Preparation and characterization of polymeric micelles with chemical conjugation of doxorubicin (DOX-P) / 中国药学杂志

ABSTRACT

OBJECTIVE: Poloxamer-doxorubicin polymer (DOX-P) was prepared through covalent binding mode via an amide bond, DOX-P can be self-assemble to form nanoscale Characterization and anti-tumor activity of chemical conjugation of doxorubicin (DOX) in polymeric micelles were investigated. METHODS: Succinic anhydride activated Poloxamer188 was first synthesized and the primary amine group in doxorubicin was conjugated to the terminal carboxyl of Poloxamerl88 via a amide. The resulting polymeric micelles in aqueous solution were characterized by measurement of size, ℰ-potential, drug loading and critical micelle concentration. RESULTS: DOX-P micelles had superiorities over physically-loaded DOX micelles in loading efficiency, diameter and CMC value. From drug release experiment in vitro, DOX-P micelles reached a sustained release profile for DOX with 10 d while physically-loaded DOX only 2 d. CONCLUSION: With low CMC value, high loading efficiency, nanometer diameter and controlled release behaviour, DOX-P micelles might be developed as a new cancer targeted delivery system.