Triblock copolymer of poly(ethylene glycol)-b-poly(2-dimethylaminoethyl methacrylate)-b-poly(pyrenylmethyl methacrylate) (PEG-b-PDMAEMA-b-PPy) has been developed for use as an ideal gene delivery system, which showed both high stability under physiological conditions and efficient gene release in a mimetic cancer environment. The siRNA release from this system without external stimulation was 16% in 1 h and then remained steady. However, the photo-triggered siRNA release was 78% within 1 h and was higher than 91% after 24 h. The remarkable contrast between the stability and release efficiency of these siRNA-condensed micelleplexes before and after photo-irradiation has been rationalized by the light- and pH-induced structural transitions of the triblock copolymer micelles. The negligible cytotoxicity, high cellular uptake efficiency, and remarkable knockdown efficiency shown in in vitro tests further revealed the promising potential of these triblock copolymer micelleplexes for use in stimuli-responsive gene therapy.

中文翻译：

---

通过光和 pH 双重响应共聚物实现时空精度的高效基因释放†


聚(乙二醇) -b-聚(2-二甲氨基乙基甲基丙烯酸酯) -b-聚(芘基甲基丙烯酸甲酯)(PEG- b- PDMAEMA -b -PPy)三嵌段共聚物已被开发用作理想的基因递送系统，其在生理条件下表现出高稳定性，在模拟癌症环境中表现出有效的基因释放。在没有外部刺激的情况下，该系统的 siRNA 释放量在 1 小时内为 16%，然后保持稳定。然而，光触发的siRNA释放在1小时内为78%，24小时后高于91%。这些 siRNA 缩合胶束复合物在光照射前后的稳定性和释放效率之间的显着差异已通过光和 pH 诱导的三嵌段共聚物胶束的结构转变合理化。体外测试中显示的可忽略的细胞毒性、高细胞摄取效率和显着的敲低效率进一步揭示了这些三嵌段共聚物胶束复合物在刺激响应基因治疗中的应用前景。