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The siRNAsome: A Cation‐Free and Versatile Nanostructure for siRNA and Drug Co‐delivery
Author(s) -
Zheng Meng,
Jiang Tong,
Yang Wen,
Zou Yan,
Wu Haigang,
Liu Xiuhua,
Zhu Fengping,
Qian Rongjun,
Ling Daishun,
McDonald Kerrie,
Shi Jinjun,
Shi Bingyang
Publication year - 2019
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201814289
Subject(s) - small interfering rna , chemistry , drug delivery , cytotoxicity , transfection , drug , drug carrier , nanostructure , doxorubicin hydrochloride , nanotechnology , intracellular , nanoparticle , targeted drug delivery , biophysics , combinatorial chemistry , doxorubicin , in vitro , pharmacology , materials science , biochemistry , organic chemistry , biology , chemotherapy , genetics , gene
Nanoparticles show great potential for drug delivery. However, suitable nanostructures capable of loading a range of drugs together with the co‐delivery of siRNAs, which avoid the problem of cation‐associated cytotoxicity, are lacking. Herein, we report an small interfering RNA (siRNA)‐based vesicle (siRNAsome), which consists of a hydrophilic siRNA shell, a thermal‐ and intracellular‐reduction‐sensitive hydrophobic median layer, and an empty aqueous interior that meets this need. The siRNAsome can serve as a versatile nanostructure to load drug agents with divergent chemical properties, therapeutic proteins as well as co‐delivering immobilized siRNAs without transfection agents. Importantly, the inherent thermal/reduction‐responsiveness enables controlled drug loading and release. When siRNAsomes are loaded with the hydrophilic drug doxorubicin hydrochloride and anti‐P‐glycoprotein siRNA, synergistic therapeutic activity is achieved in multidrug resistant cancer cells and a tumor model.