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Biopartitioning Micellar Chromatography-Partition Coefficient Micelle/Water as a Potential Descriptor for Hydrophobicity in Prediction of Oral Drug Absorption

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2012
Authors
Čudina, Olivera
Marković, Bojan
Karljiković-Rajić, Katarina
Vladimirov, Sote
Article (Published version)
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Abstract
Biopartitioning micellar chromatography (BMC), which is useful to mimic the drug partitioning process in biological systems, was used as a method for determination of partition coefficients micelle/water (P-m/w) of a set of structurally diverse drugs. BMC is a chromatographic system consisting of polyoxyethylene (23) lauryl ether (Brij 35) micellar mobile phase prepared in physiological conditions and C-18 reversed stationary phase. The retention factors were determined for all selected and studied compounds and a correlation between P-m/w and oral drug absorption values were obtained. In order to study the similarity between the BMC system and other natural systems of biomembranes, the retention data on BMC were compared with permeability data obtained in Parallel artificial membrane permeation assays (PAMPA lipid model). Molecular descriptors that are believed to influence trans-cellular transport and oral drug absorption have been calculated in order to obtain a predictive and relia...ble model for drug permeability. Results presented in this paper indicate that a proposed descriptor for hydrophobicity P-m/w, provided, from a statistical point of view, is a better model than other hydrophobicity descriptors.

Keywords:
Biopartitioning micellar chromatography / Oral absorption / Partition coefficient
Source:
Analytical Letters, 2012, 45, 7, 677-688
Publisher:
  • Taylor & Francis Inc, Philadelphia
Projects:
  • Development of molecules with antiinflammatory and cardioprotective activity: structural modifications, modelling, physicochemical characterization and formulation investigations (RS-172041)

DOI: 10.1080/00032719.2011.653904

ISSN: 0003-2719

WoS: 000303820400004

Scopus: 2-s2.0-84861205362
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URI
http://farfar.pharmacy.bg.ac.rs/handle/123456789/1750
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Institution
Pharmacy

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