Expression of Peptide Transporters on the Rabbit Retina: A Strategy to Improve Retinal Delivery of Ganciclovir

Author(s): Soumyajit Majumdar, Sreeraj Macha, Yasser Nashed, Ashim K. Mitra

Journal Name: Letters in Drug Design & Discovery

Volume 1 , Issue 1 , 2004

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The objective of this study was to investigate functional expression of peptide transporters on the rabbit retina. In vivo and ex vivo retina / choroidal uptake studies were carried out with New Zealand albino rabbits. [3H]Gly-Sar was used as the model peptide transporter substrate. [3H]Gly-Sar solutions, in the presence and absence of specific inhibitors, were added to the vitreal side of the retina. Results indicate that retinal uptake of [3H]Gly-Sar was significantly inhibited in the presence of other known peptide transporter substrates, such as Gly-Pro and cephalexin. Importantly, valganciclovir, a peptidomimetic prodrug of ganciclovir, also inhibited uptake of [3H]Gly-Sar. These studies therefore, indicate that peptide transporters are functionally expressed on the rabbit retina and retinal concentrations of GCV may be enhanced by targeting these transporters through prodrug derivatization.

Keywords: peptide transporters, ganciclovir, valganciclovir, cmv retinitis, retina

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Article Details

Year: 2004
Page: [73 - 77]
Pages: 5
DOI: 10.2174/1570180043485707

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