Human vitreous concentrations of citicoline following topical application of citicoline 2% ophthalmic solution.

ABSTRACT: PURPOSE:To evaluate the presence and concentration of citicoline and its metabolites (choline, cytidine and uridine) in the vitreous body in human eyes after topical application of an ophthalmic solution of citicoline 2%, in vivo. METHODS:Twenty-one subjects affected by epiretinal membrane with surgical indication for pars-plana vitrectomy underwent treatment with 1 drop 3 times/day of a solution of citicoline 2%, 0.2% high molecular weight hyaluronic acid and 0.01% benzalkonium chloride (OMK1, Omikron Italia s.r.l., Rome, Italy) 14 days before surgery and 2 hours prior to surgery. Five additional patients served as controls and received an OMK1 vehicle solution without citicoline. The vitreous samples were taken at the beginning of the pars-plana vitrectomy and analyzed for qualitative/quantitative determination of vitreous concentration of citicoline and its metabolites by means of high performance liquid chromatography. RESULTS:The overall mean concentration of citicoline in patients treated with citicoline 2% solution was 406.72 ± 52.99 ?g/mL, while the mean concentration of choline, cytidine and uridine was 180.88 ± 41.49 ?g/mL, 44.45 ± 10.19 ?g/mL and 330.41 ± 75.8 ?g/mL, respectively. The concentration of citicoline in phakic eyes (n = 13, 366.61 ± 129.61 ?g/mL) was lower compared to that found in pseudophakic eyes (n = 8, 435.89 ± 131.42 ?g/mL) and the difference was not statistically significant. The concentration of citicoline in the control eyes was 45.66 ± 26.36 ?g/mL, while the concentration of choline, cytidine and uridine were 17.21 ± 9.93 ?g/mL, 6.24 ± 3.6 ?g/mL and 172.80 ± 99.76 ?g/mL, respectively. CONCLUSION:Citicoline can reach the human vitreous in high concentration when administered in ophthalmic solution. This evidence contributes to the build-up of the pyramid of the evidences required for determining the role of citicoline administered in ophthalmic formulation in retinal and optic nerve neurodegenerative diseases.

SUBMITTER: Carnevale C 

PROVIDER: S-EPMC6855484 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature