Data for: "High-Throughput Screening of Excipients with a Biological Effect: A Kinetic Study on the Effects of Surfactants on Efflux-Mediated Transport"

This data supports a study where, we develop and apply a high-throughput screening protocol to investigate the activities of non-ionic surfactants, with a broad range of hydrophilic-lipophilic balance values, against ABCB1- and ABCC2-mediated efflux transport. To achieve this Caco-2 cells were grown for 7 days in 96 well plates, then washed and incubated with the test materials for 2 h in the presence of 2.5 µM of either rhodamine 123 (R-123) or 5(6)-Carboxy-2’, 7’ dichlorofluorescein diacetate as probes of ABCB1 and ABCC2 respectively. Within the work we find that of the surfactants tested, no activity against ABCC2 was detected and all surfactants showing efficacy against ABCB1 had a HLB value of 22 or below. Inhibition of ABCB1 was seen in the order of efficacy to be poloxamer 335 > poloxamer 40 > Crovol A-70 > Myrj S-40 > poloxamer 184 > poloxamer 182 > Etocas 40 > Tween 20 > Etocas 29 > Tween 80 > Acconon C-44 > Span 20. With regard to this inhibition, the distribution of hydrophilic regions is more important than the HLB value.
This work demonstrates a high-throughput protocol for detecting materials that can modulate ABCB1-mediated efflux. These surfactants could be exploited to improve oral delivery of drugs prone to efflux.

The data included in this data set is represented in two figures:
Figure 1. The IC50 curves of inhibitors of efflux proteins, showing activity against A) ABCB1 and B) ABCC2. Caco-2 cells were grown for 5-7 days on 96-well plates prior to experimentation. Data presented as each of a minimum of 4 replicates from 2.5 μM initial extracellular concentration of either R-123 or CDFDA as probes of ABCB1 and ABCC2 activity respectively.

Figure 2. Percentage inhibition curves of various surfactants against ABCB1 showing A) Poloxamer 182, B) Span 20, C) Crovol A70, D) Etocas 29, E) Poloxamer 184, F) Etocas 40, G) Acconon C44, H) Tween 80, I) Tween 20, J) Myrj S40, K) Poloxamer 407 and L) Poloxamer 335. Sigmoidal curves were constructed from 4 different passage numbers on confluent Caco-2 monolayers grown on 96 well plates for 5-7 days and are shown pooled from a minimum of 4 replicates per concentration. Data presented as a function of overall R-123 uptake for ABCB1 with initial conditions of 2.5 µM extracellular tracer dye per well, with excipient-free control wells set to 100 % transporter activity.