Adeboye Adejare
University of the Sciences in Philadelphia, USA
Title: Immobilized artificial membrane chromatography: A useful tool for predicting membrane permeability
Biography
Biography: Adeboye Adejare
Abstract
The partitioning of structurally diverse and functionally unrelated set of 21 compounds was studied on immobilized artificial membranes (IAM) column using high performance liquid chromatography (HPLC). The aqueous capacity factors (log KIAMW) of the compounds were correlated with their logarithms of octanol/water partition coefficient (log P) and blood/brain partition coefficient (log BB) to determine whether molecular binding on IAM columns can predict permeability of drugs through biological membranes such as intestinal membrane and blood brain barrier. Good correlation was obtained between log KIAMW and log P of the compounds. Log KIAMW values of the compounds also showed an acceptable correlation with log BB. Inclusion of the molecular size with the log P or log KIAMW data had a negative effect on correlations when the data was re-plotted vs. log BB values. For a subset of 8 compounds, log KIAMW showed better correlation with log % of human absorption than did log P. Though many in vitro physicochemical based techniques are available to predict membranes permeability, IAM.HPLC seems to be a promising tool for easy and reproducible prediction.