Back to the Top
Dear Members:
Does anybody know if Tween 80 has any effect on the Pgp at low
concentrations (1%) when used as a dosing vehicle in preclinical
species. There is a report published indicating that it inhibits the
Pgp ATPase activity.
Thanks,
Azher
Back to the Top
The following message was posted to: PharmPK
Dear Azher,
yes, it does! You'll find lots of Literature on the effect of common
pharmaceutical excipients (like Tween) on Efflux transporters (like
Pgp),
which is mostly discussed as alteration of the membrane fluidity by the
excipients, e.g.:
A comparison of commonly used polyethoxylated pharmaceutical
excipients on
their ability to inhibit P-glycoprotein activity in vitro.
J Pharm Sci. 2002 Sep;91(9):1991-2002.
Nerurkar, Ho PS, Burton TJ, Vidmar RT. 1997. Mechanistic roles of
neutral
surfactants on concurrent polarized and passive membrane transport of a
model peptide in Caco-2 cells. J Pharm Sci 86:813-821.
Woodcock DM, Jefferson S, Linsenmeyer ME, Crowther PJ, Chojnowski GM,
Williams B, Bertoncello I. 1990. Reversal of multidrug resistance
phenotype with Cremophor EL, a common vehicle for water-insoluble
vitamins
and drugs. Cancer Res 50:4199-4203.
and many more...
best regards,
Philip
*************************************
Philip Lienau
Schering AG
Research Pharmacokinetics
Tel.: +49 - 30 - 468 - 18507
Fax: +49 - 30 - 468 - 12238
Back to the Top
The following message was posted to: PharmPK
Dear Azher:
Another good reference to add to those given by Phillip Lienau is:
Effects of nonionic surfactants on membrane transporters in Caco-2 cell
monolayers
Rege, B.D., Kao, J.P.Y., Polli, J.E., Eu. J. Pharm. Sci. 2002 Vol
16(4-5):237-246.
This reference shows Caco-2 results for Tween 80, Chremophor EL and
Vitamin E TPGS.
Nancy E. Kinkade, Ph.D.
Pharmaceutical Excipients Technical Service
Eastman Chemical Company
Kingsport, TN 37660
Tel: 423-229-4898
Fax: 423-224-0414
PharmPK Discussion List Archive Index page
Copyright 1995-2010 David W. A. Bourne (david@boomer.org)