Journal
ADVANCED DRUG DELIVERY REVIEWS
Volume 104, Issue -, Pages 16-28Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.addr.2015.10.015
Keywords
siRNA; RNA interference; siRNA delivery; Chemical modification; Structural modification
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Funding
- Global Innovative Research Center (GiRC) project of National Research Foundation of Korea [2012K1A1A2A01056095]
- Intramural Research Program of KIST
- National Research Foundation of Korea [2012K1A1A2A01056095] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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Small interfering RNA (siRNA), a 21-23 nt double-stranded RNA responsible for post-transcriptional gene silencing, has attracted great interests as promising genomic drugs, due to its strong ability to silence target genes in a sequence-specific manner. Despite high silencing efficiency and on-target specificity, the clinical translation of siRNA has been hindered by its inherent features: poor intracellular delivery, limited blood stability, unpredictable immune responses and unwanted off-targeting effects. To overcome these hindrances, researchers have made various advances to modify siRNA itself and to improve its delivery. In this review paper, first we briefly discuss the innate properties and delivery barriers of siRNA. Then, we describe recent progress in (1) chemically and structurally modified siRNAs to solve their intrinsic problems and (2) siRNA delivery formulations including siRNA conjugates, polymerized siRNA, and nucleic acid-based nanoparticles to improve in vivo delivery. (C) 2015 Elsevier B.V. All rights reserved.
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