Potential of biopartitioning micellar chromatography as an in vitro technique for predicting drug penetration across the blood–brain barrier

Application of High Performance Liquid Chromatography for the Measurements of Lipophilicity and Biomimetic Binding Properties in Drug Discovery

“…The IAM retention data of drugs were used to estimate brain to blood partition [88] and compound permeation through the intestinal wall [89]. There are several publications [90][91][92][93] about the use of bio-partitioning micellar chromatographic retention to mimic biological in vivo distribution processes. However, when the physico-chemical or bio-mimetic models are applied for the estimation of compounds in vivo behaviour it is very important to keep in mind the limitations of such models.…”

Biopartitioning micellar chromatography separation methods: modelling quantitative retention–activity relationships of cephalosporins

“…In all cases, the equations and statistics for the QRAR models were adjusted to the format recommended by Sagrado and Cronin (Balon et al, 1999;Molero-Monfort et al, 2001;Escuder-Gilabert et al, 2004). Data can be fitted to a second-order polynomial model, see Fig.…”

Mixed micellar liquid chromatography methods: modelling quantitative retention–activity relationships of angiotensin converting enzyme inhibitors

“…Table 5 summarizes the statistical analysis of the second-order polynomial models using BMC Brij35 and BMC Brij35:SDS=85:15 systems. In all cases, the equations and statistics for the QRAR models are adjusted to the format recommended by Sagrado and Cronin (Balon et al, 1999;Molero-Monfort et al, 2001;Escuder-Gilabert et al, 2004). The p-values were less than 0.01, which indicated that there were statistically significant relationships between these parameters and log K values obtained in the BMC Brij35 and BMC Brij35:SDS=85:15 systems at the 99% confidence level, for V d , CL and IC50 models with mixed micellar solution at pH 6.5 and 7.4 and the T 1/2 model with the same mobile phase at pH 7.4; the p-values were less than for those models with pure Brij35 solution.…”

“…With amphipathic properties and the capability to mimic the biomembrane, surfactants with unique structures are often used in the field of drug separation and evaluation of drug membranetransport. Biopartitioning micellar chromatography (BMC), an MLC system optimized in order to describe the biological behavior of drugs, comprises a hydrophobic stationary phase and saline solutions of Brij35 micelles as mobile phase, and has been shown to be useful for describing and predicting the biological activities of different pharmacological kinds of drugs (Quiñones-Torrelo et al, 1999Escuder-Gilabert et al, 2000), and permeability across the intestinal barrier (Balon et al, 1999;Molero-Monfort et al, 2001), blood-brain barrier and cornea (Escuder-Gilabert et al, 2004).…”