Amino acid prodrug of quinidine: an approach to circumvent P-glycoprotein mediated cellular efflux.

@article{Patel2014AminoAP,
  title={Amino acid prodrug of quinidine: an approach to circumvent P-glycoprotein mediated cellular efflux.},
  author={Mitesh D. Patel and Nanda Kishore Mandava and Dhananjay Pal and Ashim K Mitra},
  journal={International journal of pharmaceutics},
  year={2014},
  volume={464 1-2},
  pages={196-204}
}
In the present study, we investigated the effect of large neutral amino acid modification in overcoming P-gp mediated cellular efflux of quinidine. L-isoleucine ester prodrug of quinidine (Ile-quinidine) was synthesized in our laboratory. [14C]-erythromycin was selected as a model substrate to study interaction of quinidine and Ile-quinidine with P-gp. Transport studies were conducted to study translocation kinetics of quinidine and Ile-quinidine in MDCK-MDR1 cells. In cellular accumulation… CONTINUE READING