Related Experiment Video
Updated: May 13, 2026

Expression, Detergent Solubilization, and Purification of a Membrane Transporter, the MexB Multidrug Resistance Protein
Published on: December 3, 2010
Interactions between human multidrug resistance related protein (MRP2; ABCC2) and excipients commonly used in
Liang Li1, Tao Yi, Christopher Wai-kei Lam
1State Key Laboratory for Quality Research in Chinese Medicine, Macau Institute for Applied Research in Medicine and Health, Macau University of Science and Technology, Taipa, Macau. LL726nj@gmail.com
Abstract:
The aim of this study was to investigate the multidrug resistance related protein-2 (MRP2) inhibition effect of excipients commonly employed in the formulation of self-emulsifying drug delivery systems (SEDDS). Cytotoxicity and safe dosages of fifteen excipients, including five surfactants, three oils, three co-surfactants and four solid carriers, were compared using MTT assay. Caco-2 cell permeability and MRP2 vesicles transport assays were used in the inhibition analysis. Scutellarin was shown to be a substrate of MRP2 and used as a probe in the inhibition assay. Twelve excipients decreased efflux ratio of scutellarin in Caco-2 model, among them six excipients showed inhibition effect on MRP2 in MRP2 transport model. In Caco-2 model, Cremophor EL, Maisine 35-1, PEG 2000 and β-cyclodextrin reduced efflux ratio of scutellarin the most in the four different excipients groups. The efflux reduction mechanism was further validated by MRP2 transport assay in inhibiting MRP2 activity in Cremophor EL and PEG 2000. It is suggested that scutellarin quantified by LC-MS can be used as a model drug for MRP2 inhibition analysis using Caco-2 permeability and vesicles transport analyses. Together they constitute a sensitive and rapid screening method for assessing interactions between excipients and MRP2 in SEDDS formulation.
Related Concept Videos
Drug Delivery Systems: Different Types
Modified-Release Drug Delivery Systems: Bioavailability
Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters
Modified-Release Drug Delivery Systems: Overview
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
Carrier-Mediated Transport
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
