Dynamic, ultra-pH-sensitive graft copolymer micelles mediated rapid, complete destruction of 3-D tumor spheroids in vitro

Publication date: 24 February 2017
Source:Polymer, Volume 111
Author(s): Guoqing Yan, Qian Zha, Jun Wang, Xin Wang, Xu Cheng, Weijing Yao, Rupei Tang
PEGylated poly(ortho ester amides) copolymer micelles (POEAd-g-MPEG micelles) with ultra-pH-sensitivity, which exhibited a dynamic change in size under mildly acidic conditions, were constructed by facile method, therefore achieving: (i) remaining stealthy and long-circulating in the blood; (ii) small NPs once in the tumor extracellular space for enhancing penetration; (iii) bigger NPs after penetration into the core of tumor for improving retention; (iv) rapid and complete dissolution to release drug at intracellular pH for improving toxicity to tumor cells upon being internalized by tumor cells. The enhanced tumor penetration and inhibition are closely related to these dynamic characteristics, resulting in unprecedentedly rapid, complete destruction of 3-D tumor spheroids in vitro.

Graphical abstract

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