Redox-sensitive dendrimersomes assembled from amphiphilic Janus dendrimers for siRNA delivery†,Biomaterials Science

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Redox-sensitive dendrimersomes assembled from amphiphilic Janus dendrimers for siRNA delivery†
Biomaterials Science ( IF 5.8 ) Pub Date : 2018-06-05 00:00:00 , DOI: 10.1039/c8bm00491a
Xiao-Jiao Du _{1,

2,

3,

4} , Ze-Yu Wang _{4,

5,

6,

7} , Yu-Cai Wang _{1,

2,

3,

4}

Affiliation

The development of delivery systems for small interfering RNA (siRNA) plays a key role in its clinical application. As the major delivery systems for siRNA, cationic polymer- or lipid-based vehicles are plagued by inherent issues. As proof of concept, a disulfide bond-containing amphiphilic Janus dendrimer (ssJD), which could be conveniently synthesized and readily scaled up with high reproducibility, was explored as a siRNA delivery system to circumvent these issues. The cationic hydrophilic head of this Janus dendrimer ensured strong and stable binding with negatively charged siRNA via electrostatic interactions, and the loaded siRNA was rapidly released from the obtained complexes under a redox environment. Therefore, after efficient internalization into tumor cells, redox-sensitive dendrimersome (RSDs)/siRNA exhibited significantly improved gene silencing efficacy.

中文翻译：

由两亲性Janus树状聚合物组装而成的氧化还原敏感树状体，用于siRNA递送†

小干扰RNA（siRNA）递送系统的开发在其临床应用中起着关键作用。作为siRNA的主要递送系统，基于阳离子聚合物或脂质的载体受到固有问题的困扰。作为概念的证明，探索了可以方便地合成且易于放大且具有高重现性的含二硫键的两亲性Janus树状大分子（ssJD），作为解决这些问题的siRNA传递系统。该Janus树状大分子的阳离子亲水头确保通过负电荷的siRNA通过以下方式牢固而稳定地结合在氧化还原环境下，静电相互作用和负载的siRNA迅速从获得的复合物中释放出来。因此，在有效内化到肿瘤细胞后，氧化还原敏感的树状大分子（RSDs）/ siRNA表现出显着改善的基因沉默功效。

更新日期：2018-06-05

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