Profiling drug membrane permeability and activity via biopartitioning chromatography

Drug in vivo pharmacokinetic performances in nature consist of sequential membrane transporting processes and are based on the entry into and exit of drugs from cell, even for metabolism process requiring parent drugs delivered into and metabolites effluxed from the metabolizing cells. Efficient and reliable high throughput screen of membrane permeability properties as early as possible in drug discovery and development program is accordingly desirable. Biopartitioning chromatography (BPC) introduces biomembrane-mimetic structures (such as liposome, phospholipid monolayer, micelle, microemulsion, vesicle and bicelle, etc) into chromatographic system, i.e. liquid system or capillary electrophoresis, and thereby emulates drug-membrane interactions difficult to study in the liquid state by well reproducible, rapid, sensitive and adequately designed chromatographic technique. And recently BPC has been becoming a high-throughput screening platform for drug membrane permeability and biological activity. The theoretical basis, classification and application of BPC were summarized based on the latest advances and our recent works. The development potential and perspectives of this field were also discussed.