Small-interfering RNA (siRNA) is both a powerful tool in research and a promising therapeutic platform to modulate expression of disease-related genes. Malignant tumors are attractive disease targets for nucleic acid-based therapies. siRNA directed against oncogenes, and genes driving metastases or angiogenesis have been evaluated in animal models and in some cases, in humans. The outcomes of these studies indicate that drug delivery is a significant limiting factor. This review provides perspectives on in vivo validated nanoparticle-based siRNA delivery systems. Results of recent advances in liposomes and polymeric and inorganic formulations illustrate the need for mutually optimized attributes for performance in systemic circulation, tumor interstitial space, plasma membrane, and endosomes. Physiochemical properties conducive to efficient siRNA delivery are summarized and directions for future research are discussed.

中文翻译：

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最近体内基于颗粒的小干扰 RNA (siRNA) 递送至实体瘤的证据。


小干扰 RNA (siRNA) 既是强大的研究工具，也是调节疾病相关基因表达的有前景的治疗平台。恶性肿瘤是基于核酸的疗法的有吸引力的疾病靶标。针对癌基因以及驱动转移或血管生成的基因的 siRNA 已在动物模型中以及在某些情况下在人类中进行了评估。这些研究的结果表明药物输送是一个重要的限制因素。本综述提供了体内验证的基于纳米粒子的 siRNA 递送系统的观点。脂质体以及聚合物和无机制剂的最新进展表明，为了实现体循环、肿瘤间隙、质膜和内体的性能，需要相互优化的属性。总结了有利于高效 siRNA 递送的理化特性，并讨论了未来研究的方向。