Zarabi Bahar, Nan Anjan, Zhuo Jiachen, Gullapalli Rao, Ghandehari Hamidreza
Department of Pharmaceutical Sciences, University of Maryland, Baltimore, Maryland 21201, USA.
Macromol Biosci. 2008 Aug 11;8(8):741-8. doi: 10.1002/mabi.200700290.
This study describes the synthesis, characterization, and in vitro evaluation of N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-gadolinium (Gd)-doxorubicin (Dox) conjugates. Copolymers of HPMA were derivatized to incorporate side chains for Gd chelation and Dox conjugation. The conjugates were characterized by their side chain contents, T(1) relaxivity (r(1)), stability, and in vitro cytotoxicity. High stability and relaxivity of these conjugates coupled with low toxicity show their potential for monitoring the in vivo fate of HPMA-based drug delivery systems by magnetic resonance imaging techniques.
本研究描述了N-（2-羟丙基）甲基丙烯酰胺（HPMA）共聚物-钆（Gd）-阿霉素（Dox）偶联物的合成、表征及体外评价。对HPMA共聚物进行衍生化处理，以引入用于钆螯合和阿霉素偶联的侧链。通过侧链含量、纵向弛豫率（r(1)）、稳定性和体外细胞毒性对这些偶联物进行了表征。这些偶联物具有高稳定性和弛豫率，且毒性较低，显示出它们通过磁共振成像技术监测基于HPMA的药物递送系统体内命运的潜力。
