ArticlePharmaceutical research2000
Mechanisms of transport and structure-permeability relationship of sulfasalazine and its analogs in Caco-2 cell monolayers.
Article in Pharmaceutical research, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 81 citations in OpenAlex.
- Mesalazine-PAMAM Nanoparticles for Transporter-Independent Intracellular Drug Delivery: Cellular Uptake and Anti-Inflammatory Activity.International journal of nanomedicine · 2023Article
- Clinical Pharmacokinetic and Pharmacodynamic Considerations in the Treatment of Inflammatory Bowel Disease.Clinical pharmacokinetics · 2018Review
- A novel biosensor based on intestinal 3D organoids for detecting the function of BCRP.Drug delivery · 2017Article
- Real-time imaging and quantitative analysis of doxorubicin transport in a perfusable microvessel platform.Integrative biology : quantitative biosciences from nano to macro · 2016Article
- Prediction of the permeability of neutral drugs inferred from their solvation properties.Bioinformatics (Oxford, England) · 2016Article
- Review article: The pharmacokinetics and pharmacodynamics of drugs used in inflammatory bowel disease treatment.European journal of clinical pharmacology · 2015Review
- Study on the mechanism of intestinal absorption of epimedins a, B and C in the Caco-2 cell model.Molecules (Basel, Switzerland) · 2014Article
- Computational models to assign biopharmaceutics drug disposition classification from molecular structure.Pharmaceutical research · 2007Article
- Predicting effect of food on extent of drug absorption based on physicochemical properties.Pharmaceutical research · 2007Article
- Mechanisms responsible for poor oral bioavailability of paeoniflorin: Role of intestinal disposition and interactions with sinomenine.Pharmaceutical research · 2006Article
- Transport studies with 5-aminosalicylate.European journal of clinical pharmacology · 2006Article
- Membrane transport of camptothecin: facilitation by human P-glycoprotein (ABCB1) and multidrug resistance protein 2 (ABCC2).BMC medicine · 2004Article
- Development of sulfasalazine resistance in human T cells induces expression of the multidrug resistance transporter ABCG2 (BCRP) and augmented production of TNFalpha.Annals of the rheumatic diseases · 2004Article
- The "high solubility" definition of the current FDA Guidance on Biopharmaceutical Classification System may be too strict for acidic drugs.Pharmaceutical research · 2004Article
- Pharmacokinetic considerations in the treatment of inflammatory bowel disease.Clinical pharmacokinetics · 2001Review
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Authors and funding
3 authors at 1 institution in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo investigate the mechanisms involved in transport of sulfasalazine in Caco-2 cells.
methodsPermeability coefficients of sulfasalazine and its analogs across Caco-2 cell monolayers were measured as a function of direction of transport, energy and concentration dependence, and in the presence of inhibitors of various cellular efflux pumps and transporters.
resultsPermeability coefficients of sulfasalazine across Caco-2 cell monolayers were approximately 342-, 261-, and 176-fold higher from basolateral to apical direction (BL-->AP) than from apical to basolateral direction (AP-->BL) at 100, 200, and 500 microM, respectively. Carrier permeability coefficient, non-saturable membrane permeability coefficient, and Michaelis constant were estimated to be 1.4x10(-5) cm/s, 1.9x10(-8) cm/s, and 369 microM, respectively. The efflux of sulfasalazine was completely blocked at 4 degrees C and in the presence of an uncoupler of oxidative phosphorylation. Using cellular efflux inhibitors, the permeability of sulfasalazine was shown to depend on multidrug resistance-associated protein and anion sensitive transport mechanisms. Structure-permeability studies showed that the affinity of sulfasalazine for the cellular efflux pumps and transporters in Caco-2 cells depended strongly on the carboxylic acid functional group.
conclusionsThe permeability of sulfasalazine across Caco-2 cell monolayer is very low due to its strong interaction with multiple cellular efflux pumps and transporters. This may partially explain its low absorption in vivo.
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