Using drug-excipient interactions for siRNA delivery

被引:39
作者
Bruno, Katharina [1 ]
机构
[1] Novartis Pharma AG, TRD, Pharmaceut & Analyt Dev PHAD, CH-4057 Basel, Switzerland
关键词
Small interfering RNA; siRNA; RNAi; Formulation; Delivery; Clinic; SMALL INTERFERING RNA; IN-VIVO DELIVERY; ENDOTHELIAL GROWTH-FACTOR; INHIBITS TUMOR-GROWTH; DOUBLE-STRANDED-RNA; EFFICIENT DELIVERY; TARGETED DELIVERY; GENE-EXPRESSION; CELLULAR UPTAKE; INTRACELLULAR DELIVERY;
D O I
10.1016/j.addr.2011.09.003
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
SiRNA is the trigger of RNA interference, a mechanism discovered in the late 1990s. To release the therapeutic potential of this versatile but large and fragile molecule, excipients are used which either interact by electrostatic interaction, passively encapsulate siRNA or are covalently attached to enable specific and safe delivery of the drug substance. Controlling the delicate balance between protective complexation and release of siRNA at the right point and time is done by understanding excipients-siRNA interactions. These can be lipids, polymers such as PEI, PLGA, Chitosans, Cyclodextrins, as well as aptamers and peptides. This review describes the mechanisms of interaction of the most commonly used siRNA delivery vehicles, and looks at the results of their clinical and preclinical studies. (C) 2011 Elsevier B.V. All rights reserved.
引用
收藏
页码:1210 / 1226
页数:17
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