多肽类药物鼻腔给药研究进展

Research advances of nasal delivery of peptide drugs

随着生物制药技术的发展,越来越多的多肽类药物在医药领域得到应用。但由于这类药物稳定性不佳、口服易被酶解等问题,临床多采用注射途径给药。鼻腔给药不仅能够克服口服给药的首过效应、注射给药的顺应性差等问题,而且具有脑靶向、低剂量高活性的优点。本文主要就多肽类药物的鼻腔给药进行综述,系统地介绍了鼻腔的组织构造,药物本身性质、制剂的特性和鼻腔内环境对药物鼻腔吸收的影响,以及通过添加吸收促进剂、酶抑制剂和设计成不同药物载体等方法改善药物鼻腔吸收,并叙述了鼻腔给药的研究热点-鼻脑传递,为后续相关制剂研发提供参考。

With the rapid development of biopharmaceutical technology,more and more peptide agents are applied in clinical medicine.However,due to their problems of poor stability and easy enzymolysis by oral administration,injections are often employed.Nasal dosing can not only overcome the problems of the first pass effect of oral administration and poor compliance of injection form,but also offers the advantages of brain targeting,low dose and high potency.Focusing upon nasal dosing of peptide drugs,this review systematically explored the tissue structure of nasal cavity,influencing factors and improvement methods of peptide nasal drug delivery and research focus of nasal drug delivery.Nasal-brain delivery was also described so as to provide references for the development of related preparations.