Glucocorticoid-Loaded Core-Cross-Linked Polymeric Micelles with Tailorable Release Kinetics for Targeted Therapy of Rheumatoid Arthritis (pages 7254–7258)
Dr. Bart J. Crielaard, Dr. Cristianne J. F. Rijcken, Dr. Lingdong Quan, Steffen van der Wal, Isil Altintas, Martin van der Pot, Dr. John A. W. Kruijtzer, Prof. Rob M. J. Liskamp, Dr. Raymond M. Schiffelers, Dr. Cornelus F. van Nostrum, Prof. Wim E. Hennink, Prof. Dong Wang, Dr. Twan Lammers and Prof. Gert Storm
Article first published online: 12 JUN 2012 | DOI: 10.1002/anie.201202713
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.