Immobilized artificial membranes - Screens for drug membrane interactions

被引:87
作者
Yang, CY [1 ]
Cai, SJ [1 ]
Liu, HL [1 ]
Pidgeon, C [1 ]
机构
[1] PURDUE UNIV, SCH PHARM, DEPT MED CHEM & MOL PHARMACOL, W LAFAYETTE, IN 47907 USA
关键词
permeability; bioavailability; partitioning coefficient; hydrophobicity parameter; pharmacokinetics; chromatography; IAM; passive transport; diffusion; drug screen; in vitro model;
D O I
10.1016/S0169-409X(96)00438-3
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Immobilized Artificial Membranes (IAMs) are monolayers of phospholipid analogs covalently bonded to the surface of silica particles. P-31 NMR and molecular dynamics (MD) simulations demonstrated that IAMs and liposome membranes exhibit similar interfacial properties. These similar interfacial properties have resulted in IAMs' being useful as a physico-chemical model of drug-membrane partitioning. IAM chromatography has been successful used to predict: (1) solute partitioning into liposome membranes; (2) drug permeability through Caco-2 cells; (3) drug intestinal absorption; (4) brain uptake of amino acids; (5) bile salt-membrane interactions; and (6) human skin permeability of steroids and alcohols. In addition, IAM chromatography has also been used to obtain hydrophobicity parameters for SAR studies.
引用
收藏
页码:229 / 256
页数:28
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