ArticlePharmaceutical research2008
Safe and effective permeation enhancers for oral drug delivery.
Article in Pharmaceutical research, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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Who cites it
44 citing papers in PubMed, 133 citations in OpenAlex.
- Numerical simulation of PDRN iontophoresis: comparison with passive diffusion and key parameter analysis.Drug delivery · 2026Article
- Oral peptide drug delivery: design of SEDDS providing a protective effect against intestinal membrane-bound enzymes.Drug delivery and translational research · 2026Article
- Piperazine-Functionalized Nanoparticles Enable Oral Insulin Delivery in Obese Mice.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Skin-Interfaced Therapeutic Patches for Wound Fluid Management and Transdermal Drug Delivery.Advanced healthcare materials · 2026Article
- Extended local anesthesia enabled by flavonoid permeation enhancers.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- Oral delivery of peptides and proteins: pharmacokinetic boundaries, negative selection, and route triage.Frontiers in drug delivery · 2026Review
- 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
- Modification of Peptide and Permeation Enhancer In Vitro Release Rates by Dispersion with a Gel-Forming Polymer.Pharmaceutical research · 2025Article
- 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
- A new crystalline daidzein-piperazine salt with enhanced solubility, permeability, and bioavailability.Frontiers in pharmacology · 2024Article
- Mucosal Penetrative Polymeric Micelle Formulations for Insulin Delivery to the Respiratory Tract.International journal of nanomedicine · 2024Article
- Storming the gate: New approaches for targeting the dynamic tight junction for improved drug delivery.Advanced drug delivery reviews · 2023Review
- SNAC for Enhanced Oral Bioavailability: An Updated Review.Pharmaceutical research · 2023Review
- Long-term daily oral administration of intestinal permeation enhancers is safe and effective in mice.Bioengineering & translational medicine · 2023Article
- The strawberry-derived permeation enhancer pelargonidin enables oral protein delivery.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Surfactant-Free Glibenclamide Nanoparticles: Formulation, Characterization and Evaluation of Interactions with Biological Barriers.Pharmaceutical research · 2021Article
- Zwitterionic micelles efficiently deliver oral insulin without opening tight junctions.Nature nanotechnology · 2020Article
- Review of recently used techniques and materials to improve the efficiency of orally administered proteins/peptides.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2020Review
- Advances in oral peptide therapeutics.Nature reviews. Drug discovery · 2020Review
- Investigations of Piperazine Derivatives as Intestinal Permeation Enhancers in Isolated Rat Intestinal Tissue Mucosae.The AAPS journal · 2020Article
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
purposeThe use of intestinal permeation enhancers to overcome the absorption challenges associated with oral drug delivery has been hampered by the notion that enhancer efficacy is directly linked to toxicity. This study attempts to gain insight into the principles governing the potency and toxicity behavior of enhancers.
methodsFifty-one enhancers were selected from 11 chemical categories and their potency and toxicity were analyzed in Caco-2 monolayers at concentrations spanning three orders of magnitude.
resultsA small but significant fraction of the 153 enhancer formulations studied demonstrated unexpected but desired behavior, that is, substantial efficacy without marked toxicity. Our results revealed that both chemical category and concentration proved critical in determining the usefulness of many enhancers, and the concept of an enhancer's 'therapeutic window' is discussed. Several of the most promising enhancers identified by the study were tested for their effect on the transport of the marker molecules mannitol and 70 kDa dextran across Caco-2 cells and were capable of increasing permeability more than 10-fold.
conclusionsThe results presented here underscore the potential of chemical permeation enhancers while providing valuable direction as to what classes and concentrations of compounds are of interest when searching for safe and effective additions to oral formulations.
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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.