Related Experiment Video
Updated: Jun 11, 2026

A Proteoliposome-Based Efflux Assay to Determine Single-molecule Properties of Cl- Channels and Transporters
Published on: April 20, 2015
Commonly used nonionic surfactants interact differently with the human efflux transporters ABCB1 (p-glycoprotein) and
Ulrike Hanke1, Karen May, Veronika Rozehnal
1Institute of Pharmacy, Department of Biopharmaceutics and Pharmaceutical Technology, University of Greifswald, Greifswald, Germany. ulrike.hanke@uni-greifswald.de
Abstract:
The efflux transporters ABCB1 (p-glycoprotein) and ABCC2 (MRP2) play an essential role in the limitation of oral bioavailability of drugs. In the last years, pharmaceutical surfactants like cremophor® EL or polysorbate 80 have been shown to interact with ABCB1. However, the knowledge about their influence on ABCC2 is still limited. In this study, the interactions of the nonionic surfactants cremophor® EL, cremophor® RH 40, polysorbate 80, vitamin E TPGS 1000, pluronic® PE 10300 and sucrose ester L-1695 with both efflux transporters were investigated on cellular level. Cell accumulation studies and transport studies were performed using transfected MDCK II cell models. The influence of ABCC2 inhibiting surfactants on the expression level of ABCC2 was also studied. The investigations showed that cremophor® EL, vitamin E TPGS 1000 and higher concentrations of polysorbate 80 inhibit both transporters. Pluronic® PE 10300 and sucrose ester L-1695 inhibit ABCB1 but not ABCC2. Cremophor® RH 40 only shows inhibitory activity on ABCC2. During the investigated incubation period none of the inhibiting surfactants caused an alteration in ABCC2mRNA or protein expression. These findings indicate that the observed interactions are caused by specific inhibition of the transport activity of ABCC2.
Related Concept Videos
Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters
Hepatic Drug Clearance: Role of Transporters
Carrier-Mediated Transport
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
ABC Transporters: Exporter
Pore Transport and Ion-Pair Transport
Pore transport, also known as convective transport, is a process where small molecules like urea, water, and sugars rapidly cross cell membranes as though there were channels or pores in the membrane. Although direct microscopic evidence is limited but the concept of pores or channels is widely accepted based on physiological evidence. Despite the lack of direct microscopic...
Drug Absorption Mechanism: Carrier-Mediated Membrane Transport
Facilitated diffusion is a passive process that utilizes human Solute Carrier (SLC) transporters. These transporters bind to the drug, undergo structural...

