Kofuji Kyoko, Murata Yoshifumi, Kawashima Susumu
Faculty of Pharmaceutical Sciences, Hokuriku University, Ho-3, Kanagawa-machi, Kanazawa 920-1181, Japan.
Int J Pharm. 2005 Oct 13;303(1-2):95-103. doi: 10.1016/j.ijpharm.2005.07.011.
Chitosan (CS) gel beads were prepared with chelated copper (II) ions as a vehicle for the delivery of peptide and protein drugs. Insulin, which is a model of peptide and protein drugs, was scarcely released from the CS gel beads in vitro, presumably due to the nature of interactions occurring between insulin, CS and the copper (II) ions. The efficacy of insulin released from the CS gel beads was confirmed by implantation into diabetic mice. A consistent reduction in blood glucose level was observed in vivo due to insulin release as the CS gel beads were degraded. Control over insulin release was achieved by altering the properties of the CS. Thus, CS gel beads are promising as a biocompatible and biodegradable vehicle by which peptide and protein drugs can be delivered.
壳聚糖（CS）凝胶珠是以螯合铜（II）离子为载体来递送肽类和蛋白质药物而制备的。胰岛素作为肽类和蛋白质药物的一个范例，在体外几乎不会从CS凝胶珠中释放出来，推测这是由于胰岛素、CS和铜（II）离子之间发生的相互作用的性质所致。将CS凝胶珠植入糖尿病小鼠体内后，证实了从中释放的胰岛素的疗效。随着CS凝胶珠的降解，体内观察到由于胰岛素释放导致血糖水平持续降低。通过改变CS的性质实现了对胰岛素释放的控制。因此，CS凝胶珠有望成为一种生物相容性和可生物降解的载体，通过它可以递送肽类和蛋白质药物。
