ArticleEuropean journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V2010
Commonly used nonionic surfactants interact differently with the human efflux transporters ABCB1 (p-glycoprotein) and ABCC2 (MRP2).
Article in European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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22 citing papers in PubMed, 92 citations in OpenAlex.
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- Surfactant-Enabled Nanocarriers in Breast Cancer Therapy: Targeted Delivery and Multidrug Resistance Reversal.Pharmaceutics · 2025Review
- Preparation and Evaluation of a Self-Emulsifying Drug Delivery System for Improving the Solubility and Permeability of Ticagrelor.ACS omega · 2024Article
- Safety and efficacy of a feed additive consisting of glyceryl polyethyleneglycol ricinoleate (PEG castor oil) for all animal species (FEFANA asbl).EFSA journal. European Food Safety Authority · 2022Article
- A Critical Overview of the Biological Effects of Excipients (Part I): Impact on Gastrointestinal Absorption.The AAPS journal · 2022Review
- Non-ionic Surfactants as a P-Glycoprotein(P-gp) Efflux Inhibitor for Optimal Drug Delivery-A Concise Outlook.AAPS PharmSciTech · 2022Review
- Functional Excipients and Novel Drug Delivery Scenario in Self-nanoemulsifying Drug Delivery System: A Critical Note.Pharmaceutical nanotechnology · 2022Review
- Effects of self-assembled cell-penetrating peptides and their nano-complexes on ABCB1 expression and activity.Iranian journal of basic medical sciences · 2021Article
- Article
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- Temperature Effect on the Adsorption and Volumetric Properties of Aqueous Solutions of KolliphorMolecules (Basel, Switzerland) · 2020Article
- Development and in vitro Evaluation of Gastro-protective Aceclofenac-loaded Self-emulsifying Drug Delivery System.International journal of nanomedicine · 2020Article
- Development and Evaluation of Poorly Water-Soluble Celecoxib as Solid Dispersions Containing Nonionic Surfactants Using Fluidized-Bed Granulation.Pharmaceutics · 2019Article
- Barriers to Drug Distribution into the Perinatal and Postnatal Brain.Pharmaceutical research · 2018Review
- Using Physiologically Based Pharmacokinetic (PBPK) Modeling to Evaluate the Impact of Pharmaceutical Excipients on Oral Drug Absorption: Sensitivity Analyses.The AAPS journal · 2016Article
- The Effects of Pharmaceutical Excipients on Gastrointestinal Tract Metabolic Enzymes and Transporters-an Update.The AAPS journal · 2016Article
- Drug Delivery Innovations for Enhancing the Anticancer Potential of Vitamin E Isoforms and Their Derivatives.BioMed research international · 2015Review
- Polymers influencing transportability profile of drug.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2013Review
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6 authors at 1 institution in 1 country.
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No grant is acknowledged in the PubMed record.
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.
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