ReviewTissue barriers
Safety concerns over the use of intestinal permeation enhancers: A mini-review.
Review in Tissue barriers. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 51 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
51 citing papers in PubMed, 146 citations in OpenAlex.
- Re-engineering insulin for oral delivery: structural modifications, advanced formulation strategies, and future directions.Drug delivery · 2026Review
- Engineering Oral Nanoparticles: Navigating Biological Barriers in the Gastrointestinal Tract.Pharmaceutical research · 2026Review
- Natural Oral Absorption of Therapeutic Peptides: Mechanisms and Physiological Determinants.Pharmaceutics · 2026Review
- Formulation Engineering of Oral Semaglutide Tablets: Unleashing Gastric Intestinal Permeation with Sodium Caprate.Pharmaceutics · 2026Article
- Plant- and Microalgae-Based Biotechnological Strategies for Affordable and Non-Invasive Delivery of Antidiabetic Peptides.Pharmaceutics · 2026Review
- Small Intestine-Targeted Long-Acting Oral Insulin Formulation Based on Engineered Milk Protein Nanoparticles.ACS applied bio materials · 2026Article
- Inflammation-triggered self-immolative conjugates enable oral peptide delivery by overcoming gastrointestinal barriers.Science advances · 2026Article
- Recent Advances in Oral Drug Delivery Systems for BCS III Drugs.Current issues in molecular biology · 2026Review
- Food-derived molecules as regulators of intestinal tight junctions and barrier function: mechanisms and implications.Frontiers in drug delivery · 2026Review
- Longitudinal Plasma Multiomics Characterization of Nephrotoxicity in Beagles Following Repeated Dosing of Enteric-Coated Propyl Gallate Tablets.ACS pharmacology & translational science · 2025Article
- Enhanced macromolecule bioavailability in rats and pigs using an in situ forming synthetic epithelial lining.Journal of controlled release : official journal of the Controlled Release Society · 2025Article
- Overcoming Oral Cavity Barriers for Peptide Delivery Using Advanced Pharmaceutical Techniques and Nano-Formulation Platforms.Biomedicines · 2025Review
- Permeation enhancer-induced membrane defects assist the oral absorption of peptide drugs.Nature communications · 2025Article
- Impact of Permeation Enhancers on the Release of Insulin from Tablets in Biorelevant Media.Molecular pharmaceutics · 2025Article
- Modification of Peptide and Permeation Enhancer In Vitro Release Rates by Dispersion with a Gel-Forming Polymer.Pharmaceutical research · 2025Article
- Porcine intestinal organoids cultured in an organ-on-a-chip microphysiological system.Biochemistry and biophysics reports · 2025Article
- Biofunctional Excipients: Their Emerging Role in Overcoming the Inherent Poor Biopharmaceutical Characteristics of Drugs.Pharmaceutics · 2025Review
- Size-selective permeation-enhancing modulation of the tight junction by receptor-binding domains ofTissue barriers · 2025Article
- Molecular Chimera in Cancer Drug Discovery: Beyond Antibody Therapy, Designing Grafted Stable Peptides Targeting Cancer.International journal of peptide research and therapeutics · 2025Review
- Inflammation-oriented montmorillonite adjuvant enhanced oral delivery of anti-TNF-α nanobody against inflammatory bowel disease.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Intestinal permeation enhancers (PEs) are key components in ∼12 oral peptide formulations in clinical trials for a range of molecules, primarily insulin and glucagon-like-peptide 1 (GLP-1) analogs. The main PEs comprise medium chain fatty acid-based systems (sodium caprate, sodium caprylate, and N-[8-(2-hydroxybenzoyl) amino] caprylate (SNAC)), bile salts, acyl carnitines, and EDTA. Their mechanism of action is complex with subtle differences between the different molecules. With the exception of SNAC and EDTA, most PEs fluidize the plasma membrane causing plasma membrane perturbation, as well as enzymatic and intracellular mediator changes that lead to alteration of intestinal epithelial tight junction protein expression. The question arises as to whether PEs can cause irreversible epithelial damage and tight junction openings sufficient to permit co-absorption of payloads with bystander pathogens, lipopolysaccharides and its fragment, or exo- and endotoxins that may be associated with sepsis, inflammation and autoimmune conditions. Most PEs seem to cause membrane perturbation to varying extents that is rapidly reversible, and overall evidence of pathogen co-absorption is generally lacking. It is unknown however, whether the intestinal epithelial damage-repair cycle is sustained during repeat-dosing regimens for chronic therapy.
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What OpenQuestion holds
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.