Methotrexate-loaded biodegradable polymeric micelles: preparation, physicochemical properties and in vitro drug release.

Ying Zhang, Tuo Jin, Ren-Xi Zhuo

Index: Colloids Surf. B Biointerfaces 44(2-3) , 104-9, (2005)

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Abstract

Polymeric micelles based on amphiphilic diblock copolymers methoxy poly(ethylene glycol)-polylactide with various hydrophobic lengths were designed as carriers of poorly water-soluble anticancer drug methotrexate (MTX). Relationship between physicochemical characteristics of micelles and release behavior was explored. The critical micelle concentration was determined by fluorescence spectroscopy using 9-chloromethyl anthracene as fluorescence probe. Core-shell type polymeric micelles were prepared by free-surfactant dialysis technique. The mean size of micelles loaded with MTX was 50-200 nm with narrow polydispersity. Physicochemical properties of drug-loaded micelles were evaluated. In vitro release behavior of MTX was also investigated. MTX was continuously released from micelles and less than 50% MTX was released in 5 days. Release rate was dependent on chemical structures of micelles and enhanced by decreasing polylactide lengths.