WU Yan1, WU Cheng2, SUN Chang-zheng3, ZHAO Ying-zheng3
1.The General Hospital of Air Force, Beijing 100142, China; 2.General Hospital of the Second Artillery, Beijing 100088, China; 3.Wenzhou Medical college, Wenzhou 325035, China
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 Poloxamer188 via a amide. The resulting polymeric micelles in aqueous solution were characterized by measurement of size, ��-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.
WU Yan-,
WU Cheng-,
SUN Chang-Zheng- etc
.Preparation and Characterization of Polymeric Micelles with Chemical Conjugation of Doxorubicin(DOX-P)[J] Chinese Pharmaceutical Journal, 2014,V49(12): 1040-1044
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