Thermoresponsive pegylated bubble liposome nanovectors for efficient siRNA delivery via endosomal escape

NANOMEDICINE(2017)

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摘要
Aim: Improving the delivery of siRNA into cancer cells via bubble liposomes. Designing a thermoresponsive pegylated liposome through the introduction of ammonium bicarbonate salt into liposomes so as to control their endosomal escape for gene therapy. Methods: A sub-200 nm nanovector was fully characterized and examined for cellular uptake, cytotoxicity, endosomal escape and gene silencing. Results: The siRNA-liposomes were internalized into cancer cells within 5 min and then released siRNAs in the cytosol prior to lysosomal degradation upon external temperature elevation. This was confirmed by confocal bioimaging and gene silencing reaching up to 90% and further demonstrated by the protein inhibition of both target genes. Conclusion: The thermoresponsiveness of ammonium bicarbonate containing liposomes enabled the rapid endosomal escape of the particles and resulted in an efficient gene silencing.
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关键词
bubble generation,endosomal escape,gene silencing,lipoplex,liposome,multidrug-resistant cell,nanomedicine,siRNA delivery
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