[KSCI] Korea Science Citation Index Service

http://dx.doi.org/10.4333/KPS.2010.40.6.363

Optimization of Experimental Conditions for In vitro P-glycoprotein Assay Using LLC-GA5 Cells

Ahn, A-Ra (Division of Biopharmaceutics, College of Pharmacy, Kyung Hee University)
Oh, Ju-Hee (Division of Biopharmaceutics, College of Pharmacy, Kyung Hee University)
Lee, Joo-Hyun (Division of Biopharmaceutics, College of Pharmacy, Kyung Hee University)
Lee, Young-Joo (Division of Biopharmaceutics, College of Pharmacy, Kyung Hee University)

Publication Information

Journal of Pharmaceutical Investigation / v.40, no.6, 2010 , pp. 363-366 More about this Journal

Abstract

Identification of compounds that function as P-glycoprotein (P-gp) substrates or inhibitors can facilitate the selection and optimization of new drug candidates. The purpose of this study is to optimize the experimental conditions for in vitro P-gp assay using LLC-GA5 cells, which is a well-known transformant cell line derived by transfecting LLC-PK1 with human MDR1. The amount of rhodamine123 transported by the LLC-GA5 and LLC-PK1 cells was evaluated under the following experimental conditions: 3 different types of transport media, colchicine pretreatment or nontreatment of the cells in the culture media, and with and without poly-L-lysine coating of the culture plates. The assay sensitivity was found to considerably differ depending on the diluents used in the transport media. P-gp-mediated transport in LLC-GA5 cells was most clearly characterized in the Hanks' balanced salt solution based transport media. The sensitivity of P-gp-mediated transport was not changed by colchicine pretreatment or poly-L-lysine coating of the culture plates.

Keywords

P-glycoprotein; LLC-GA5; Rhodamine 123; Efflux transporter;

Citations & Related Records

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