Development of fluorinated polyplex nanoemulsions for improved small interfering RNA delivery and cancer therapy

Gang Chen, Kaikai Wang, Pengkai Wu, Yixin Wang, Zhanwei Zhou, Lifang Yin, Minjie Sun, David Oupický

Research output: Contribution to journalArticle

10 Scopus citations

Abstract

We report the development of a small interfering RNA (siRNA) delivery vector based on cationic perfluorocarbon nanoemulsions. We have prepared perfluorodecalin (PFD) emulsions with a positive surface charge provided by a fluorinated poly(ethylenimine) (F-PEI). The fluorinated emulsion (F-PEI@PFD) reduced cytotoxicity of F-PEI and demonstrated effective binding with siRNAs to form nanosized emulsion polyplexes. The prepared emulsion polyplexes enhanced cellular uptake and improved endosomal escape of the siRNA. In addition to increased reporter gene silencing in multiple cancer cell lines, when compared with control F-PEI and PEI polyplexes, the siRNA emulsion polyplexes showed an excellent resistance to serum deactivation and maintained high activity, even in high-serum conditions. The F-PEI@PFD emulsion polyplexes carrying an siRNA to silence the expression of Bcl2 gene induced apoptosis and inhibited tumor growth in a melanoma mouse model in vivo and showed potential for in vivo ultrasound imaging. This study demonstrates the potential of F-PEI@PFD emulsions as a multifunctional theranostic nanoplatform for safe siRNA delivery, with integrated ultrasound imaging functionality.

Original languageEnglish (US)
Pages (from-to)3746-3761
Number of pages16
JournalNano Research
Volume11
Issue number7
DOIs
StatePublished - Jul 1 2018

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Keywords

  • fluorous interactions
  • perfluorocarbon emulsion
  • polyplexes
  • small interfering RNA (siRNA) delivery
  • tumor delivery

ASJC Scopus subject areas

  • Materials Science(all)
  • Electrical and Electronic Engineering

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