Affinity of Lipophilic Drugs to Mixed Lipid Aggregates in Simulated Gastrointestinal Fluids

Mixed lipid aggregates, comprising of bile salts and phospholipids, present in the small intestine assist drug solubilization subsequent dissolution absorption through intestinal epithelium. The increased variability their levels, observed physiologically, may create challenges not only for vivo bioavailability bioequivalence studies, but also vitro bio-predictive studies as correlations between data are always successful. current study investigated impact biorelevant media, with physiologically relevant sodium taurocholate lecithin on apparent solubility affinity lipophilic compounds a wide range physicochemical properties (drug ionization, lipophilicity, molecular weight) to mixed aggregates. Apparent media studied neutral drugs, weak bases acids were compared against phosphate buffer pH 6.5 absence these lipidic components. Presence aggregates enhanced majority use multivariate analysis identified significant parameters affecting based chemical class drug. For increasing salt concentrations and/or lipophilicity resulted greater enhancement at 24-hr. acids, effect levels depended mostly an interplay ionization.