PMID: 2118955Jul 1, 1990Paper

Epithelial transport of drugs in cell culture. II: Effect of extracellular calcium concentration on the paracellular transport of drugs of different lipophilicities across monolayers of intestinal epithelial (Caco-2) cells

Journal of Pharmaceutical Sciences
P Artursson, C Magnusson

Abstract

A human intestinal cell line, Caco-2, was used as a model to study the passive diffusion of a homologous series of drugs (beta-blocking agents) of different lipophilicity across intestinal epithelium. The permeability of the Caco-2 monolayers was modulated by the use of a calcium switch assay. The transmembrane resistance could be reversibly decreased from approximately 280 ohms.cm2 (a resistance similar to that of colon epithelium) to approximately 60 ohms.cm2 (a resistance similar to that of small intestine epithelium). Transmission electron microscopy showed that the increased electrical permeability was caused by a reversible separation of the components of the junctional complex and not by cell detachment. In general, the increased paracellular permeability resulted in a 2- to 9-fold increase in the apparent permeability coefficients for the more hydrophilic drugs (e.g., from 0.20 +/- 0.010 x 10(-6) to 1.43 +/- 0.185 x 10(-6) cm/s for atenolol), while the transport parameters for the more lipophilic drugs remained unchanged (e.g., 43.03 +/- 3.64 x 10(-6) and 46.10 +/- 3.25 x 10(-6) cm/s for propranolol). These findings indicate that it is possible to study the contribution of the paracellular pathway to the transport of dr...Continue Reading

References

Dec 1, 1985·The Journal of Cell Biology·J L Madara, K Dharmsathaphorn
Dec 1, 1980·The Journal of Cell Biology·A Martinez-PalomoM Cereijido
Jan 1, 1980·Journal of Immunological Methods·J J HesslingN L Levy

❮ Previous
Next ❯

Citations

Mar 1, 1995·Medicinal Research Reviews·K M HillgrenR T Borchardt
Apr 1, 1993·Pflügers Archiv : European journal of physiology·M ParisiJ Bourguet
Sep 2, 1998·European Journal of Drug Metabolism and Pharmacokinetics·L BartheG Houin
May 24, 2006·European Journal of Drug Metabolism and Pharmacokinetics·C R HuangJ G Sun
Jul 14, 2005·European Journal of Drug Metabolism and Pharmacokinetics·F MathieuC Lartigue
Jan 26, 2007·Pharmaceutical Research·Cécile MénezGillian Barratt
Sep 15, 1994·Biochemical Pharmacology·M SakaiD D Breimer
Jun 6, 1993·Biochimica Et Biophysica Acta·P WilsD Scherman
Mar 17, 2004·International Journal of Pharmaceutics·Simon ZakeljAlbin Kristl
May 28, 2013·International Journal of Pharmaceutics·Ellen HagesaetherTrond Ulven
Oct 9, 2002·Toxicon : Official Journal of the International Society on Toxinology·Darío AndrinoloNéstor Lagos
Aug 19, 2003·Biomaterials·Ruxandra GrefEvgueni Mysiakine
Aug 1, 1998·Journal of Controlled Release : Official Journal of the Controlled Release Society·A F KotzéH E Junginger
Jul 25, 2003·International Journal of Pharmaceutics·Johanna RaimanJukka Mönkkönen
Apr 17, 1999·International Journal of Pharmaceutics·M J Ginski, J E Polli
Aug 1, 1999·Toxicology in Vitro : an International Journal Published in Association with BIBRA·G VelardeJ M Porcher
Sep 24, 1999·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·J KarlssonP Artursson
Sep 28, 2012·Journal of Agricultural and Food Chemistry·Bing ZhangZe-Yuan Deng
Jul 1, 1992·Antimicrobial Agents and Chemotherapy·G RanaldiY Sambuy
Dec 15, 2015·Bioinformatics·Edoardo MilanettiAnna Tramontano
Apr 25, 2008·Expert Opinion on Drug Metabolism & Toxicology·Huadong SunK Sandy Pang
Jul 29, 2000·Drug Development and Industrial Pharmacy·A K SinglaA Singh
Jan 23, 2009·Journal of Pharmaceutical Sciences·C BeckerD M Barends

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.