作者：Siqin Chen, Yin Zhong, Wufa Fan, Jiajia Xiang, Guowei Wang, Quan Zhou, Jinqiang Wang, Yu Geng, 等
关键字：非EPR依赖的主动渗透
论文来源：期刊
具体来源：Nature Biomedical Engineering
发表时间：2021年

Effective anticancer nanomedicines need to exhibit prolonged circulation in blood, to extravasate and accumulate in tumours, and to be taken up by tumour cells. These contrasting criteria for persistent circulation and cell-membrane affinity have often led to complex nanoparticle designs with hampered clinical translatability. Here, we show that conjugates of small-molecule anticancer drugs with the polyzwitterion poly (2-(N-oxide-N, N-diethylamino) ethyl methacrylate) have long blood-circulation half-lives and bind reversibly to cell membranes, owing to the negligible interaction of the polyzwitterion with proteins and its weak interaction with phospholipids. Adsorption of the polyzwitterion–drug conjugates to tumour endothelial cells and then to cancer cells favoured their transcytosis-mediated extravasation into tumour interstitium and infiltration into tumours, and led to the eradication of large tumours and PDX tumors.

https://www.nature.com/articles/s41551-021-00701-4