ArticlePharmaceutical research2013
Effect of PEGylation on biodistribution and gene silencing of siRNA/lipid nanoparticle complexes.
Article in Pharmaceutical research, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 47 papers.
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Who cites it
47 citing papers in PubMed, 103 citations in OpenAlex.
- siRNA Nanoparticle Delivery Strategies and Clinical Trial Advances in Tumor Therapy.International journal of molecular sciences · 2026Review
- Impact and Significance of Viral Vectors for siRNA Delivery in the Treatment of Alzheimer's Disease.Current pharmaceutical biotechnology · 2026Review
- mRNA delivery systems 2.0: Engineering extrahepatic delivery for non-vaccine therapeutics.Materials today. Bio · 2025Review
- Targeting and tracking mRNA lipid nanoparticles at the particle, transcript and protein level.Nature biomedical engineering · 2025Review
- Modulating Immunogenicity and Reactogenicity in mRNA-Lipid Nanoparticle Vaccines through Lipid Component Optimization.ACS nano · 2025Article
- Liposome Encapsulation Enhances Ripasudil Therapeutic Efficacy Against Proliferative Vitreoretinal Diseases: Implications in Advanced Ocular Treatment.Investigative ophthalmology & visual science · 2025Article
- Multiparametric functional characterization of individual lipid nanoparticles using surface-sensitive light-scattering microscopy.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Cationic Liposomes Carrying HPV16 E6-siRNA Inhibit the Proliferation, Migration, and Invasion of Cervical Cancer Cells.Pharmaceutics · 2024Article
- Advances in non-viral mRNA delivery to the spleen.Biomaterials science · 2024Review
- Strategies to reduce the risks of mRNA drug and vaccine toxicity.Nature reviews. Drug discovery · 2024Review
- Poly(2-methyl-2-oxazoline) as a polyethylene glycol alternative for lipid nanoparticle formulation.Frontiers in drug delivery · 2024Article
- Immunogenicity of lipid nanoparticles and its impact on the efficacy of mRNA vaccines and therapeutics.Experimental & molecular medicine · 2023Review
- Understanding Intracellular Biology to Improve mRNA Delivery by Lipid Nanoparticles.Small methods · 2023Article
- Analysis of PEG-lipid anchor length on lipid nanoparticle pharmacokinetics and activity in a mouse model of traumatic brain injury.Biomaterials science · 2023Article
- Taylor Dispersion Analysis to support lipid-nanoparticle formulations for mRNA vaccines.Gene therapy · 2023Article
- Lipid Nanoparticles as Promising Carriers for mRNA Vaccines for Viral Lung Infections.Pharmaceutics · 2023Review
- A Comprehensive Review of Small Interfering RNAs (siRNAs): Mechanism, Therapeutic Targets, and Delivery Strategies for Cancer Therapy.International journal of nanomedicine · 2023Review
- Cancerous pH-responsive polycarboxybetaine-coated lipid nanoparticle for smart delivery of siRNA against subcutaneous tumor model in mice.Cancer science · 2022Article
- Protection of Double-Stranded RNABiomacromolecules · 2022Article
- Optimization of phospholipid chemistry for improved lipid nanoparticle (LNP) delivery of messenger RNA (mRNA).Biomaterials science · 2022Article
Corrections and comments
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Authors and funding
12 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo determine the influence of physicochemical properties of lipid nanoparticles (LNPs) carrying siRNA on their gene silencing in vivo. Mechanistic understanding of how the architecture of the nanoparticle can alter gene expression has also been studied.
methodsThe effect of 3-N-[(ω-methoxypoly(ethylene glycol)2000)carbamoyl]-1,2-dimyristyloxy-propylamine (PEG-C-DMA) on hepatic distribution and FVII gene silencing was determined. FVII mRNA in hepatocytes and liver tissues was determined by Q-PCR. Hepatic distribution was quantified by FACS analysis using Cy5 labeled siRNA.
resultsGene silencing was highly dependent on the amount of PEG-C-DMA present. FVII gene silencing inversely correlated to the amount of PEG-C-DMA in LNPs. High FVII gene silencing was obtained in vitro and in vivo when the molar ratio of PEG-C-DMA to lipid was 0.5 mol%. Surprisingly, PEGylation didn't alter the hepatic distribution of the LNPs at 5 h post administration. Instead the amount of PEG present in the LNPs has an effect on red blood cell disruption at low pH.
conclusionLow but sufficient PEG-C-DMA amount in LNPs plays an important role for efficient FVII gene silencing in vivo. PEGylation did not alter the hepatic distribution of LNPs, but altered gene silencing efficacy by potentially reducing endosomal disruption.
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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.