ArticleACS nano2017
Zwitterionic Nanocarrier Surface Chemistry Improves siRNA Tumor Delivery and Silencing Activity Relative to Polyethylene Glycol.
Article in ACS nano, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 52 papers.
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Who cites it
52 citing papers in PubMed, 125 citations in OpenAlex.
- Engineering Functional Biomaterials for Targeted and Localized Cancer Drug Delivery: A Structure-Property-Performance Design Perspective.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Rationally Designed Zwitterionic Peptides Improve siRNA Delivery of Cationic Diblock Copolymer-Based Nanoparticle Drug-Delivery Systems.ACS applied nano materials · 2026Article
- Blood-brain barrier-penetrative lipid nanoparticles enable systemic delivery of TRIM11 mRNA to disaggregate Tau in Alzheimer's disease models.Cell reports. Medicine · 2026Article
- Advances in constructing biocompatible nanocarriers.Drug delivery and translational research · 2025Review
- Induction of Triple-Negative Breast Cancer Cell Death and Chemosensitivity Using mTORC2-Directed RNAi Nanomedicine.Cancer research communications · 2025Article
- Precision tumor treatment utilizing bacteria: principles and future perspectives.Applied microbiology and biotechnology · 2025Review
- Synthetic-polymer-assisted antisense oligonucleotide delivery: targeted approaches for precision disease treatment.Beilstein journal of nanotechnology · 2025Review
- Zwitterionic lipid nanoparticles for efficient siRNA delivery and hypercholesterolemia therapy with rational charge self-transformation.Theranostics · 2025Article
- Efficient siRNA delivery to murine melanoma cellsNanoscale advances · 2024Article
- Injectable hydrogel encapsulating siMMP13 with anti-ROS and anti-apoptotic functions for osteoarthritis treatment.Journal of nanobiotechnology · 2024Article
- Beyond Lipids: Exploring Advances in Polymeric Gene Delivery in the Lipid Nanoparticles Era.Advanced materials (Deerfield Beach, Fla.) · 2024Review
- Synthesis of a dendritic cell-targeted self-assembled polymeric nanoparticle for selective delivery of mRNA vaccines to elicit enhanced immune responses.Chemical science · 2024Article
- Polymeric Nanoparticles for Drug Delivery.Chemical reviews · 2024Review
- Microfluidics-enabled fluorinated assembly of EGCG-ligands-siTOX nanoparticles for synergetic tumor cells and exhausted t cells regulation in cancer immunotherapy.Journal of nanobiotechnology · 2024Article
- Recent advances in zwitterionic nanoscale drug delivery systems to overcome biological barriers.Asian journal of pharmaceutical sciences · 2024Review
- Zwitterionic peptides: Tunable next-generation stealth nanoparticle modifications.Bioactive materials · 2023Article
- Core polymer optimization of ternary siRNA nanoparticles enhances in vivo safety, pharmacokinetics, and tumor gene silencing.Biomaterials · 2023Article
- Bacterial-Mediated Tumor Therapy: Old Treatment in a New Context.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2023Review
- Nanobiotechnology-Enabled mRNA Stabilization.Pharmaceutics · 2023Review
- Tissue-Targeted Drug Delivery Strategies to Promote Antigen-Specific Immune Tolerance.Advanced healthcare materials · 2023Review
Corrections and comments
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
Abstract
Although siRNA-based nanomedicines hold promise for cancer treatment, conventional siRNA-polymer complex (polyplex) nanocarrier systems have poor pharmacokinetics following intravenous delivery, hindering tumor accumulation. Here, we determined the impact of surface chemistry on the in vivo pharmacokinetics and tumor delivery of siRNA polyplexes. A library of diblock polymers was synthesized, all containing the same pH-responsive, endosomolytic polyplex core-forming block but different corona blocks: 5 kDa (benchmark) and 20 kDa linear polyethylene glycol (PEG), 10 kDa and 20 kDa brush-like poly(oligo ethylene glycol), and 10 kDa and 20 kDa zwitterionic phosphorylcholine-based polymers (PMPC). In vitro, it was found that 20 kDa PEG and 20 kDa PMPC had the highest stability in the presence of salt or heparin and were the most effective at blocking protein adsorption. Following intravenous delivery, 20 kDa PEG and PMPC coronas both extended circulation half-lives 5-fold compared to 5 kDa PEG. However, in mouse orthotopic xenograft tumors, zwitterionic PMPC-based polyplexes showed highest in vivo luciferase silencing (>75% knockdown for 10 days with single IV 1 mg/kg dose) and 3-fold higher average tumor cell uptake than 5 kDa PEG polyplexes (20 kDa PEG polyplexes were only 2-fold higher than 5 kDa PEG). These results show that high molecular weight zwitterionic polyplex coronas significantly enhance siRNA polyplex pharmacokinetics without sacrificing polyplex uptake and bioactivity within tumors when compared to traditional PEG architectures.
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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.