ArticlePharmaceutical research1997
In vitro permeability across Caco-2 cells (colonic) can predict in vivo (small intestinal) absorption in man--fact or myth.
Article in Pharmaceutical research, 1997. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 252 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
252 citing papers in PubMed.
- Copper oxide nanoparticles: from EU-regulatory landscape and mechanistic toxicity towards a cuproptosis-linked adverse outcome pathway.Archives of toxicology · 2026Review
- About the impact of medium chain fatty acids on the permeation enhancing effects of self-emulsifying drug delivery systems.Drug delivery and translational research · 2026Article
- A Dynamic Gastrointestinal Mucus Simulator for Biorelevant Assessment of Nutrient Mucopenetration: Effects of Mucus Purification, Calcium, and Soluble Fibers.Foods (Basel, Switzerland) · 2026Article
- Estimating Permeabilities from Biased Molecular Dynamics with a Green-Kubo Formalism for Transport across the Blood-Brain Barrier.Journal of chemical information and modeling · 2026Article
- The Transepithelial Transport and Transport Pathways of Free and Bound Nε-Carboxymethyllysine Using a Caco-2 Cell Monolayer Model.Foods (Basel, Switzerland) · 2026Article
- Evaluation of the antimicrobial and NorA and MepA efflux pump inhibitory activity of a hydrazone derivative of hydralazine against Staphylococcus aureus.Archives of microbiology · 2026Article
- Article
- Polydatin for treating spinal cord injury: Multiple mechanisms and challenges.Journal of pharmaceutical analysis · 2026Review
- Enhancing the Predictive Power of Macrocyclic Drug Permeability by Knowledge Distillation from Analogous Pretraining Data.Journal of medicinal chemistry · 2026Article
- CaliciBoost: Performance-driven evaluation of molecular representations for caco-2 permeability prediction.Journal of cheminformatics · 2025Article
- Preclinical Development of GT-14, a Novel Inhibitor of GαThe AAPS journal · 2025Article
- Evaluation of the intestinal transmembrane transport and absorption characteristics of mangiferin in rats by the Ussing chamber technique.Biochemistry and biophysics reports · 2025Article
- Challenges of Aufheben to Promote Druglikeness: Chemical Modification Strategies to Improve Aqueous Solubility and Permeability.Journal of medicinal chemistry · 2025Review
- Evaluation of the Pharmacokinetic Interactions ofACS omega · 2025Article
- Investigating the Antimicrobial Efficacy of Cannabinoids and Their Derivatives AgainstBiology · 2025Article
- Fingerprinting the Intestinal Transport of Low-Molecular-Mass Advanced Glycation End-Products (AGEs) Using a Caco-2 Transwell Model.Journal of agricultural and food chemistry · 2025Article
- Exploring absorption indices for a variety of polyphenols through Caco-2 cell model: insights from permeability studies and principal component analysis.Journal of the science of food and agriculture · 2025Article
- Angiotensin-Converting Enzyme Inhibitory Peptide Derived from UltrafineJournal of agricultural and food chemistry · 2025Article
- Application of Lipophilic Prodrug Charge Masking Strategy to Obtain Novel, Potential Oxytocin Prodrugs.International journal of molecular sciences · 2025Article
- In vitro and in silico evaluation of synthetic compounds derived from bi-triazoles against asexual and sexual forms of Plasmodium falciparum.Malaria journal · 2025Article
192 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
1 author.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo evaluate and optimize the use of Caco-2 cell monolayers to predict the in vivo absorption of a broad range of compounds in man.
methodsCaco-2 cells are derived from human adenocarcinoma colon cells and spontaneously differentiate when grown on porous polyethylene terephthalate membranes (PETP) in a 12 well format to form monolayers of polarized cells possessing function similar to intestinal enterocytes. Transport experiments were conducted using 21 day cultured cells in a shaking water bath at 37 degrees C. Radiolabeled mannitol was used to determine monolayer integrity. Apparent permeability coefficient (Papp) was calculated from the appearance of drug in the receiver side.
resultsA strong correlation was observed between in vivo human absorption and in vitro Papp for a variety of compounds (R = 0.95, N = 35). For compounds that are substrates of p-glycoprotein (Pgp), use of a Pgp inhibitor resulted in a better estimate of absorption in humans. The results of this study suggest that the overall ranking of compounds with Papp < 1 x 10(-6) cm/sec, between 1-10 x 10(-5) cm/ sec, and > 10 x 10(-6) cm/sec can be classified as poorly (0-20%), moderately (20-70%) and well (70-100%) absorbed compounds, respectively.
conclusionsThese data suggest that Caco-2 cells developed under the culturing and transport conditions defined herein can be used to predict in vivo human absorption of compounds regardless of transport mechanism, viz., transcellular, paracellular and carrier-mediated.
Indexed as
Identifiers
9210194What 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.