Pharmacokinetics of Melphalan After Intravitreal Injection in a Rabbit Model

Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics
Emiliano BuitragoPaula Schaiquevich

Abstract

Although widely used for vitreous seed control in retinoblastoma patients, currently there are no data on melphalan pharmacokinetics after intravitreal injections. Therefore, in this study, we characterized the ocular and systemic disposition of melphalan after intravitreal injection in the rabbit eye. New Zealand rabbits received a single intravitreal injection of 15 μg of melphalan. Vitreous, aqueous, retina, and blood samples were collected at different times up to 12 h after the injection. Melphalan was quantitated in the biological samples using a validated high-performance liquid-chromatography technique and pharmacokinetic parameters were calculated by means of compartmental models. Model-predicted melphalan maximum vitreous, aqueous, and retina concentrations were 7.8 μg/mL, 0.024 μg/mL, and 9.8 μg/g tissue, respectively, attained immediately and at 0.8 and 0.25 h after intravitreal injection. Melphalan vitreous concentrations were higher than 0.3 μg/mL for 5 h after dosing. The elimination half-life from the vitreous, aqueous humor, and retina was 1.0, 0.2, and 1.2 h, respectively. Aqueous exposure [area under the curve (AUC)] was only 0.7% of that of the vitreous AUC. Melphalan concentrations in the retina were still ...Continue Reading

References

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Citations

Jun 8, 2018·The British Journal of Ophthalmology·David H AbramsonLarissa Habib
Dec 25, 2019·Clinical & Experimental Ophthalmology·Stéphanie LemaîtreCarole D Thomas
Sep 13, 2016·Retina·Paula SchaiquevichDavid H Abramson
Jun 30, 2021·Clinical & Experimental Ophthalmology·Swathi Kaliki
Aug 2, 2019·Ocular Oncology and Pathology·Michael D YuCarol L Shields
Nov 11, 2021·Investigative Ophthalmology & Visual Science·Jessica V KaczmarekAnthony B Daniels

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