UV-DIB: label-free permeability determination using droplet interface bilayers

Abstract

Label-free permeability measurement in droplet interface bilayers to assess the relationship between bilayer lipid composition and permeant chemical structure.

Label-free quantification of passive membrane permeability of cyclic peptides across lipid bilayers: penetration speed of cyclosporin A across lipid bilayers

“…R. Strutt and coworkers measured the lipid bilayer permeability using their permeability assay based on DIB of DOPC and a UV detector. 17 In this assay, a lipid bilayer is formed at the droplet interface and the permeability of an analyte is determined based on the UV absorbance of the analyte. In their report, the permeability coefficient of caffeine was determined to be 2.81 ± 0.0920 × 10 −4 cm s −1 .…”

Open microfluidics: droplet microarrays as next generation multiwell plates for high throughput screening

“…57 2D and 3D networks of droplets can thereby be assembled through controlled deposition and arrangement of lipid coated droplets. 58,59 Membrane permeable compounds can pass passively through the bilayer by diffusion, 26,60 or through integrated membrane pores. 27 Krishna Kumar et al report a hydrogel dropletbased method to arrange bacterial communities.…”

Liposomal Permeation Assay for Droplet-Scale Pharmacokinetic Screening

“…Neither transwell assay is particularly convenient for ultrahigh-throughput screening, but they have been deployed on the scale of conventional compound collections because knowledge of membrane permeability is critical for further development . Recent innovative permeation measurement technology development has included fluorogenic copper-catalyzed azide alkyne cycloaddition (CuAAC), liposomal dye displacement or LC-MS liposome pulldown, − droplet-interface bilayer (DIB) permeation assay, , black lipid membrane (BLM) label-free penetration assay, or cellular chloroalkane penetration assay (CAPA). , Although all of these approaches can measure the permeation of bRo5 molecules individually, none are amenable to screening large split-and-pool combinatorial libraries (>10 4 members), which are the source of most bRo5 chemical matter.…”