Shen Yu
siRNA Therapeutics, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60031, USA.
IDrugs. 2008 Aug;11(8):572-8.
Short interfering (si)RNA represents a promising novel therapeutic modality for the treatment of cancer. However, delivering siRNA to tumors via clinically relevant means is a major technical hurdle that has impeded the successful development of siRNA-based cancer therapeutics. Significant progress has been made in recent years for the delivery of siRNA to tumors, and several promising siRNA delivery platforms have begun to emerge. These platforms include liposomes, in which siRNA is encapsulated in a lipid vesicle; polyplexes, in which a cationic carrier is used to bind siRNA to form siRNA-containing nanoparticles; liposome-polycation-DNA (LPD) complexes, in which an siRNA-containing polyplex is encapsulated in a lipid vesicle; and siRNA conjugates, in which siRNA is coupled to a targeting moiety that carries the siRNA into target cells via receptor-mediated endocytosis. An unbiased, independent evaluation of various tumor-delivery approaches will be a critical starting point in identifying the most promising delivery platforms for the development of siRNA-based cancer therapeutics.
短干扰（si）RNA是一种很有前景的新型癌症治疗方式。然而，通过临床相关手段将siRNA递送至肿瘤是一个重大技术障碍，阻碍了基于siRNA的癌症治疗药物的成功研发。近年来，在将siRNA递送至肿瘤方面取得了显著进展，一些有前景的siRNA递送平台已开始出现。这些平台包括脂质体，其中siRNA被包裹在脂质囊泡中；多聚体，其中使用阳离子载体结合siRNA以形成含siRNA的纳米颗粒；脂质体-聚阳离子-DNA（LPD）复合物，其中含siRNA的多聚体被包裹在脂质囊泡中；以及siRNA缀合物，其中siRNA与靶向部分偶联，该靶向部分通过受体介导的内吞作用将siRNA携带到靶细胞中。对各种肿瘤递送方法进行无偏倚、独立的评估，将是确定基于siRNA的癌症治疗药物研发中最有前景的递送平台的关键起点。
