ArticleDrug delivery and translational research2021
PEI fluorination reduces toxicity and promotes liver-targeted siRNA delivery.
Article in Drug delivery and translational research, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
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Who cites it
33 citing papers in PubMed.
- Smart Nanodelivery for Eye-Brain Disorders: Synergistic CCL2 Neutralization and MMP9 Silencing Reverse Anxiety in High Myopia.Small (Weinheim an der Bergstrasse, Germany) · 2026Article
- Advances in Polyethyleneimine-Derived Nanoformulations.Small science · 2026Review
- Tissue-specific gene delivery approaches.Bioengineering & translational medicine · 2026Review
- The application of nanoparticle-mediated siRNA delivery systems in ovarian cancer.Cancer gene therapy · 2026Review
- siRNA Nanoparticle Delivery Strategies and Clinical Trial Advances in Tumor Therapy.International journal of molecular sciences · 2026Review
- Research Progress on Polymer-Based Nanocarriers for Tumor-Targeted Delivery of Survivin siRNA.Polymers · 2025Review
- Microfluidic Optimization of PEI-Lipid Hybrid Nanoparticles for Efficient DNA Delivery and Transgene Expression.Pharmaceutics · 2025Article
- Advances in RNA-Based Therapeutics: Challenges and Innovations in RNA Delivery Systems.Current issues in molecular biology · 2024Review
- Advances in Nonviral mRNA Delivery Materials and Their Application as Vaccines for Melanoma Therapy.ACS applied bio materials · 2024Review
- Beyond Lipids: Exploring Advances in Polymeric Gene Delivery in the Lipid Nanoparticles Era.Advanced materials (Deerfield Beach, Fla.) · 2024Review
- Involvement of miR-199a-5p-loaded mesoporous silica nanoparticle-polyethyleneimine-KALA in osteogenic differentiation.Journal of dental sciences · 2024Article
- Advances in non-viral mRNA delivery to the spleen.Biomaterials science · 2024Review
- The landscape of nanoparticle-based siRNA delivery and therapeutic development.Molecular therapy : the journal of the American Society of Gene Therapy · 2024Review
- Revisiting of Properties and Modified Polyethylenimine-Based Cancer Gene Delivery Systems.Biochemical genetics · 2024Review
- Revisiting of Properties and Modified Polyethylenimine-Based Cancer Gene Delivery Systems.Biochemical genetics · 2024Review
- Fluorinated amphiphilic Poly(β-Amino ester) nanoparticle for highly efficient and specific delivery of nucleic acids to the Lung capillary endothelium.Bioactive materials · 2024Article
- Ultrasound-targeted microbubble destruction improves the suppression and magnetic resonance imaging of pancreatic cancer with polyethyleneimine nanogels.Journal of Cancer · 2024Article
- Albumin Nanoparticle-Based Drug Delivery Systems.International journal of nanomedicine · 2024Review
- Delivery of miRNAs Using Nanoparticles for the Treatment of Osteosarcoma.International journal of nanomedicine · 2024Review
- Delivery of nucleic acids using nanomaterials.Molecular biomedicine · 2023Review
Corrections and comments
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Authors and funding
5 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Polyethyleneimine (PEI) has been extensively investigated as an efficient carrier for nucleic acid delivery. Yet, it suffers from a high toxicity profile that hinders clinical translation. Fluorination has proven to be a valid approach to reduce the cytotoxicity of PEI and improve the in vitro siRNA delivery potency. Hydrophobicity and lipophobicity can be controllably introduced into the side chains of PEI. However, the effect of fluorination on siRNA delivery in vivo, particularly the biodistribution of siRNA polyplex nanoparticles with fluorinated PEIs, has not been extensively explored. Here, we introduce two series of fluorinated PEIs via amidation with ethyl trifluoroacetate and perfluorobutyryl chloride. Fluorination substantially improved the performance of PEI for siRNA delivery by reducing the cytotoxicity to MDA-MB-231 cells. Importantly, fluorinated PEI enabled the major accumulation of siRNA polyplex nanoparticles in the liver while non-fluorinated PEI delivered siRNA nanoparticles mainly to the lungs after intravenous administration to mice. It is envisioned that fluorination may be an important general strategy for lowering toxicity of cationic polymers, and that the fluorination-induced alteration of biodistribution may be applicable for improved delivery to different organs. Graphical abstract.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.