There is a continuing quest to rationally fabricate polymeric biomaterials with both high transfection efficiency and minimal toxicity for the emerging opportunities in small interfering RNA (siRNA) delivery. Recently, this goal was promoted highly by developing a robust and efficient strategy to facilitate polymer-mediated RNAi using natural polyphenols with multiple phenol groups that could condense siRNA effectively into negatively charged nanoparticles (NPs). Further coating of these NPs with cationic polymers of low molecular weight enabled their intracellular siRNA delivery. Inspired by the structural and functional features of natural polyphenols, we aimed to further the development of low molecular weight polycatechols as a new class of efficient and biocompatible polymers for siRNA delivery in our current study. The fabricated polycatechols have benefits of requiring only one-step fabrication toward efficient siRNA nanoformulations. Moreover, they could deliver siRNA into cells and silence target genes both in vitro and in vivo. The resulting polycatechol/siRNA formulations were also functionally competent, demonstrating a successful, profound downregulation of a proinflammatory enzyme to attenuate chronic intestinal inflammation in an intestinal injury model. This study provides a new approach in chemistry for the development of efficient synthetic polymers for therapeutic siRNA delivery.

对于小干扰RNA（siRNA）输送中出现的新机会，人们一直在寻求合理地制造具有高转染效率和最小毒性的聚合物生物材料。最近，通过开发一种稳健而有效的策略来促进这一目标的实现，该策略使用具有多个酚基团的天然多酚促进聚合物介导的RNAi，可以将siRNA有效地冷凝成带负电荷的纳米粒子（NP）。用低分子量的阳离子聚合物进一步覆盖这些NP，可以实现其细胞内siRNA递送。受到天然多酚的结构和功能特性的启发，我们的目标是进一步发展低分子量聚儿茶酚，这是我们目前研究中作为一类新型的高效且生物相容的siRNA递送聚合物。所制备的聚儿茶酚具有仅需一步制备即可实现高效siRNA纳米制剂的优势。而且，它们可以在体内外将siRNA传递到细胞中并沉默靶基因。所得的聚儿茶酚/ siRNA制剂在功能上也具有竞争力，证明了在肠道损伤模型中成功，深刻地下调了促炎酶，以减轻慢性肠道炎症。这项研究为开发用于治疗性siRNA递送的高效合成聚合物提供了一种新的化学方法。所得的聚儿茶酚/ siRNA制剂在功能上也具有竞争力，证明了在肠道损伤模型中成功，深刻地下调了促炎酶以减轻慢性肠道炎症。这项研究为开发用于治疗性siRNA递送的高效合成聚合物提供了一种新的化学方法。所得的聚儿茶酚/ siRNA制剂在功能上也具有竞争力，证明了在肠道损伤模型中成功，深刻地下调了促炎酶以减轻慢性肠道炎症。这项研究为开发用于治疗性siRNA递送的高效合成聚合物提供了一种新的化学方法。