Glucocorticoid-loaded core-crosslinked polymeric micelles with tailorable release kinetics for targeted rheumatoid arthritis therapy

摘要

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.