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Taillardat-Bertschinger, Agnes; Martinet, Catherine a Marca; Carrupt, Pierre‐Alain; Reist, Marianne; Caron, Giulia; Fruttero, Roberta; Testa, Bernard

doi:10.1023/a:1016156927420

Cited by 97 publications

(43 citation statements)

References 17 publications

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“…IAM chromatography has been evaluated as a permeability screen method [16][17][18][19][20][21]. However, the relatively weaker electrostatic interactions and single layer structure of phospholipids limited its applications in some cases.…”

Section: Introductionmentioning

confidence: 99%

A method for rapidly predicting drug tissue distribution using surfactant vesicle electrokinetic chromatography

2008

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Lung tissue distribution of an inhaled drug is important for its potency in the airways and with minimum systemic effects within its dose range. As the lung has the smallest diffusion distance of all the organs in the body and negligible diffusion delays, the characteristics of drug distribution in the lung will mainly depend on drug binding to both tissue and plasma protein. This research aims to develop and evaluate surfactant vesicle electrokinetic chromatography (SEKC) methods for high throughput profile prediction of tissue distribution for inhaled drugs. Several electrokinetic chromatography methods reported in the literature, as well as immobilised artificial membrane chromatography, were compared and evaluated in respect to chromatographic characteristics and statistical correlations. Among these methods, the docusate sodium salt (AOT) SEKC system showed good reproducibility, short run time, and the highest selectivity for alkylphenone test compounds. It also showed a significant statistical correlation between the retention of inhaled drugs and their in vivo volume of distribution at steady-state (V(ss)) in whole human body neglecting the plasma protein-binding differences. Stronger correlations were observed between the AOT SEKC retention of a series of basic drugs and their rat lung tissue-to-plasma water partitioning coefficient (K(pu)), which is affected only by drug binding to the tissue constituent. Further, on comparing correlations between AOT SEKC retention and K(pu) at various rat tissues, it was observed that the strongest correlation was with lung tissue distribution, while the weakest was with brain tissue distribution.

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Section: Introductionmentioning

confidence: 99%

A method for rapidly predicting drug tissue distribution using surfactant vesicle electrokinetic chromatography

2008

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“…Thus, the development of membrane-like systems such as liposome/H 2 O partitioning systems [17] [18] has been of marked interest to obtain lipophilicity parameters of greater biologic relevance, especially for ionized compounds. However, the determination of drug partitioning in liposome/H 2 O systems is time-consuming and tedious, and, therefore, of little use in medium or high-throughput screening in drug discovery.…”

mentioning

confidence: 99%

“…As surrogates, immobilized artificial membrane (IAM) chromatography [18 -21] and immobilized liposome chromatography (ILC) [22 -24] were recently developed as convenient and rapid methods for the analysis of drug -membrane interactions. However, it was shown for a set of structurally unrelated compounds that IAM retention and liposome/H 2 O partitioning are governed by a different balance of intermolecular interactions, and, thus, the lipophilicity index from IAM retention is not exchangeable with that from liposome/H 2 O partitioning for structurally unrelated compounds [18] [25].…”

mentioning

confidence: 99%

Drug–Membrane Interaction on Immobilized Liposome Chromatography Compared to Immobilized Artificial Membrane (IAM), Liposome/Water, and Octan‐1‐ol/Water Systems

Liu

Fan

Chen

et al. 2010

Helvetica Chimica Acta

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The objective of this study was to investigate drug -membrane interaction by immobilized liposome chromatography (ILC; expressed as lipophilicity index log K s ) and the comparison with lipophilicity indices obtained by liposome/H 2 O, octan-1-ol/H 2 O, and immobilized artificial membrane (IAM) systems. A set of structurally diverse monofunctional compounds and drugs (nonsteroidal antiinflammatory drugs and b-blockers) were selected in this study. This set of solutes consists of basic or acidic functionalities which are positively or negatively charged at physiological pH 7.4. No correlation was found between log K s from ILC and lipophilicity indices from any of the other membrane model systems for the whole set of compounds. For structurally related compounds, significant correlations could be established between log K s from ILC and lipophilicity indices from IAM chromatography and octan-1-ol/H 2 O. However, ILC and liposome/H 2 O systems only yield parallel partitioning information for structurally related large molecules. For hydrophilic compounds, the balance between electrostatic and hydrophobic interactions dominating drug partitioning is different in these two systems.

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“…Using Eq. (6) for cations, it is advisable to employ the effective mobility (m eff, aq ) of the cations in a buffer solution containing surfactant monomers below the critical micelle concentration (CMC) to compensate for eventual ion-pair interaction [32,42].…”

Section: Equationsmentioning

confidence: 99%

“…The influence of the micelles on the ionic strength, the dielectric constant and the viscosity are regarded as negligible and it is also assumed that an interaction between analyte and micelle monomer does not occur. TaillardatBertschinger et al [42] suggest that instead of using the effective mobility in pure buffer solution, the surfactant should be added to the buffer but kept below the CMC. The overall effective mobility will then be corrected both for the compound's own mobility and for the occurrence -, SAL did not reach the detection window in experiments N17 and N19 since the analysis time was too short.…”

Section: Additional Experiments To Study the Effective Mobility Of Thmentioning

confidence: 99%

Microemulsion electrokinetic chromatography of drugs varying in charge and hydrophobicity: I. Impact of parameters on separation performance evaluated by multiple linear regression models

et al. 2004

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The separation of anionic, cationic and neutral drugs in microemulsion electrokinetic chromatography (MEEKC) was studied with a statistical experimental design. The concentration of sodium dodecyl sulfate (SDS, surfactant), 1-butanol (co-surfactant) and borate buffer and the factors Brij 35 (surfactant), 2-propanol (organic solvent) and cassette temperature were varied simultaneously, while the parameters pH (9.2), the concentration of octane (oil, 0.8% w/w), the voltage (10 kV) and the dimension of the fused-silica capillary, were kept constant. Eight different model substances were chosen with different hydrophobicities. Two of the analytes were positively charged, two were negatively charged, and the remaining four were neutral or close to neutral at the pH explored. The importance of each parameter on the separation window, the plate height and the retention factor for each of the analytes was studied by means of multiple linear regression (MLR) models. A new response was evaluated for anions, the quotient between the effective mobility in the microemulsion and the effective mobility in the corresponding buffer. Factors affecting selectivity changes were also explored, and it was found that SDS and 2-propanol had the largest effect on selectivity.

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Cited by 97 publications

References 17 publications

A method for rapidly predicting drug tissue distribution using surfactant vesicle electrokinetic chromatography

A method for rapidly predicting drug tissue distribution using surfactant vesicle electrokinetic chromatography

Drug–Membrane Interaction on Immobilized Liposome Chromatography Compared to Immobilized Artificial Membrane (IAM), Liposome/Water, and Octan‐1‐ol/Water Systems

Microemulsion electrokinetic chromatography of drugs varying in charge and hydrophobicity: I. Impact of parameters on separation performance evaluated by multiple linear regression models

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