Synthesis, self‐assembly in water, and cytotoxicity of MPEG‐block‐PLLA/DX conjugates

Abstract Docetaxel (DX) is one of the most effective antineoplastic drugs. Its current clinical administration is limited because of its hydrophobicity and serious side effects. A polymer/DX conjugate is designed and successfully prepared to solve these problems. It is monomethoxy‐poly(ethylene glycol)‐block‐poly(L‐lactide)/DX (MPEG‐PLLA/DX). It was synthesized by reacting DX with carboxyl‐terminated copolymer MPEG‐PLLA, which was prepared by reacting succinic anhydride with hydroxyl‐terminated copolymer monomethoxy‐poly(ethylene glycol)‐block‐poly(L‐lactide) (MPEG‐PLLA). Its structure and molecular weight was confirmed by ¹H NMR and GPC. The MPEG‐PLLA/DX micelles in aqueous solution were prepared using a solvent displacement method and characterized by dynamic light scattering for size and size distribution, and by transmission electron microscopy for surface morphology. Its antitumor activity against HeLa cancer cells evaluated by MTT assay showed that it had a similar antitumor activity to pure DX at the same drug content. © 2008 Wiley Periodicals, Inc. J Biomed Mater Res, 2009