Transepithelial Transport of Prodrugs of the HIV Protease Inhibitors Saquinavir, Indinavir, and Nelfinavir Across Caco-2 Cell Monolayers

@article{Rouquayrol2004TransepithelialTO,
  title={Transepithelial Transport of Prodrugs of the HIV Protease Inhibitors Saquinavir, Indinavir, and Nelfinavir Across Caco-2 Cell Monolayers},
  author={M. Rouquayrol and B. Gaucher and D. Roche and J. Greiner and P. Vierling},
  journal={Pharmaceutical Research},
  year={2004},
  volume={19},
  pages={1704-1712}
}
AbstractPurpose. This study is dedicated to the permeation of various amino acid-, D-glucose-, and PEG-conjugates of indinavir, saquinavir, and nelfinavir across monolayers of Caco-2 cells as models of the intestinal barrier. This screening is aimed at detecting the most promising prodrugs for improving the intestinal absorption of these protease inhibitors. Methods. The bidirectional transport of the prodrugs was investigated using P-gp-expressing Caco-2 monolayers grown on membrane inserts… Expand
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References

SHOWING 1-10 OF 22 REFERENCES
The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors.
Comparison of the Disposition of Ester Prodrugs of the Antiviral Agent 9-(2-phosphonylmethoxyethyl)adenine [PMEA] in Caco-2 Monolayers
Synthesis and Anti-HIV Activity of Prodrugs Derived from Saquinavir and Indinavir
USE OF CACO-2 CELLS AS AN IN VITRO INTESTINAL ABSORPTION AND METABOLISM MODEL
Age-dependent Expression of P-Glycoprotein gp17O in Caco-2 Cell Monolayers
Investigation of distribution, transport and uptake of anti-HIV drugs to the central nervous system.
  • Sawchuk, Yang
  • Biology, Medicine
  • Advanced drug delivery reviews
  • 1999
...
1
2
3
...