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