Multidisciplinary Ophthalmic Imaging Positron Emission Tomography for the Development and Characterization of Corneal Permanence of Ophthalmic Pharmaceutical Formulations
BibTeX
@MISC{Fernández-Ferreiro_multidisciplinaryophthalmic,
author = {Anxo Fernández-Ferreiro and Jesús Silva-Rodríguez and Francisco Javier Otero-Espinar and Miguel González-Barcia and María Jesús Lamas and Alvaro Ruibal and Andrea Luaces-Rodriguez and Alba Vieites-Prado and Tomas Sobrino and Michel Herranz and Lara García-Varela and José Blanco-Mendez and María Gil-Martínez and María Pardo and Alexis Moscoso and Santiago Medín-Aguerre and Juan Pardo-Montero and Pablo Aguiar and Juan Pardo-Montero and Pablo Aguiar},
title = {Multidisciplinary Ophthalmic Imaging Positron Emission Tomography for the Development and Characterization of Corneal Permanence of Ophthalmic Pharmaceutical Formulations},
year = {}
}
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Abstract
Citation: Fernández-Ferreiro A, SilvaRodríguez J, Otero-Espinar FJ, et al. Positron emission tomography for the development and characterization of corneal permanence of ophthalmic pharmaceutical formulations. Invest Ophthalmol Vis Sci. 2017;58:772-780. DOI:10.1167/iovs.16-20766 PURPOSE. This work is aimed at describing the utility of positron emission tomography/ computed tomography (PET/CT) as a noninvasive tool for pharmacokinetic studies of biopermanence of topical ocular formulations. METHODS. The corneal biopermanence of a topical ophthalmic formulation containing gellan gum and kappa carragenan (0.82% wt/vol) labeled with 18 Fluorine ( 18 F) radiotracers ( 18 F-FDG and 18 F-NaF) was evaluated by using a dedicated small-animal PET/CT, and compared with the biopermanence of an aqueous solution labeled with the same compounds. Regions of interest (ROIs) were manually drawn on the reconstructed PET images for quantifying the radioactivity concentration in the eye. The biopermanence of the formulations was determined by measuring the radioactivity concentration at different times after topical application. Additionally, cellular and ex vivo safety assays were performed to assess the safety of the performed procedures. RESULTS. Differences were observed in the ocular pharmacokinetics of the two formulations. After 1.5 hours of contact, 90% of the hydrogel remained in the ocular surface, while only 69% of the control solution remained. Furthermore, it was observed that flickering had a very important role in the approach of the trial. The application of 18 F-FDG in the eye was neither irritating nor cytotoxic for human corneal epithelial cells. CONCLUSIONS. The use of small-animal PET and 18 F radiotracers in ocular pharmacokinetics of ophthalmic formulations is feasible and could be a safe method for future ocular pharmacokinetic studies in humans.
