title: Synthesis and cytotoxicity of brefeldin A conjugated monomethoxy-poly(ethylene glycol)-b-poly(L-lactide) polymeric micelles.
abstract: A diblock copolymer of monomethoxy-poly(ethylene glycol)-b-poly(L-lactide) (MePEG-PLLA)/brefeldin A (BFA) conjugate was synthesized by the reaction of carboxyl-terminated copolymer MePEG-PLLA with BFA in the presence of dicyclohexylcarbodiimide and dimethylaminopyridine. The conjugation efficiency was found to be 95%. Its structure was confirmed by (1)H nuclear magnetic resonance and gel permeation chromatography. The MePEG-PLLA/BFA conjugate could self-assemble into micelles in aqueous solutions with a low critical micelle concentration of 1.8 × 10(-3 )g/L. Dynamic light scattering and transmission electron microscopy analyses of the MePEG-PLLA/BFA micelles revealed their spherical structure with an average diameter of 120 nm. The release profiles of BFA in PBS were measured by high performance liquid chromatography (HPLC), demonstrating that the controlled release of BFA can be gained for long time. The in vitro antitumor activity of the conjugate micelles against human liver carcinoma HepG2 cells was evaluated by 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyl tetrazolium bromide method, and the results showed that BFA can be released from the conjugate micelles without losing cytotoxicity.
authors: Department of Chemistry, Institute of Polymers, Nanchang University, 999 Xuefu Avenue, Nanchang 330031, China.
authors: Wanyun
authors: W
authors: Liu
authors: Junchao
authors: J
authors: Wei
authors: Ping
authors: P
authors: Huo
authors: Yunhua
authors: Y
authors: Lu
authors: Yiwang
authors: Y
authors: Chen
authors: Yen
authors: Y
authors: Wei
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D020126:Brefeldin A / Q000737:chemistry* / Q000494:pharmacology; D004337:Drug Carriers; D056945:Hep G2 Cells; D006801:Humans; D008823:Micelles; D008970:Molecular Weight; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D013778:Tetrazolium Salts / Q000737:chemistry; D013844:Thiazoles / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; D011091:Polyesters; D013778:Tetrazolium Salts; D013844:Thiazoles; C492425:methoxy poly(ethylene glycol)-poly(lactide); D020126:Brefeldin A; D011092:Polyethylene Glycols; C033616:poly(lactide); C022616:thiazolyl blue