靶向纳米载体用于口服胰岛素递送的研究进展  

Research Progress of Targeted Nanocarriers for Oral Insulin Delivery

作　　者：刘燕 熊向源 LIU Yan;XIONG Xiangyuan(School of Life Sciences,Jiangxi Science and Technology Normal University,Nanchang 330013,China)

机构地区：[1]江西科技师范大学生命科学学院,南昌330013

出　　处：《功能高分子学报》2024年第1期82-90,共9页Journal of Functional Polymers

基　　金：江西省自然科学基金重点项目(20212ACB206003)。

摘　　要：皮下注射胰岛素主要用于治疗糖尿病,但存在局限性。虽然口服胰岛素作为简便的给药方式,能降低副作用、提高患者的依从性;但是蛋白类药物口服后会被胃肠道酶解失活。随着纳米技术的快速发展,靶向纳米递送体系被广泛用于口服胰岛素的研究。其通过与肠细胞表面的受体进行配体-受体特异性结合,增强胰岛素的肠道吸收来提高降血糖作用。本文基于靶向纳米载体的作用机理及主要影响因素,综述了用于口服胰岛素递送的靶向纳米载体的最新进展。Subcutaneous insulin injection is mainly used to treat diabetes,but it has limitations,such as hyperinsulinemia,adipose tissue atrophy and hypoglycemia.As a simple way of administration,oral insulin can reduce side effects and improve patients’compliance.However,protein drugs can be inactivated by gastrointestinal enzymes after oral administration.In recent years,with the rapid development of nanotechnology,targeted nano-delivery systems have been widely used in the study of oral insulin.Compared with unmodified nanocarriers,targeted nano delivery system has obvious advantages.Insulin can not only be loaded by it,but also smoothly pass through the gastrointestinal barrier and be successfully transported to the site of action.At the same time,the structural stability of insulin can also be protected,so as to maintain its biological activity and finally achieve mild hypoglycemic effect.Therefore,targeted oral delivery of insulin is promising to replace the common subcutaneous injection of insulin and provide painless treatment for diabetic patients.The ligand-modified targeting nanocarriers enhance the intestinal absorption and transport of insulin by specifically binding to receptors on the surface of intestinal cells and play a mild hypoglycemic effect.The main characteristics,targeting mechanism and main factors affecting the targeting effect of targeting nanocarriers are discussed.The main factors include the size,shape and ligand density of nanoparticles.The design ideas,research methods and oral bioavailability of nano-carriers modified with different surface ligands are reviewed in detail.These targeting ligands are folic acid(FA),fragment crystallizable(Fc),biotin,polypeptide,transferrin and VB12.The existing problems and future development directions of targeting nanocarriers for oral insulin are also put forward.

关 键 词：糖尿病 靶向 纳米载体 口服胰岛素 配体含量 

分 类 号：R319[医药卫生—基础医学]