Now showing items 1-5 of 5
The Phospholipid Vesicle-Based Drug Permeability Assay: 5. Development Toward an Automated Procedure for High-Throughput Permeability Screening
(Journal article; Tidsskriftartikkel; Peer reviewed, 2009-02)
In-vitro screening for oral absorption has become an essential part of drug discovery and development. Recently, a new phospholipid vesicle-based permeation assay was developed which has shown to satisfyingly predict passive absorption of drugs in humans. The purpose of the current study was to investigate whether the assay may be further developed into a high-throughput tool by automating its ...
Drug permeability across a phospholipid vesicle-based barrier: 4. The effect of tensides, co-solvent and pH changes on barrier integrity and on drug permeability
(Journal article; Tidsskriftartikkel; Peer reviewed, 2008-07-03)
In this study the integrity of the recently developed phospholipid vesicle-based permeability barrier in the presence of a variety of co-solvents and tensides has been investigated. Also included are studies of the influence of these additives on drug permeation and the effect of pH changes on the permeability of ionogenic drug compounds. Permeability experiments using the hydrophilic model ...
Drug permeability across a phospholipid vesicle-based barrier - 2. Characterization of barrier structure, storage stability and stability towards pH changes
(Journal article; Tidsskriftartikkel; Peer reviewed, 2006-04-18)
Recently we reported on the development of a phospholipid vesicle-based barrier as a medium throughput method for screening of drug permeability. The aim of this present study is to characterize the barrier structure, including an estimation of the amount of phospholipid within it, its storage stability and its stability over various pH ranges found in different parts of the gastrointestinal tract. ...
Drug permeability across a phospholipid vesicle based barrier: A novel approach for studying passive diffusion
(Journal article; Peer reviewed; Tidsskriftartikkel, 2005-10)
The aim of this study was to develop a novel predictive medium-throughput screening method for drug permeability, with use of a tight barrier of liposomes on a filter support. To our knowledge no one has succeeded in depositing membrane barriers without the use of inert solvent such as hexadecane. The first part of the study involved development of a protocol for preparation of these barriers, which ...
Drug permeability across a phospholipid vesicle based barrier: 3. Characterization of drug-membrane interactions and the effect of agitation on the barrier integrity and on the permeability
(Journal article; Tidsskriftartikkel; Peer reviewed, 2007)
Recently, we reported on the development and structural characterization of a phospholipid vesicle based barrier useful for medium throughput screening of passive drug permeability. Here, we investigate the physical and functional integrity of the phospholipid vesicle based barriers to agitation by stirring or shaking, and whether agitation affects drug permeability of sulpiride, metoprolol and ...