Fatty acid ester surfactants Cremophor EL and Solutol H S I 5 were described earlier as modulators of multidrug resistance mediated by MDR I P-glycoprotein (Pgp). We have shown that the most active components of these polydisperse surfactants are fatty acid-polyethylene glycol-fatty acid diesters (F
Automated analysis of polyethylene glycol-induced inhibition of P-glycoprotein activity in vitro
โ Scribed by Erin D. Hugger; Clayton J. Cole; Thomas J. Raub; Philip S. Burton; Ronald T. Borchardt
- Publisher
- John Wiley and Sons
- Year
- 2003
- Tongue
- English
- Weight
- 89 KB
- Volume
- 92
- Category
- Article
- ISSN
- 0022-3549
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โฆ Synopsis
Previous studies in our laboratories have shown that commonly used polyethoxylated pharmaceutical excipients inhibit P-glycoprotein activity in cell culture models of the intestinal mucosa. The results presented in this technical note show that the TECAN Genesis robotic workstation can be utilized to automate cellular transport studies for evaluating excipient effects on P-glycoprotein activity in vitro and for estimating the permeation of drug-like molecules across cell monolayers.
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A series of five homodimeric polyethylene glycol (PEG) linked homodimers based on the multidrug resistance reversal agent (-)-stipiamide were made and tested for their ability to interact with P-glycoprotein, the protein responsible for multidrug resistance, using ATPase and photoaffinity displaceme
P-glycoprotein (P-gp), a multidrug resistance (MDR) protein encoded by the MDR1 gene in humans, is responsible for the efflux of structurally diverse drugs. Previous studies in our laboratory have shown that excipients such as poly(ethylene)glycol (PEG)-300, Cremophor EL, and Tween 80 inhibit P-gp a