Biodegradable vesicular nanocarriers based on poly(ε-caprolactone)-block-poly(ethyl ethylene phosphate) for drug delivery

Biodegradable polymer vesicle for drug delivery is reported. Poly(epsilon-caprolactone)-block-poly(ethyl ethylene phosphate) with well-defined structure (PCL150-b-PEEP30) has been prepared by ring-opening polymerization. It forms vesicles in aqueous solution using the thin-film hydration method and further exclusion of the as-formed vesicles results in vesicles at nano-size, demonstrated by confocal laser scanning microscope (CLSM) and transmission electron microscopy observations. Doxorubicin (DOX) has been loaded into the vesicles with a loading content of 4.38% using an acid gradient method. The release of DOX from the vesicles is accelerated in the presence of an enzyme phosphodiesterase I that is known to catalyze the degradation of polyphosphoester, achieving 83.8% release of total loaded DOX in 140 h. The DOX-loaded vesicles can be successfully internalized by A549 cells, and it results in enhanced inhibition to A549 cell proliferation, likely owning to the sustained intracellular release of DOX as observed by CLSM. With these properties, the vesicles based on the block copolymer of PCL and PEEP are attractive as drug carriers for pharmaceutical application. (C) 2009 Elsevier Ltd. All rights reserved.