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Green Tea Catechin Dramatically Promotes RNAi Mediated by Low-Molecular-Weight Polymers
ACS Central Science ( IF 18.2 ) Pub Date : 2018-09-19 00:00:00 , DOI: 10.1021/acscentsci.8b00363
Wanwan Shen 1 , Qingwei Wang 1 , Yang Shen 1 , Xiao Gao 1 , Lei Li 1 , Yang Yan 1 , Hui Wang 2 , Yiyun Cheng 1, 2
Affiliation  

Cytosolic delivery is the major challenge that limits the clinical translation of siRNA-based therapeutics. Although thousands of polymers have been developed for siRNA delivery, the efficiency–toxicity correlation is unsatisfactory. Here, we report a facile strategy to fabricate core–shell-structured nanoparticles with robust siRNA delivery efficiency. The nanoparticle is prepared by entropy-driven complexation of siRNA with a green tea catechin to yield a negatively charged core, followed by coating low-molecular-weight polymers to form the shell. This supramolecular strategy facilitates the polymers condensing siRNA into uniform nanoparticles. The nanoparticle specifically down-regulates target genes in vitro and in vivo, and efficiently attenuates chronic intestinal inflammation in an inflammatory bowel disease model. Notably, the highly efficient nanoparticles are applicable for various polymers with different topologies and chemical compositions, providing a versatile technique to break down the efficiency–toxicity correlation of cationic polymers. The proposed strategy in this study permits the development of a promising platform for polymer-mediated siRNA delivery.

中文翻译:

绿茶儿茶素显着促进低分子量聚合物介导的RNAi

胞质递送是限制基于siRNA的疗法的临床翻译的主要挑战。尽管已开发出数千种用于siRNA递送的聚合物,但其效率与毒性之间的关系并不令人满意。在这里,我们报告了一种简便的策略来制造具有强大siRNA传递效率的核-壳结构纳米颗粒。通过将siRNA与绿茶儿茶素进行熵驱动的络合以产生带负电荷的核,然后包覆低分子量聚合物以形成壳,来制备纳米粒子。这种超分子策略有助于聚合物将siRNA浓缩成均匀的纳米颗粒。所述纳米颗粒特异性下调靶基因在体外体内,并有效减轻炎症性肠病模型中的慢性肠道炎症。值得注意的是,高效纳米粒子适用于具有不同拓扑和化学组成的各种聚合物,提供了一种打破阳离子聚合物效率与毒性相关性的通用技术。这项研究中提出的策略允许开发一个有前途的平台,用于聚合物介导的siRNA传递。
更新日期:2018-09-19
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