pgp - publications

Predict more pgp - ligand interactions now!

1. J Microencapsul. 2012 Mar 22. [Epub ahead of print]

Dual approach utilizing self microemulsifying technique and novel P-gp inhibitor
for effective delivery of taxanes.

Chaurasiya A, Singh AK, Jain GK, Warsi MH, Sublet E, Ahmad FJ, Borchard G, Khar

Faculty of Pharmacy, Hamdard University , New Delhi 110062 , India.

In the present work, concomitant use of self-microemulsifying drug delivery
systems (SMEDDS) and a novel third-generation P-gp inhibitor, GF120918
(elacridar), for the effective transport of taxanes (paclitaxel and docetaxel)
across an in vitro model of the intestinal epithelium and uptake into tumor cells
were investigated. On the basis of solubility studies and ternary phase diagrams,
different SMEDDS formulations of taxanes were prepared and characterized. In
caco-2 cell permeation study, paclitaxel-loaded SMEDDS along with GF120918 showed
a four-fold increase in apparent permeability, while docetaxel-loaded SMEDDS in
combination with GF120918 showed a nine-fold increase in permeability, as
compared to plain drug solution. Cell uptake studies on A549 cells were performed
with microemulsions formed from both SMEDDS formulations loaded with rhodamine
123 dye and showed good uptake than plain dye solution. Confocal laser scanning
microscopic images further confirmed the higher uptake of both SMEDDS
formulations in the presence of GF120918.

PMID: 22439872 [PubMed - as supplied by publisher]