泼尼松龙
药理学
氨基葡萄糖
肾
药物输送
体内
化学
结合
靶向给药
药品
医学
内科学
生物化学
生物
有机化学
生物技术
数学分析
数学
作者
Yan Lin,Yanping Li,Xiaohong Wang,Tao Gong,Ling Zhang,Xun Sun
标识
DOI:10.1016/j.jconrel.2013.02.001
摘要
In order to develop a novel kidney-targeted drug delivery system, we synthesized prednisolone carbamate–glucosamine conjugate (PCG) using 2-glucosamine as a ligand, and investigated its potential targeting efficacy. In vitro studies demonstrated that PCG could remarkably improve the uptake of drug by kidney cells. And the specific uptake of PCG could be largely reduced by the inhibitors of megalin receptor. More importantly, PCG showed an excellent kidney targeting property in vivo, and the concentration of the conjugate in the kidney was 8.1-fold higher than that of prednisolone group at 60 min after intravenous injection. Besides, PCG could significantly reverse the disease progression in renal ischemia–reperfusion (I/R) injury animal models. Furthermore, PCG presented no adverse effect on bone density while prednisolone resulted in severe osteoporosis. Thus, it indicated that 2-glucosamine could be a potential ligand for kidney-targeted delivery of prednisolone.
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