Glucocorticoid-loaded core-cross-linked polymeric micelles with tailorable release kinetics for targeted therapy of rheumatoid arthritis.

Glucocorticoid-loaded core-cross-linked polymeric micelles with tailorable release kinetics for targeted therapy of rheumatoid arthritis.
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糖皮质激素负载的核心连锁聚合物胶束具有可降低的释放动力学,用于靶向类风湿关节炎的靶向治疗。

DOI:
10.1002/anie.201202713
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发表时间:
2012-07-16
影响因子:
16.6
通讯作者:
Storm, Gert
Storm, Gert
中科院分区:
化学1区
文献类型:
--
作者:
Crielaard, Bart J.;Rijcken, Cristianne J. F.;Quan, Lingdong;van der Wal, Steffen;Altintas, Isil;van der Pot, Martin;Kruijtzer, John A. W.;Liskamp, Rob M. J.;Schiffelers, Raymond M.;van Nostrum, Cornelus F.;Hennink, Wim E.;Wang, Dong;Lammers, Twan;Storm, Gert

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为了实现类风湿性关节炎治疗的高效糖皮质激素靶向,新型可聚合且可水解裂解的地塞米松 (DEX) 衍生物被共价包埋在核心交联的聚合物胶束中。通过改变药物连接体中硫醚的氧化程度,可以严格控制 DEX 的释放速率。在施用释放速度最快的 DEX 胶束后,在两种不同的炎症性关节炎动物模型中实现了高效的疾病治疗。
To achieve highly effective glucocorticoid targeting for rheumatoid arthritis therapy, novel, polymerizable and hydrolytically cleavable dexamethasone (DEX) derivatives were covalently entrapped in core-crosslinked polymeric micelles. By varying the oxidation degree of the thioether in the drug linker, the release rate of DEX could be tightly controlled. Upon administration of the most rapidly releasing DEX-micelles, highly efficient disease treatment was achieved in two different animal models of inflammatory arthritis.
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