Green Tea Catechin Dramatically Promotes RNAi Mediated
by Low-Molecular-Weight Polymers
Version 2 2018-10-24, 04:22
Version 1 2018-09-19, 12:09
Posted on 2018-10-24 - 04:22
Cytosolic delivery
is the major challenge that limits the clinical
translation of siRNA-based therapeutics. Although thousands of polymers
have been developed for siRNA delivery, the efficiency–toxicity
correlation is unsatisfactory. Here, we report a facile strategy to
fabricate core–shell-structured nanoparticles with robust siRNA
delivery efficiency. The nanoparticle is prepared by entropy-driven
complexation of siRNA with a green tea catechin to yield a negatively
charged core, followed by coating low-molecular-weight polymers to
form the shell. This supramolecular strategy facilitates the polymers
condensing siRNA into uniform nanoparticles. The nanoparticle specifically
down-regulates target genes in vitro and in vivo, and efficiently attenuates chronic intestinal inflammation
in an inflammatory bowel disease model. Notably, the highly efficient
nanoparticles are applicable for various polymers with different topologies
and chemical compositions, providing a versatile technique to break
down the efficiency–toxicity correlation of cationic polymers.
The proposed strategy in this study permits the development of a promising
platform for polymer-mediated siRNA delivery.
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Shen, Wanwan; Wang, Qingwei; Shen, Yang; Gao, Xiao; Li, Lei; Yan, Yang; et al. (2018). Green Tea Catechin Dramatically Promotes RNAi Mediated
by Low-Molecular-Weight Polymers. ACS Publications. Collection. https://doi.org/10.1021/acscentsci.8b00363
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AUTHORS (8)
WS
Wanwan Shen
QW
Qingwei Wang
YS
Yang Shen
XG
Xiao Gao
LL
Lei Li
YY
Yang Yan
HW
Hui Wang
YC
Yiyun Cheng
KEYWORDS
coating low-molecular-weight polymerssiRNA-based therapeuticsdown-regulates target genesGreen Tea Catechin Dramatically Promotes RNAi MediatedsiRNA delivery efficiencypolymer-mediated siRNA deliverychemical compositionsentropy-driven complexationcoresiRNA deliverybowel disease modelcationic polymerstea catechinuniform nanoparticlessupramolecular strategyLow-Molecular-Weight Polymers Cytosolic deliverycorrelation