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Molecules 2017, 22(10), 1724; doi:10.3390/molecules22101724

Enhancing the Therapeutic Delivery of Oligonucleotides by Chemical Modification and Nanoparticle Encapsulation

1
School of Life Sciences, Jilin University, Changchun 130012, China
2
College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
3
Tavistock Life Sciences, San Diego, CA 92130, USA
*
Authors to whom correspondence should be addressed.
Received: 20 August 2017 / Revised: 22 September 2017 / Accepted: 9 October 2017 / Published: 13 October 2017
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Abstract

Oligonucleotide (ON) drugs, including small interfering RNA (siRNA), microRNA (miRNA) and antisense oligonucleotides, are promising therapeutic agents. However, their low membrane permeability and sensitivity to nucleases present challenges to in vivo delivery. Chemical modifications of the ON offer a potential solution to improve the stability and efficacy of ON drugs. Combined with nanoparticle encapsulation, delivery at the site of action and gene silencing activity of chemically modified ON drugs can be further enhanced. In the present review, several types of ON drugs, selection of chemical modification, and nanoparticle-based delivery systems to deliver these ON drugs are discussed. View Full-Text
Keywords: oligonucleotide; siRNA; miRNA; antisense; nanocarriers oligonucleotide; siRNA; miRNA; antisense; nanocarriers
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Sun, Y.; Zhao, Y.; Zhao, X.; Lee, R.J.; Teng, L.; Zhou, C. Enhancing the Therapeutic Delivery of Oligonucleotides by Chemical Modification and Nanoparticle Encapsulation. Molecules 2017, 22, 1724.

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