Effectiveness and Toxicity Screening of Various Absorption Enhancers Using Caco-2 Cell Monolayers

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概要

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• 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 50mM 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.

• 公益社団法人日本薬学会の論文
• 1998-06-15

著者

• YAMAMOTO Akira

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• MURAKAMI Masahiro

  Department of Synthetic Chemistry and Biological Chemistry, Graduate School of Engineering, Kyoto Un

• Lundborg Ewa

  Department Of Pharmaceutics Uppsala University

• MURANISHI Shozo

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• FUJITA Takuya

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• HATTORI KOJI

  Department of Orthopaedic Surgery, Nara Medical University

• Hattori Koji

  Department Of Cardiovascular Surgery Osaka City University Graduate School Of Medicine

• Fujita T

  Division Of Oral Cytology And Cell Biology Department Of Developmental And Reconstructive Medicine N

• FUJITA Takuya

  Ritsumeikan University College of Information Science and Engeneering

• Quan Ying-shu

  Department Of Biopharmaceutics Kyoto Pharmaceutical University:cosmed Pharmaceutical Co. Ltd.

• Yamamoto Akira

  Dep. Of Biopharmaceutics Kyoto Pharmaceutical Univ.

• Fujita T

  Ritsumeikan University College Of Information Science And Engeneering

• Fujita Takuya

  Department Of Basic Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University

• Fujita T

  Showa College Of Pharmaceutical Sciences

• Murakami Masahiro

  Department Of Biopharmaceutics Kyoto Pharmaceutical University

• Fukushima Tohru

  Department Of Pharmacology Faculty Of Pharmaceutical Sciences Setsunan University

• 村西 昌三

  京都薬大

• Muranishi Shozo

  Department Of Biopharmaceutics Kyoto Pharmaceutical University:exploratory Development Laboratories

• Muranishi Shozo

  Department Of Biopharmaceutics Kyoto Pharmaceutical University

• Yamamoto Akira

  Department Of Biopharmaceutics Kyoto Pharmaceutical University

• Yamamoto Akira

  Department Of Anatomy School Of Medicine University Of Tokushuma

• Hattori Koji

  Department Of Applied Biological Sciences Saga University

• Murakami Masahiro

  Department Of Aquatic Bioscience Graduate School Of Agricultural And Life Sciences The University Of

• Yamamoto Akira

  Department Of Anatomy School Of Medicine University Of Tokushima

• MURAKAMI MASAHIRO

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• MURAKAMI Masahiro

  Department of Anatomy, Kurume University School of Medicine

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