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


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.

SUBMITTER: Crielaard BJ 

PROVIDER: S-EPMC3499037 | biostudies-literature | 2012 Jul

REPOSITORIES: biostudies-literature

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

Crielaard Bart J BJ   Rijcken Cristianne J F CJ   Quan Lingdong L   van der Wal Steffen S   Altintas Isil I   van der Pot Martin M   Kruijtzer John A W JA   Liskamp Rob M J RM   Schiffelers Raymond M RM   van Nostrum Cornelus F CF   Hennink Wim E WE   Wang Dong D   Lammers Twan T   Storm Gert G  

Angewandte Chemie (International ed. in English) 20120612 29


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. ...[more]

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