载糖皮质激素的核交联聚合物胶束，具有可调节的释放动力学，用于类风湿性关节炎的靶向治疗。
Glucocorticoid-loaded core-cross-linked polymeric micelles with tailorable release kinetics for targeted therapy of rheumatoid arthritis.
机构信息
Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, Universiteitsweg 99, 3584 CG Utrecht, The Netherlands.
出版信息
Angew Chem Int Ed Engl. 2012 Jul 16;51(29):7254-8. doi: 10.1002/anie.201202713. Epub 2012 Jun 12.
Abstract
Polymerizable and hydrolytically cleavable dexamethasone (DEX, red dot in picture) derivatives were covalently entrapped in core-cross-linked polymeric micelles that were prepared from a thermosensitive block copolymer (yellow and gray building block). By varying the oxidation degree of the thioether in the drug linker, the release rate of DEX could be controlled. The DEX-loaded micelles were used for efficient treatment of inflammatory arthritis in two animal models.
摘要
将可聚合和可水解的地塞米松（DEX，图片中的红点）衍生物共价包埋在核心交联聚合物胶束中，这些胶束是由热敏嵌段共聚物（黄色和灰色结构单元）制备的。通过改变药物连接物中硫醚的氧化程度，可以控制 DEX 的释放速率。载有 DEX 的胶束用于两种动物模型中炎症性关节炎的有效治疗。
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