THE USE OF CACO-2 CELL MONOLAYERS AS A MODEL TO PREDICT HUMAN INTESTINAL PERMEABILILITY AND DRUG ABSORPTION

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ZAKERI MILANI P.; VALIZADEH H.

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Journal: PHARMACEUTICAL SCIENCES Year:2006 | Volume:- | Issue:4 Page(s): 71-77

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Title

THE USE OF CACO-2 CELL MONOLAYERS AS A MODEL TO PREDICT HUMAN INTESTINAL PERMEABILILITY AND DRUG ABSORPTION

Author(s)

ZAKERI MILANI P. | VALIZADEH H. | Issue Writer Certificate

Keywords

CACO-2Q2

PEFFQ2

PAPPQ2

PERMEABILITY- PASSIVELY ABSORBEDQ2

FRACTION DOSE ABSORBEDQ2

Abstract

Objectives: The purpose of the study was to predict the human intestinal permeability and the fraction of oral dose absorbed using CACO-2 system. METHODS: Permeability coefficients were determined for nine passively absorbed compounds in CACO-2 system. CACO-2 monolayers were grown on porous filters in multi-well plates as monolayers. Drug solution in HBSS was added to top inserts (apical sides) and then the inserts with plate were incubated at 37° C for 60 min with shaking (-70 rpm). Samples were collected at 60 min from basolateral sides. Lucifer yellow was applied as marker for monolayer integrity in CACO-2 minelayers. Drug concentrations in samples were determined using HPLC equipment and permeability coefficients were calculated. Finally the obtained values were compared with published data for human intestinal permeability and fraction of dose absorbed in human. RESULTS: The relationship between penneabilities was found to be 10gPeff(human)= 0.65 logP app(CACO-2) - 0.37 (R2= 0.79, P= 0.001). The fraction of dose absorbed in vivo in human (Fa) after oral dosing can also be estimated from Fa (human) = 100 (1-e 1917852 Papp(CACO-2) (R2= 0.91, P= 0.0002). CONCLUSION: Therefore we conclude that the CACO-2 system has the potential for the prediction of human intestinal permeability and fraction of oral dose absorbed in human (Fa) as well.

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APA: Copy

ZAKERI MILANI, P., & VALIZADEH, H.. (2006). THE USE OF CACO-2 CELL MONOLAYERS AS A MODEL TO PREDICT HUMAN INTESTINAL PERMEABILILITY AND DRUG ABSORPTION. PHARMACEUTICAL SCIENCES, -(4), 71-77. SID. https://sid.ir/paper/48738/en

Vancouver: Copy

ZAKERI MILANI P., VALIZADEH H.. THE USE OF CACO-2 CELL MONOLAYERS AS A MODEL TO PREDICT HUMAN INTESTINAL PERMEABILILITY AND DRUG ABSORPTION. PHARMACEUTICAL SCIENCES[Internet]. 2006;-(4):71-77. Available from: https://sid.ir/paper/48738/en

IEEE: Copy

P. ZAKERI MILANI, and H. VALIZADEH, “THE USE OF CACO-2 CELL MONOLAYERS AS A MODEL TO PREDICT HUMAN INTESTINAL PERMEABILILITY AND DRUG ABSORPTION,” PHARMACEUTICAL SCIENCES, vol. -, no. 4, pp. 71–77, 2006, [Online]. Available: https://sid.ir/paper/48738/en

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