siRNA nanoparticles: the future of RNAi therapeutics for oncology?

With the emergence of siRNA-based nanomedicine as a powerful therapeutic strategy for cancers, seven of these therapeutics have now advanced to clinical trials. Carriers of siRNA therapeutics include transferrin-modified cyclodextrin (CALAA-01, Arrowhead Research Corporation, CA, USA), in vivo jetPEI® (SNS01-T; Sevion Technologies, NJ, USA), cationic liposomes (ALN-VSP02, Alnylam Pharmaceuticals, MA, USA; TKM080301, Tekmira Pharmaceuticals, Burnaby, Canada; Atu027, Silence Therapeutics, London, UK; and DCR-MYC, Dicerna Pharmaceuticals, Watertown, MA, USA) and neutral liposomes (siRNA–EphA2–1,2-dioleoyl-sn-glycero-3-phosphocholine [DOPC], MD Anderson Cancer Center, TX, USA ). Among those in clinical trials, the cationic lipoplex targeting MYC1a (DCR-MYC) is the only nanoplex that requires the Dicer enzyme in order to obtain functional siRNA.

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