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Journal of Biomolecular Screening
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Rapid Screening of Blood-Brain Barrier Penetration of Drugs Using the Immobilized Artificial Membrane Phosphatidylcholine Column Chromatography

Chi Ho Yoon

College of Pharmacy, Sungkyunkwan University, Gyeonggi-do, Korea

Soo Jin Kim

C&C Research Laboratories, Gyeonggi-do, Korea

Beom Soo Shin

Kang Choon Lee

College of Pharmacy, Sungkyunkwan University, Gyeonggi-do, Korea

Sun Dong Yoo

College of Pharmacy, Sungkyunkwan University, 300 Cheoncheon-dong, Jangan-gu, Suwon, Gyeonggi-do, 440-746, Korea; sdyoo{at}skku.ac.kr

The chromatographic capacity factors (kIAM) of 23 structurally diverse drugs were measured by the immobilized artificial membrane (kIAM) phosphatidylcholine chromatography for the prediction of blood-brain barrier (BBB) penetration. The kIAM was determined using themobile phase consisting of acetonitrile:DPBS (20:80 v/v) and corrected for the molar volume of the solutes (kIAM/MWn). The correlation between kIAM/MWn and CNS penetration was highest when measured at pH 5.5 with the power function of n = 4. This in vitro predictionmethod was validated with 7 newly synthesized PDE-4 inhibitors. The relationship between in vivo plasma-to-brain concentration ratios and in vitro CNS penetration was excellent (r= 0.959). The developed in vitro prediction method may be used as a rapid screening tool for BBB penetration of drugs with passive transport mechanism, with high success, low cost, and reproducibility.

Key Words: immobilized artificial membrane • blood-brain barrier • CNS penetration • high-throughput screening

This version was published on February 1, 2006

Journal of Biomolecular Screening, Vol. 11, No. 1, 13-20 (2006)
DOI: 10.1177/1087057105281656
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