A macromolecular prodrug-type injectable polymer composed of poly(depsipeptide-co-lactide)-g-PEG for sustained release of drugs†

摘要: We propose a macromolecular prodrug strategy of an injectable polymer (IP) system for continuous and sustained release water-soluble low-molecular-weight drugs. A biodegradable graft copolymer-type IP covalently immobilizing model drugs via hydrolyzable ester bonds was synthesized through the coupling reaction poly(depsipeptide-co-dl-lactide), P(DG-dl-LA), having reactive carboxylic acid side-chain groups with amino derivative drug (levofloxacin [LEV]) monomethoxy-poly(ethylene glycol) (PEG). The solution obtained IP/model conjugate exhibited temperature-responsive sol-to-gel transition between room temperature body in phosphate buffer solution, similar to P(GD-dl-LA)-g-PEG without LEV. immobilization LEV molecule onto P(DG-dl-LA)-g-PEG did not have significant influence on behavior, physical properties, or vitro degradation rates hydrogels. derivatives from P(DG-dl-LA)-g-PEG/LEV hydrogel 11 weeks, which corresponded period hydrogel, slower than that control hydrogels prepared PLGA-b-PEG-b-PLGA physically entrapped molecules. These results suggest covalent attachment is effective achieving systems can be applied delivery devices highly bioactive Copyright © 2014 John Wiley & Sons, Ltd.