Chromatographic surfaces prepared from lyso phosphatidylcholine ligands

Rhee, Dong Mi; Markovich, Robert J.; Chae, Whi-Gun; Qiu, Xiaoxing; Pidgeon, Charles

doi:10.1016/0003-2670(94)00260-6

Cited by 34 publications

(23 citation statements)

References 11 publications

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“…Importantly, however, the POPC/PS liposomes, which are more tedious to prepare and have a shorter shelf life than surfactant vesicles, did not offer a better correlation between log k and log Caco-2 permeability than CTAB/SOS vesicles. In an effort to develop new and rapid methods for the estimation of drug intestinal permeability, over the past 10 years, HPLC columns incorporating immobilized artificial membranes (IAMs) have been developed [37][38][39][40][41]. IAM columns consist of chromatographic surfaces prepared by covalently bonding phospholipid molecules to solid surfaces at monolayer type densities.…”

Section: Structurally Diverse Compoundsmentioning

confidence: 99%

Investigation of vesicle electrokinetic chromatography as an in vitro assay for the estimation of intestinal permeability of pharmaceutical drug candidates

2006

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As the pharmaceutical industry continues the daunting search for novel drug candidates, there remains a need for rapid screening methods not only for biological activity, but for physiochemical properties as well. It is invaluable that adequate model systems for absorption and/or bioavailability be developed early in the drug evaluation process to avoid the loss of promising compounds late in development. The focus of this paper is the use of vesicle EKC (VEKC) as a high-throughput, easy, cost-effective, and predictive model for the passive transcellular diffusion of drug candidates in the intestinal epithelium. Vesicles are large aggregates of molecules containing a spherical bilayer structure encapsulating an internal cavity of solvent. It is this bilayer structure that makes vesicles attractive as model membranes. In this study, vesicles were synthesized from both phospholipids and surfactant aggregates, and then employed as pseudostationary phases in EKC (VEKC). The interaction of drug molecules with vesicles in EKC was then used as the basis for an in vitro assay to evaluate passive diffusion. The VEKC technique showed a statistical correlation between the retention of drug candidates using surfactant and phospholipid vesicles and passive diffusion data (log Pow and colon adenocarcinoma). VEKC analysis offers high-throughput capabilities due to the short run times, low sample, and solvent volumes necessary, as well as instrument automation. However, due to the complexity of drug absorption in the intestine, difficulty arises when a single in vitro model is used to predict in vivo absorption characteristics. Therefore, the retention of drug candidates using VEKC in conjunction with other permeability prediction methods can provide a primary screen for a large number of drug candidates early in the drug discovery process with minimal resources.

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Section: Structurally Diverse Compoundsmentioning

confidence: 99%

Investigation of vesicle electrokinetic chromatography as an in vitro assay for the estimation of intestinal permeability of pharmaceutical drug candidates

2006

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“…The use of methanol as organic modifier is avoided, since it affects the stability of the column, leading to methanolysis of the phospholipids. Nevertheless, the ageing of the column should be checked from time to time using standard compounds 163–165…”

Section: Immobilised Artificial Membrane Chromatographymentioning

confidence: 99%

Alternative Measures of Lipophilicity: From Octanol–Water Partitioning to IAM Retention

Giaginis

Tsantili‐Kakoulidou

2008

Journal of Pharmaceutical Sciences

134

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“…A single-chain phosphatidylcholine functionalized silica column with the commercial name IAM.PC.DD was also prepared through the reaction between 11-carboxylundecylphosphocholine and propylamine functionalized silica to increase the surface density of phospholipids and stability under acidic conditions [10]. However, the unreacted silanol groups and residual amino groups still exist on end-capped IAM surfaces [8,11], which could elicit silanophilic interactions and hydrolysis of amide bonds. The preparation processes is not trivial and is laborious [3,10,12], which limited their application for self-lab preparation.…”

Section: Introductionmentioning

confidence: 99%

Preparation of a biomimetic polyphosphorylcholine monolithic column for immobilized artificial membrane chromatography

Zhao

Chen

Zhou

et al. 2015

Journal of Chromatography A

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Chromatographic surfaces prepared from lyso phosphatidylcholine ligands

Cited by 34 publications

References 11 publications

Investigation of vesicle electrokinetic chromatography as an in vitro assay for the estimation of intestinal permeability of pharmaceutical drug candidates

Investigation of vesicle electrokinetic chromatography as an in vitro assay for the estimation of intestinal permeability of pharmaceutical drug candidates

Alternative Measures of Lipophilicity: From Octanol–Water Partitioning to IAM Retention

Preparation of a biomimetic polyphosphorylcholine monolithic column for immobilized artificial membrane chromatography

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