Department of Pharmacy, Hospital 309 of PLA, Beijing, 100091, China.
Department of oncology, Xinqiao Hospital, Third Military Medical University, Chongqing, 400038, China.
Sci Rep. 2017 Jun 13;7(1):3383. doi: 10.1038/s41598-017-03111-2.
A new acidly sensitive PEGylated polyethylenimine linked by Schiff base (PEG-s-PEI) was designed to render pH-sensitive PEGylation nanoassemblies through multiple interactions with indomethacin and docetaxel (DTX). DTX nanoassemblies driven by PEG-s-PEI thus formulated exhibited an excellent pH-sensitivity PEGylation cleavage performance at extracellular pH of tumor microenvironment, compared to normal tissues, thereby long circulated in blood but were highly phagocytosed by tumor cells. Consequently, this smart pH-sensitive PEGylation cleavage provided an efficient strategy to target tumor microenvironment, in turn afforded superior therapeutic outcome in anti-tumor activity.
设计了一种新型的通过席夫碱（Schiff base）连接的酸敏感聚乙二醇化聚亚乙基亚胺（PEG-s-PEI），以通过与吲哚美辛和多西他赛（DTX）的多种相互作用来实现 pH 敏感的聚乙二醇化纳米组装体。与正常组织相比，由 PEG-s-PEI 驱动的 DTX 纳米组装体在肿瘤微环境的细胞外 pH 下表现出优异的 pH 敏感聚乙二醇化切割性能，因此在血液中循环时间长，但被肿瘤细胞高度吞噬。因此，这种智能 pH 敏感聚乙二醇化切割为靶向肿瘤微环境提供了一种有效的策略，从而在抗肿瘤活性中获得了更好的治疗效果。
