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Characterisation of systemic and ocular drug level of triamcinolone acetonide following a single sub-Tenon injection
  1. Kaihui Nan1,
  2. Shumao Sun1,
  3. Yuli Li1,
  4. Jia Qu1,
  5. Guoxing Li1,
  6. Li Luo1,
  7. Hao Chen1,
  8. Lingyun Cheng1,2
  1. 1Institute of Ocular Pharmacology, School of Ophthalmology and Optometry, Wenzhou Medical College, Wenzhou, Zhejiang, China
  2. 2Jacob's Retina Center at Shiley Eye Center, Department of Ophthalmology, University of California San Diego, La Jolla, California, USA
  1. Correspondence to Dr Lingyun Cheng and Dr Hao Chen, Institute of Ocular Pharmacology, School of Ophthalmology and Optometry, Wenzhou Medical College, 270 Xueyuan Road, Wenzhou, Zhejiang 325027, China; cheng{at}eyecenter.ucsd.edu or chenhao{at}mail.eye.ac.cn

Abstract

Aim To characterise the pharmacokinetics of triamcinolone acetonide (TA) in various ocular tissues following a single sub-Tenon injection.

Methods Twenty-one Chinchilla adult pigmented rabbits received sub-Tenon injection of TA (40 mg in 0.4 ml) in their right eyes. Three animals were killed at each designated time points (3 h, 1 day, 3 days, 7 days, 14 days, 21 days and 30 days) and the globes were snap frozen and dissected into aqueous, iris-ciliary body, vitreous, neuroretina and retinal pigment epithelium (RPE)/choroid. The concentrations of TA in the various ocular tissues were analysed using ultra-performance liquid chromatography, coupled with tandem mass spectrometric detection.

Results TA concentration followed a mono-exponential decrease over the study period in all ocular tissues of the injected eyes. The concentration was much higher in the RPE/choroid (892.14±558.11 ng/g at post-injection day 30) than in the other tissues (171.65±136.40 ng/g in neuroretina, 15.65±23.06 ng/ml in vitreous, 3.76±1.79 ng/g in iris-ciliary body, 2.64±0.96 ng/ml in aqueous at post-injection day 30). The TA level in the RPE/choroid had the lowest coefficient of logarithmic regression (0.07 in RPE/choroid, 0.10 in neuroretina, 0.11 in vitreous, 0.17 in iris-ciliary body, 0.18 in aqueous), indicating a 2.6 times slower clearance than in aqueous. The half-life of TA was 10.4 days in RPE/choroid. TA was detectable in the fellow eyes and was also detectable at very low levels in all blood samples during the entire study period.

Conclusion TA was mostly cleared from RPE/choroid and retina in a mono-exponential mode. TA was above the therapeutic level for at least 30 days following a sub-Tenon injection.

  • Choroid
  • ocular pharmacokinetics
  • pharmacology
  • rabbit eye
  • retina
  • sub-Tenon injection
  • triamcinolone acetonide
  • UPLC/MS/MS
  • vitreous

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Footnotes

  • Funding National Natural Science Foundation of China, Grant No.30870631; 2. Qianjiang Talents Grant, No.2008R10041.

  • Competing interests None.

  • Ethics approval Obtained.

  • Provenance and peer review Not commissioned; externally peer reviewed.

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