背景：研发药物新剂型和制剂新技术已成为有望提高蛋白多肽利用率的热点，尤其是近几年的纳米技术的研究进展更是促进了蛋白质药物的临床应用。目的：综述蛋白口服纳米给药的研究现状。方法：应用计算机检索CNKI数据库、SCI数据库1996至2014年文献，检索中英文关键词为“蛋白多肽，纳米粒，口服制剂；protein，peptide drugs，nanoparticles，oral administration”。结果与结论：纳米材料种类、纳米粒粒径、表面电荷及其表面修饰等对药物的包封率、释药速度、纳米粒在胃肠道内的稳定性及透过肠黏膜的能力等方面有很大影响。纳米粒可增加蛋白药物的稳定性，提高药物的生物利用度；纳米粒的靶向性可减少某些药物的不良反应；纳米粒的缓释作用可以减少药物的用量，增加药物的体内循环时间。但纳米技术目前仍有很多问题有待解决：制备过程中不可避免地会使一些蛋白药物丧失活性；药物的包封率及载药量有待提高；蛋白突释问题不能完全解决；纳米粒目前大规模生产还很困难等。%BACKGROUND:The new formulation and preparation technology of new drugs have become a hot spot for improving the utilization of polypeptides. In particular, the development of nanotechnology in recent years has promoted the clinical application of polypeptide drugs. OBJECTIVE:To review the current research of nanoparticles as carriers of polypeptide drugs for oral administration. METHODS:A computer-based search of CNKI database and SCI database was performed for relevant articles published from 1996 to 2014 by using the keywords of“protein, peptide drugs, nanoparticles, oral administration”in Chinese and English, respectively. RESULTS AND CONCLUSION:The encapsulation efficiency, release rate of drug delivery, stability of nanoparticles in the gastrointestinal tract and penetrability of the intestinal mucosa are determined by many factors, such as the kind, size, surface charge and modification of nanoparticles. The nanoparticles can increase the stability of protein drugs and improve the bioavailability of drugs. The targeting property of the nanoparticles can decrease the adverse reactions of some drugs. The release effect of the nanoparticles can decrease the dosage of drugs and increase the drug circulating time. However, there are stil many problems to be solved in nanotechnology:the activities of some protein drugs are lost in the preparation process;theencapsulation efficiency and drug loading need to be improved;protein burst release cannot be solved completely;the mass production of nanoparticles is stil difficult.
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