Polyethylenimine-based formulations for delivery of oligonucleotides

Fei Hao, Yuhuan Li, Jing Zhu, Jingyao Sun, Brian Marshall, Robert J. Lee, Lesheng Teng, Zhaogang Yang, Jing Xie

Research output: Contribution to journalArticlepeer-review

36 Scopus citations


Polyethyleneimine (PEI) is well-known as a non-viral gene delivery vector, especially for oligonucleotide delivery. However, its clinical applications are significantly limited due to its high cationic charge, lack of specificity, and interaction with the proteins and nontarget cells in the biological fluids, resulting in high cytotoxicity, poor stability and low transfection efficiency for oligonucleotides transporting. It has been shown that the molecular weight (MW) of PEI, degree of branching, N/P ratio, buffer capacity, oligonucleotide structure, culture medium pH, serum, presence or absence of and method of preparation make a significant difference in the cytoxicity, stability, and transfection efficiency for the PEI-based oligonucleotides delivery systems. Ligands, hydrophobic, hydrophilic, and amphiphilic modification of PEI have been investigated to reduce the cytoxicity and improve the stability, the transfection efficiency, and therapeutic effect. Moreover, various intelligent modifications of PEI, such as pH-responsive (hydrazone bond) and redox sensitive linkers (disulfide bond) can control oligonucleotides release and have attracted much attention. In general, more efficient oligonucleotide delivery can be achieved by the introduction of modifications to PEI and by optimization of parameters of PEI or PEI-based formulations.

Original languageEnglish (US)
Pages (from-to)2264-2284
Number of pages21
JournalCurrent Medicinal Chemistry
Issue number13
StatePublished - 2019


  • Drug
  • Oligonucleotide delivery
  • Oligonucleotide delivery carrier
  • PEG modification
  • PH-sensitive linker
  • Polyethylenimine
  • Targeting

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Organic Chemistry


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