Design, Synthesis, and Biological Evaluation of a Robust, Biodegradable Dendrimer
作者:Derek G. van der Poll、Heidi M. Kieler-Ferguson、William C. Floyd、Steven J. Guillaudeu、Katherine Jerger、Francis C. Szoka、Jean M. Fréchet
DOI:10.1021/bc900553n
日期:2010.4.21
PEGylated dendrimers are attractive for biological applications due to their tunable pharmacokinetics and ability to carry multiple copies of bioactive molecules. The rapid and efficient synthesis of a robust and biodegradable PEGylated dendrimer based on a polyester−polyamide hybrid core is described. The architecture is designed to avoid destructive side reactions during dendrimer preparation while
聚乙二醇化树枝状聚合物因其可调节的药代动力学和携带多个生物活性分子拷贝的能力而对生物应用具有吸引力。描述了基于聚酯-聚酰胺杂化核的稳健且可生物降解的聚乙二醇化树枝状聚合物的快速有效合成。该架构旨在避免树枝状聚合物制备过程中的破坏性副反应,同时保持生物降解性。因此,用多柔比星 (Dox) 功能化的树枝状聚合物是从商业起始材料中通过九个高产线性步骤制备的。在 C26 鼠结肠癌的治疗中,使用等摩尔剂量并行评估树枝状聚合物和 Doxil,导致在 60 天实验结束时大多数无肿瘤小鼠的统计结果相同。