Current Aspects of siRNA Bioconjugate for In Vitro and In Vivo Delivery

Studies on siRNA delivery have seen intense growth in the past decades since siRNA has emerged as a new class of gene therapeutics for the treatment of various diseases. siRNA bioconjugate, as one of the major delivery strategies, offers the potential to enhance and broaden pharmacological propertie...

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Main Author: Wanyi Tai
Format: Article
Language:English
Published: MDPI AG 2019-06-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/24/12/2211
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author Wanyi Tai
author_facet Wanyi Tai
author_sort Wanyi Tai
collection DOAJ
description Studies on siRNA delivery have seen intense growth in the past decades since siRNA has emerged as a new class of gene therapeutics for the treatment of various diseases. siRNA bioconjugate, as one of the major delivery strategies, offers the potential to enhance and broaden pharmacological properties of siRNA, while minimizing the heterogeneity and stability-correlated toxicology. This review summarizes the recent developments of siRNA bioconjugate, including the conjugation with antibody, peptide, aptamer, small chemical, lipidoid, cell-penetrating peptide polymer, and nanoparticle. These siRNA bioconjugate, either administrated alone or formulated with other agents, could significantly improve pharmacokinetic behavior, enhance the biological half-life, and increase the targetability while maintaining sufficient gene silencing activity, with a concomitant improvement of the therapeutic outcomes and diminishment of adverse effects. This review emphasizes the delivery application of these siRNA bioconjugates, especially the conjugation strategy that control the integrity, stability and release of siRNA bioconjugates. The limitations conferred by these conjugation strategies have also been covered.
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spelling doaj.art-1ca5529e2250425a9af82227631f09202022-12-22T02:19:17ZengMDPI AGMolecules1420-30492019-06-012412221110.3390/molecules24122211molecules24122211Current Aspects of siRNA Bioconjugate for In Vitro and In Vivo DeliveryWanyi Tai0Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Wuhan University), Ministry of Education, School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, Hubei, ChinaStudies on siRNA delivery have seen intense growth in the past decades since siRNA has emerged as a new class of gene therapeutics for the treatment of various diseases. siRNA bioconjugate, as one of the major delivery strategies, offers the potential to enhance and broaden pharmacological properties of siRNA, while minimizing the heterogeneity and stability-correlated toxicology. This review summarizes the recent developments of siRNA bioconjugate, including the conjugation with antibody, peptide, aptamer, small chemical, lipidoid, cell-penetrating peptide polymer, and nanoparticle. These siRNA bioconjugate, either administrated alone or formulated with other agents, could significantly improve pharmacokinetic behavior, enhance the biological half-life, and increase the targetability while maintaining sufficient gene silencing activity, with a concomitant improvement of the therapeutic outcomes and diminishment of adverse effects. This review emphasizes the delivery application of these siRNA bioconjugates, especially the conjugation strategy that control the integrity, stability and release of siRNA bioconjugates. The limitations conferred by these conjugation strategies have also been covered.https://www.mdpi.com/1420-3049/24/12/2211siRNA bioconjugatesiRNA scaffoldasymmetric siRNAlipid siRNA conjugatespherical siRNA
spellingShingle Wanyi Tai
Current Aspects of siRNA Bioconjugate for In Vitro and In Vivo Delivery
Molecules
siRNA bioconjugate
siRNA scaffold
asymmetric siRNA
lipid siRNA conjugate
spherical siRNA
title Current Aspects of siRNA Bioconjugate for In Vitro and In Vivo Delivery
title_full Current Aspects of siRNA Bioconjugate for In Vitro and In Vivo Delivery
title_fullStr Current Aspects of siRNA Bioconjugate for In Vitro and In Vivo Delivery
title_full_unstemmed Current Aspects of siRNA Bioconjugate for In Vitro and In Vivo Delivery
title_short Current Aspects of siRNA Bioconjugate for In Vitro and In Vivo Delivery
title_sort current aspects of sirna bioconjugate for in vitro and in vivo delivery
topic siRNA bioconjugate
siRNA scaffold
asymmetric siRNA
lipid siRNA conjugate
spherical siRNA
url https://www.mdpi.com/1420-3049/24/12/2211
work_keys_str_mv AT wanyitai currentaspectsofsirnabioconjugateforinvitroandinvivodelivery