0000000000180936
AUTHOR
R.m. Villanueva-camañas
Micellar liquid chromatography for prediction of drug transport.
Abstract The vast majority of well absorbed drugs are transported passively across the cell membranes. Physicochemical descriptors of drug molecules that are believed to influence transcellular transport are routinely used to predict drug absorption by means of complex mathematical models. In this paper, a new in vitro method, based on the retention data in micellar liquid chromatography (MLC), is validated for the prediction of passive drug absorption. The retention of a heterogeneous drugs set in MLC using Brij 35 as surfactant in the mobile phase is compared with the retention data reported in literature obtained in red cell membrane lipid liposomes, human red cell membranes vesicles (ve…
Biopartitioning micellar chromatography: an in vitro technique for predicting human drug absorption.
The main oral drug absorption barriers are fluid cell membranes and generally drugs are absorbed by a passive diffusion mechanism. Biopartitioning micellar chromatography (BMC) is a mode of micellar liquid chromatography that uses micellar mobile phases of Brij35 under adequate experimental conditions and can be useful to mimic the drug partitioning process in biological systems. In this paper the usefulness of BMC for predicting oral drug absorption in humans is demonstrated. A hyperbolic model has been obtained using the retention data of a heterogeneous set of 74 compounds, which shows predictive ability for drugs absorbed by passive diffusion. The model obtained in BMC is compared with …
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
The distribution of tricyclic antidepressants from plasma to brain, where these drugs exert their main clinical action, and other organs is related to transport events across the cell membranes of the different tissues. It could be expected that all the molecular features that condition the transport processes (mainly hydrophobicity and molar total charge) also control the pharmacokinetic and biochemical behavior. Micellar liquid chromatography (MLC) has been proposed to emulate in vitro the partitioning process in the biomembranes. The use of micellar solutions of Brij35 as mobile phases in reversed-phase liquid chromatography has proven to be valid to predict the biological activities of …
Retention–property relationships of anticonvulsant drugs by biopartitioning micellar chromatography
Epilepsy may be considered as a group of disorders with only one thing in common: the fact that recurrent anomalous electrochemical phenomena appear in the central nervous system. Different classes of drugs are included under the generic term of anticonvulsant drugs. All of them work by decreasing discharge propagation in different ways. Biopartitioning micellar chromatography (BMC) is a mode of reversed-phase liquid chromatography, which can be used as an in vitro system to model the biopartitioning process of drugs when there are no active processes. In this paper, relationships between the BMC retention data of anticonvulsant drugs, their pharmacokinetics (oral absorption, protein bindin…
Potential of biopartitioning micellar chromatography as an in vitro technique for predicting drug penetration across the blood–brain barrier
The blood-brain barrier (BBB) is considered to be the main barrier to drug transport into the central nervous system (CNS). The BBB restricts the passive diffusion of many drugs from blood to brain. The ease with which any particular drug diffuses across the BBB is determined largely by the molecular features of drugs, and it is therefore possible to predict the BBB permeability of a drug from its molecular structure. Biopartitioning micellar chromatography (BMC), a mode of micellar liquid chromatography that uses micellar mobile phases of Brij35 in adequate experimental conditions, can be useful in mimicking the drug partitioning process into biological systems. Retention in BMC depends on…