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Effectiveness and toxicity screening of various absorption enhancers using Caco-2 cell monolayers.
Biol Pharm Bull. 1998 Jun; 21(6):615-20.BP

Abstract

We studied the enhancing and toxic effects of five different absorption enhancers on the transport of FITC-dextran with an average molecular weight of 4000 (FD-4) across Caco-2 cell monolayers, and their enhancing effects were also compared with those in rat intestine. The enhancing and cytotoxic properties of these enhancers were characterized using the following tests: measurement of the permeability coefficients of FD-4 and the transepithelial electrical resistance (TEER) in Caco-2, the release of cytosolic lactate dehydrogenase (LDH) and intracellular mitochondrial dehydrogenase (MDH) activity. All the absorption enhancers increased the permeability of FD-4 across Caco-2 cell monolayers and a good relationship was observed between the enhancement and their toxic effects. However, EDTA and Na-Cap were effective for improving the transport of FD-4 across Caco-2 cells without serious cytotoxicity. At concentrations with low cytotoxicity, various absorption enhancers exihibited reversible effects on the TEER values in Caco-2 cell monolayers, except for 50 mM sodium salicylate (Na-Sal). Moreover, we obtained a good correlation between the enhancement of these enhancers in Caco-2 cell monolayers and in rat large intestine. This finding indicated that the effectiveness of absorption enhancers in the Caco-2 monolayer system was similar to an in vivo rat system. Therefore, the screening system using Caco-2 cell monolayers is useful for examining the effectiveness and toxicity of absorption enhancers.

Authors+Show Affiliations

Department of Biopharmaceutics, Kyoto Pharmaceutical University, Japan.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

9657048

Citation

Quan, Y S., et al. "Effectiveness and Toxicity Screening of Various Absorption Enhancers Using Caco-2 Cell Monolayers." Biological & Pharmaceutical Bulletin, vol. 21, no. 6, 1998, pp. 615-20.
Quan YS, Hattori K, Lundborg E, et al. Effectiveness and toxicity screening of various absorption enhancers using Caco-2 cell monolayers. Biol Pharm Bull. 1998;21(6):615-20.
Quan, Y. S., Hattori, K., Lundborg, E., Fujita, T., Murakami, M., Muranishi, S., & Yamamoto, A. (1998). Effectiveness and toxicity screening of various absorption enhancers using Caco-2 cell monolayers. Biological & Pharmaceutical Bulletin, 21(6), 615-20.
Quan YS, et al. Effectiveness and Toxicity Screening of Various Absorption Enhancers Using Caco-2 Cell Monolayers. Biol Pharm Bull. 1998;21(6):615-20. PubMed PMID: 9657048.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effectiveness and toxicity screening of various absorption enhancers using Caco-2 cell monolayers. AU - Quan,Y S, AU - Hattori,K, AU - Lundborg,E, AU - Fujita,T, AU - Murakami,M, AU - Muranishi,S, AU - Yamamoto,A, PY - 1998/7/10/pubmed PY - 1998/7/10/medline PY - 1998/7/10/entrez SP - 615 EP - 20 JF - Biological & pharmaceutical bulletin JO - Biol Pharm Bull VL - 21 IS - 6 N2 - We studied the enhancing and toxic effects of five different absorption enhancers on the transport of FITC-dextran with an average molecular weight of 4000 (FD-4) across Caco-2 cell monolayers, and their enhancing effects were also compared with those in rat intestine. The enhancing and cytotoxic properties of these enhancers were characterized using the following tests: measurement of the permeability coefficients of FD-4 and the transepithelial electrical resistance (TEER) in Caco-2, the release of cytosolic lactate dehydrogenase (LDH) and intracellular mitochondrial dehydrogenase (MDH) activity. All the absorption enhancers increased the permeability of FD-4 across Caco-2 cell monolayers and a good relationship was observed between the enhancement and their toxic effects. However, EDTA and Na-Cap were effective for improving the transport of FD-4 across Caco-2 cells without serious cytotoxicity. At concentrations with low cytotoxicity, various absorption enhancers exihibited reversible effects on the TEER values in Caco-2 cell monolayers, except for 50 mM sodium salicylate (Na-Sal). Moreover, we obtained a good correlation between the enhancement of these enhancers in Caco-2 cell monolayers and in rat large intestine. This finding indicated that the effectiveness of absorption enhancers in the Caco-2 monolayer system was similar to an in vivo rat system. Therefore, the screening system using Caco-2 cell monolayers is useful for examining the effectiveness and toxicity of absorption enhancers. SN - 0918-6158 UR - https://www.unboundmedicine.com/medline/citation/9657048/Effectiveness_and_toxicity_screening_of_various_absorption_enhancers_using_Caco_2_cell_monolayers_ DB - PRIME DP - Unbound Medicine ER -