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Combining Fluorination and Bioreducibility for Improved siRNA Polyplex Delivery.

Gang Chen1, Kaikai Wang1, Qi Hu1

  • 1State Key Laboratory of Natural Medicines, Department of Pharmaceutics, China Pharmaceutical University , Nanjing, 210009, China.

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Summary

Combining fluorination and bioreducibility in polycations significantly reduces toxicity and enhances siRNA delivery. Fluorinated bioreducible polycations (F-RHB) show superior in vivo gene silencing efficacy compared to non-fluorinated or non-bioreducible counterparts.

Keywords:
cancerfluorinated polymerspolyplexesreducible polymerssiRNA delivery

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Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Drug Delivery

Background:

  • Polycations are essential for small interfering RNA (siRNA) therapeutics delivery.
  • However, their clinical application is limited by inherent toxicity and poor in vivo efficacy.
  • Novel strategies are needed to improve polycationic vectors for siRNA delivery.

Purpose of the Study:

  • To investigate the combined effects of fluorination and bioreducibility on polycationic vectors for siRNA delivery.
  • To synthesize and characterize fluorinated bioreducible polycations (F-RHB) and compare them with non-fluorinated bioreducible (RHB) and non-bioreducible (NHB) counterparts.
  • To evaluate the toxicity, cellular uptake, endosomal escape, and in vivo gene silencing efficacy of these novel polycations.

Main Methods:

  • Synthesis of bioreducible (RHB) and nonreducible (NHB) poly(amido amine)s.
  • Fluorination of RHB using heptafluorobutyric anhydride to yield F-RHB.
  • Formation of polyplexes with siRNA and assessment of cytotoxicity.
  • In vitro evaluation of siRNA delivery, cellular uptake, and endosomal escape in multiple cell lines.
  • In vivo assessment of luciferase (Luc) gene silencing efficacy in tumor models.

Main Results:

  • RHB and F-RHB exhibited significantly reduced cytotoxicity compared to NHB, enabling safer, higher-dose administration.
  • All synthesized polycations successfully formed polyplexes with siRNA.
  • F-RHB demonstrated superior siRNA silencing efficacy in vitro, attributed to enhanced cellular uptake and endosomal escape.
  • In vivo studies showed significantly improved Luc silencing in tumors with F-RHB polyplexes compared to RHB, NHB, and poly(ethylenimine) (PEI) controls.

Conclusions:

  • Combining fluorination and bioreducibility in polycations is a viable strategy to mitigate toxicity and enhance siRNA delivery.
  • F-RHB represents a promising next-generation vector for siRNA therapeutics with improved safety and efficacy profiles.
  • This approach offers a pathway for designing advanced polycationic vectors for effective in vivo gene therapy applications.