Loading and Controlled Releasing of Anti-cancer Drug Bortezomib by Glucose-Containing Diblock Copolymer
A glucose-containing diblock copolymer was employed as nanocarrier in this study for delivery of the anticancer drug bortezomib (BTZ). Our system was based on pH-induced dynamical conjugation of boronic acid on BTZ to cis-diols on glucose-containing polymer. Diblock copolymer poly(ethylene glycol)-b-poly (gluconamidoethyl methacrylate) (PEG-PGAMA), was firstly synthesized via atom transfer radical polymerization(ATRP) by successive polymerization of monomer gluconamidoethyl methacrylate (GAMA) using a PEG-based ATRP macroinitiator. BTZ was then loaded in glucose-containing copolymer as chemical conjugation occurred of boronic acid to glucose groups and the drug-released behavior of this system was simulated in vitro. The results demonstrated that PEG-PGAMA copolymer had strong ability to bind BTZ at physiological pH of 7.4; it could also effectively release BTZ at acid pH of 5.5(close to environment of cancer tissue or the subcellular endosome) in a pH-dependent manner. In our study, a facile and interesting nanocarrier system for anti-cancer drug bortezomib (BTZ) was provided with a kind of glucose-containing block copolymer without any need of chemical modification, which only utilized dynamic chemical complexation to reach effective drug-loading and controlled release of BTZ upon responsiveness to external pH.
KeywordsDynamic chemical complexation Glucose BTZ Diblock copolymer pH-responsive
The authors gratefully acknowledged the financial support of the National Natural Science Foundation of China (No. 21204010, No. 51473035), and the Research Program of Shanghai Science and Technology Commission (No. 13NM1400102).
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