Intravitreal acetylsalicylic acid in silicon oil: Pharmacokinetics and evaluation of its safety by ERG and histology

Martina T. Kralinger, Duco Hamasaki, Gerhard F. Kieselbach, Monika Voigt, Jean-Marie A Parel

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

Background: A new method of intravitreal drug delivery of acetylsalicylic acid (AS) in silicone oil was investigated for safety and for its pharmacokinetics in the posterior pole of the eye. Methods: The AS was mixed in silicone oil to a concentration of 1.67 mg/ml. After vitrectomy, 15 NZW rabbits received an intravitreal injection of AS/silicone oil suspension. Clinical examination, pre-and postoperative electroretinography (ERG) and histology were performed. The pharmacokinetics of the distribution of salicylic acid was determined by HPLC analysis at 6 h, 24 h and 5 days in optic nerve, retina, choroid, vitreous, and blood. Results: Clinical examination and histology revealed no adverse effects or signs of toxicity. The ERGs showed no significant difference between the pre- and postoperative results. The salicylic acid concentrations demonstrated peak values in the residual vitreous (640.0 υg/ml), choroid (446.0 ng/mg) and retina (281.3 ng/mg) at 6 h. At 24 h, the salicylic acid concentration decreased to 20.9 υg/ml in the residual vitreous and to 38.5 ng/mg in the retina. At 5 days the retinal level was still 48.1 ng/mg. Conclusions: AS delivery by intravitreal administration of loaded silicone oil is a safe method and results in high concentrations of salicylic acid in the posterior segment of the eye while maintaining low blood levels.

Original languageEnglish
Pages (from-to)208-216
Number of pages9
JournalGraefe's Archive for Clinical and Experimental Ophthalmology
Volume239
Issue number3
StatePublished - May 21 2001
Externally publishedYes

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Silicone Oils
Electroretinography
Salicylic Acid
Silicon
Aspirin
Histology
Oils
Pharmacokinetics
Safety
Retina
Choroid
Posterior Eye Segment
Intravitreal Injections
Vitrectomy
Optic Nerve
Suspensions
High Pressure Liquid Chromatography
Rabbits
Pharmaceutical Preparations

ASJC Scopus subject areas

  • Ophthalmology

Cite this

Intravitreal acetylsalicylic acid in silicon oil : Pharmacokinetics and evaluation of its safety by ERG and histology. / Kralinger, Martina T.; Hamasaki, Duco; Kieselbach, Gerhard F.; Voigt, Monika; Parel, Jean-Marie A.

In: Graefe's Archive for Clinical and Experimental Ophthalmology, Vol. 239, No. 3, 21.05.2001, p. 208-216.

Research output: Contribution to journalArticle

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