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 language | English |
|---|---|
| Pages (from-to) | 208-216 |
| Number of pages | 9 |
| Journal | Graefe's Archive for Clinical and Experimental Ophthalmology |
| Volume | 239 |
| Issue number | 3 |
| State | Published - May 21 2001 |
| Externally published | Yes |
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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 journal › Article
}
TY - JOUR
T1 - Intravitreal acetylsalicylic acid in silicon oil
T2 - Pharmacokinetics and evaluation of its safety by ERG and histology
AU - Kralinger, Martina T.
AU - Hamasaki, Duco
AU - Kieselbach, Gerhard F.
AU - Voigt, Monika
AU - Parel, Jean-Marie A
PY - 2001/5/21
Y1 - 2001/5/21
N2 - 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.
AB - 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.
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UR - http://www.scopus.com/inward/citedby.url?scp=0035022626&partnerID=8YFLogxK
M3 - Article
C2 - 11405070
AN - SCOPUS:0035022626
VL - 239
SP - 208
EP - 216
JO - Albrecht von Graefes Archiv für Klinische und Experimentelle Ophthalmologie
JF - Albrecht von Graefes Archiv für Klinische und Experimentelle Ophthalmologie
SN - 0065-6100
IS - 3
ER -