pH-responsive oral formulations, and their application for drug delivery, such as protein and peptide therapeutics, vaccination, inflammatory bowel disease (IBD) and bacterial infections.
由于其便利性以及患者依从性的提高，口服给药是胃肠外给药的一种理想替代方式，尤其适用于需要频繁给药的慢性疾病。尽管存在诸多限制有效给药的挑战，如酶降解、水解以及胃肠道（GI）中肠上皮的低渗透性，但口服药物递送仍是一个充满活力的研究领域。pH响应性载体作为口服治疗系统具有巨大潜力，因为它可以增强药物在胃中的递送稳定性并在肠道中实现控释。本综述广泛阐述了主要由有机聚合物或无机材料制备的pH响应性口服药物递送系统的现状，包括用于克服胃肠道屏障的策略、其开发过程中的挑战以及未来前景，重点关注提高口服给药生物利用度的技术趋势、pH响应性口服制剂的药物释放机制及其在药物递送中的应用，如蛋白质和肽类治疗药物、疫苗接种、炎症性肠病（IBD）和细菌感染。
