Gadolinium/DOTA functionalized poly(ethylene glycol)--poly(acrylamide--acrylonitrile) micelles with synergistically enhanced cellular uptake for cancer theranostics

• Published in: RSC advances 2016-05, Vol.6 (56), p.5534-5542
• Main Authors: Tong, Guoquan, Fang, Zhuangnian, Huang, Gang, Jing, Yihan, Dai, Shulin, Jiang, Qing, Zhang, Chao, Feng, Shi-Ting, Li, Zi-Ping
• Format: Article
• ISSN: 2046-2069
• DOI: 10.1039/c6ra04038a

The combination of diagnostic and therapeutic functions into a nano-carrier could achieve a delivery system with both accurate diagnosis and delivery capabilities. Herein, a functionalized polymer of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-poly(ethyleneglycol)- block -poly(acrylamide- co -acrylonitrile) (DOTA-PEG- b -poly(AAm- co -AN)) was designed and synthesized. Doxorubicin (DOX) and gadolinium ions (Gd 3+ ) were loaded into the hydrophobic core and chelated on the shell of the micelles during the self-assembling process to endow the prepared micelles with drug delivery and magnetic resonance imaging functionalities. Such theranostics micelles exhibited noticeable accelerated DOX release with elevated temperature and high proton relaxivity r 1 (25.88 mM −1 s −1 ). Moreover, the Gd 3+ /DOX loaded micelle presented a synergistically enhanced cellular uptake efficiency (2.12 times that of free DOX) as compared with free drug or that loaded in micelles without Gd 3+ . The micelles provide promising application for chemotherapy and simultaneous enhanced magnetic resonance imaging (MRI) of cancer. The combination of diagnostic and therapeutic functions into a nano-carrier could achieve a delivery system with both accurate diagnosis and delivery capabilities.