Preparation of well-defined ibuprofen prodrug micelles by RAFT polymerization.

Preparation of well-defined ibuprofen prodrug micelles by RAFT polymerization. Biomacromolecules. 2013 Aug 12; Authors: Hasegawa U, van der Vlies AJ, Wandrey C, Hubbell JA Abstract Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used to treat acute pain, fever and inflammation and are being explored in a new indication in cancer. Side effects associated with long-term use of NSAIDs such as gastrointestinal damage and elevated risk of stroke, however, can limit their use and exploration in new indications.　Here we report a facile method to prepare well-defined amphiphilic diblock copolymer NSAID prodrugs by direct reversible addition fragmentation transfer (RAFT) polymerization of the acrylamide derivative of ibuprofen (IBU), a widely used NSAID. The synthesis and self-assembling behavior of amphiphilic diblock copolymers (PEG-PIBU) having a hydrophilic poly(ethylene glycol) block and a hydrophobic IBU-bearing prodrug block were investigated. Release profiles of IBU from the micelles by hydrolysis were evaluated. Furthermore, the anti-proliferative action of the IBU-containing micelles in human cervical carcinoma (HeLa) and murine melanoma (B16-F10) cells was assessed. PMID: 23937521 [PubMed - as supplied by publisher]
Source: Biomacromolecules - Category: Biochemistry Authors: Tags: Biomacromolecules Source Type: research