High-throughput screening of excipients with a biological effect: a kinetic study on the effects of surfactants on efflux-mediated transport

John Pollard, Ali Rajabi-Siahboomi, Raj K. S. Badhan, Afzal R. Mohammed, Yvonne Perrie

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OBJECTIVE: In this study, we develop and apply a high-throughput screening protocol to investigate the activity of non-ionic surfactants, with a broad range of hydrophilic-lipophilic balance values, against ABCB1-mediated efflux transport and ABCC2-mediated efflux transport.

METHODS: 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.

KEY FINDINGS: 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.

CONCLUSION: 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.

Original languageEnglish
Pages (from-to)889-897
Number of pages9
JournalJournal of Pharmacy and Pharmacology
Issue number6
Early online date19 Feb 2019
Publication statusPublished - 1 Jun 2019


  • caco-2
  • efflux
  • excipients
  • P-glycoprotein
  • surfacants

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