ArticleScientific reports2018
Oral delivery of siRNA lipid nanoparticles: Fate in the GI tract.
Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 60 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
60 citing papers in PubMed.
- Emerging nanotechnology-enabled siRNA oral delivery platforms.Nanomedicine (London, England) · 2026Review
- Targeted oral delivery of microencapsulated TNF-α siRNA in an experimental model of colitis.Drug delivery and translational research · 2026Article
- Unveiling the Silent Regulators: Noncoding RNAs in Parasitic Disease Diagnosis and Therapy.Journal of parasitology research · 2026Review
- A Novel Method to Silence Genes in Cryptosporidium.Methods in molecular biology (Clifton, N.J.) · 2026Article
- Critical quality attributes of lipid nanoparticles andAsian journal of pharmaceutical sciences · 2025Review
- Engineered extracellular vesicles demonstrate altered endocytosis and biodistribution and have superior oral siRNA delivery efficiency compared to lipid nanoparticles.International journal of pharmaceutics: X · 2025Article
- Harnessing mRNA-lipid nanoparticles as innovative therapies for autoimmune diseases.Molecular therapy. Methods & clinical development · 2025Review
- From mechanism to applications: Advanced microneedles for clinical medicine.Bioactive materials · 2025Review
- The role of excipients in lipid nanoparticle metabolism: implications for enhanced therapeutic effect.Therapeutic delivery · 2025Review
- Nanoparticle-Driven Modulation of Mucosal Immunity and Interplay with the Microbiome.Journal of microbiology and biotechnology · 2025Review
- Oral delivery of stabilized lipid nanoparticles for nucleic acid therapeutics.Drug delivery and translational research · 2025Article
- Self-disassembling nanoparticles as oral nanotherapeutics targeting intestinal microenvironment.Nature communications · 2025Article
- Emerging role of small RNAs in inflammatory bowel disease and associated colorectal cancer (Review).International journal of molecular medicine · 2025Review
- Maternal milk cell components are uptaken by infant liver macrophages via extracellular vesicle mediated transport.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2025Article
- Comprehensive analysis of lipid nanoparticle formulation and preparation for RNA delivery.International journal of pharmaceutics: X · 2024Review
- Strategies for non-viral vectors targeting organs beyond the liver.Nature nanotechnology · 2024Review
- Current RNA strategies in treating cardiovascular diseases.Molecular therapy : the journal of the American Society of Gene Therapy · 2024Review
- Engineered smart materials for RNA based molecular therapy to treat Glioblastoma.Bioactive materials · 2024Article
- Enteral Route Nanomedicine for Cancer Therapy.International journal of nanomedicine · 2024Review
- Principle, application and challenges of development siRNA-based therapeutics against bacterial and viral infections: a comprehensive review.Frontiers in microbiology · 2024Review
Corrections and comments
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Authors and funding
3 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Oral delivery, a patient-friendly means of drug delivery, is preferred for local administration of intestinal therapeutics. Lipidoid nanoparticles, which have been previously shown to deliver siRNA to intestinal epithelial cells, have potential to treat intestinal disease. It is unknown, however, whether the oral delivery of these particles is possible. To better understand the fate of lipid nanoparticles in the gastrointestinal (GI) tract, we studied delivery under deconstructed stomach and intestinal conditions in vitro. Lipid nanoparticles remained potent and stable following exposure to solutions with pH values as low as 1.2. Efficacy decreased following exposure to "fed", but not "fasting" concentrations of pepsin and bile salts. The presence of mucin on Caco-2 cells also reduced potency, although this effect was mitigated slightly by increasing the percentage of PEG in the lipid nanoparticle. Mouse biodistribution studies indicated that siRNA-loaded nanoparticles were retained in the GI tract for at least 8 hours. Although gene silencing was not initially observed following oral LNP delivery, confocal microscopy confirmed that nanoparticles entered the epithelial cells of the mouse small intestine and colon. Together, these data suggest that orally-delivered LNPs should be protected in the stomach and upper intestine to promote siRNA delivery to intestinal epithelial cells.
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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.