Baumgartner Ryan, Kuai Diane, Cheng Jianjun
Department of Chemistry, University of Illinois at Urbana-Champaign, Urbana, Illinois 61801, USA.
Biomater Sci. 2017 Aug 22;5(9):1836-1844. doi: 10.1039/c7bm00339k.
We report the synthesis and characterization of high-molecular weight poly(l-glutamic acid) based brush polymers. Utilizing a combination of ring-opening metathesis polymerization of norbornene based monomers and ring-opening polymerization of γ-benzyl-l-glutamate N-carboxyanhydride, high-molecular weight γ-benzyl protected poly(l-glutamic acid) brush polymers are synthesized. Controlled and complete deprotection of the benzyl groups using trimethylsilyl iodide resulted in poly(l-glutamic acid) based brush polymers with molecular weights up to 3.6 MDa, which may potentially be used to prepare size-controlled unimolecular polymeric nanomedicine for drug delivery applications. Camptothecin brush poly(l-glutamic acid) conjugates were prepared and their stability, drug release kinetics, and in vitro toxicity were studied.
我们报道了基于高分子量聚(L-谷氨酸)的刷状聚合物的合成与表征。利用降冰片烯基单体的开环易位聚合反应和γ-苄基-L-谷氨酸N-羧基酐的开环聚合反应相结合的方法,合成了高分子量的γ-苄基保护的聚(L-谷氨酸)刷状聚合物。使用碘化三甲基硅烷对苄基进行可控且完全的脱保护,得到了分子量高达3.6 MDa的基于聚(L-谷氨酸)的刷状聚合物,这些聚合物有可能用于制备尺寸可控的单分子聚合物纳米药物用于药物递送应用。制备了喜树碱刷状聚(L-谷氨酸)缀合物,并研究了它们的稳定性、药物释放动力学和体外毒性。