Preparation and characterization of biodegradable nanospheres composed of methoxy poly(ethylene glycol) and DL-lactide block copolymer as novel drug carriers

[摘要] We synthesized amphiphilic diblock copolymer based on methoxy poly(ethylene glycol) (MePEG) and DL-lactide with different molar composition in bulk without catalyst. Using the resulting amphiphilic diblock copolymers, we prepared drug-loaded polymeric nanospheres by micelle formation through solution behavior of amphiphilic copolymer in selective solvents. The structure of MePEG/DL-lactide diblock copolymers was identified by IR, WAXD, GPC, H-1-NMR. The size of nanosphere measured by dynamic light scattering showed a narrow monodisperse site distribution and average diameter less than 200 nm. From the surface chemical composition of nanosphere by ESCA, the presence of MePEG chains on the nanosphere layers was confirmed. The critical micelle concentration of ML50 sample investigated by fluorescence spectroscopy was 1.44X10(-7) mol/l which is lower than common low molecular weight surfactants. In addition, we could obtain nanospheres having a relatively high drug-loading of about 33.0% when the feed weight ratio of indomethacin to polymer was 1:1. In vitro release experiments of the indomethacin-loaded MePEG/DL-lactide nanospheres exhibited sustained release behavior without any burst effects. The results of cytotoxicity tests showed that the MePEG/DL-lactide nanospheres didn't induce any relevant cell damage. (C) 1998 Elsevier Science B.V. All rights reserved.

[发布日期] 1998-12-04

[关键词] methoxy poly(ethylene glycol);DL-lactide;amphiphilic block copolymer;nanosphere;drug delivery system