Vitreal Pharmacokinetics of Biotinylated Ganciclovir: Role of Sodium-Dependent Multivitamin Transporter Expressed on Retina

Abstract

SMVT was identified and functionally characterized on ARPE-19 cells. Further, Biotin-GCV shares this transport system. Vitreal pharmacokinetics of the conjugate was determined in unconscious rabbit model.

Intravitreal loading injection of ganciclovir with or without adjunctive oral valganciclovir for cytomegalovirus anterior uveitis

“…Intravitreal ganciclovir may be more effective than systemic ganciclovir in patients with CMV anterior uveitis, presumably because of the establishment of a higher effective concentration at the site of infection. In the animal model, the vitreal concentration of ganciclovir after intravitreal injection was about 100 times higher than after intravenous injection [22]. In addition, intraocular local drug delivery could also decrease the side-effects of systemic ganciclovir-related bone marrow suppression and is also cost-effective.…”

Intravitreal clearance and volume of distribution of compounds in rabbits: In silico prediction and pharmacokinetic simulations for drug development

“…34 V ss, ivt and CL ivt values were determined from the available literature on intravitreal drug administra- 35 tion using compartmental models and curve fitting. A simple QSPR model for CL ivt of small molecular 36 weight compounds was obtained with two descriptors: Log D 7.4 and hydrogen bond donor capacity. 37 The model predicted the internal and external test sets reliably with a mean fold error of 1.50 and 38 1.33, respectively (Q 2 Y = 0.62).…”

Transporters and receptors in the posterior segment of the eye

“…Biotin, pantothenic acid, lipoic acid TR-iBRB, isolated rat retinal vascular endothelial cells, ARPE-19, rabbit retina [109], [110] Reduced folate carrier (RFC1)…”