Insulin is the most effective drug in the treatment of diabetes mellitus. At present, subcutaneous injection is still the common way for insulin delivery. However, oral delivery is considered as the most preferred way for its high patient compliance and the minimal invasiveness. In this study, a novel N-acetyl-L-cysteine and arginine modified hydroxypropyl-β-cyclodextrin (NAC-HP-β-CD-Arg) was successfully synthesized and characterized. The polymer was used as a carrier for oral delivery of insulin by forming NAC-HP-β-CD-Arg@insulin complex. Enzymatic degradation study indicated that the NAC-HP-β-CD-Arg could protect insulin from enzymolysis. Moreover, the polymer exhibited strong binding ability with mucin. The transportation efficiency of NAC-HP-β-CD-Arg@insulin across the Caco-2 cell monolayer was much greater than free insulin. The in vivo study demonstrated that the orally administered NAC-HP-β-CD-Arg@insulin exhibited an excellent and sustained hypoglycemic effect in diabetic rats. It can be concluded that the NAC-HP-β-CD-Arg is a potential carrier for oral delivery of insulin.

胰岛素是治疗糖尿病最有效的药物。目前，皮下注射仍是胰岛素递送的常用方式。然而，口服给药被认为是其高患者依从性和最小侵入性的最优选方式。在这项研究中，一种新型的N-乙酰基-L-半胱氨酸和精氨酸修饰的羟丙基-β-环糊精（NAC-HP-β-CD-Arg）已成功合成和表征。通过形成NAC-HP-β-CD-Arg@胰岛素复合物，该聚合物被用作口服口服胰岛素的载体。酶促降解研究表明，NAC-HP-β-CD-Arg可以保护胰岛素免于酶解。此外，该聚合物表现出与粘蛋白的强结合能力。NAC-HP-β-CD-Arg@胰岛素跨Caco-2细胞单层的转运效率远高于游离胰岛素。的体内研究表明，口服给药NAC-HP-β-CD-精氨酸胰岛素@表现出优异的和持续的糖尿病大鼠的降血糖作用。可以得出结论，NAC-HP-β-CD-Arg是口服胰岛素的潜在载体。