Vitreous pharmacokinetics and retinal safety of intravitreal preserved versus non-preserved triamcinolone acetonide in rabbit eyes

Rafael C. Oliveira, André Messias, Rubens C. Siqueira, Marco A. Bonini-Filho, Antnio Haddad, Francisco M. Damico, Alfredo Maia-Filho, Pedro Tb Crispim, Juliana B. Saliba, Jefferson A.S. Ribeiro, Ingrid U. Scott, Armando S. Cunha-Jr, Rodrigo Jorge

Research output: Contribution to journalArticle

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Abstract

Purpose: To compare the intravitreal pharmacokinetic profile of a triamcinolone acetonide formulation containing the preservative benzyl alcohol (TA-BA) versus a preservative-free triamcinolone acetonide formulation (TA-PF), and evaluate potential signs of toxicity to the retina. Methods: A total of 60 New Zealand male white rabbits, divided into two groups, were studied. In the TA-BA group, 30 rabbits received an intravitreal injection of TA-BA (4mg/0.1ml) into the right eye. In the TA-PF group, 30 rabbits received an intravitreal injection of TA-PF (4mg/0.1ml) into the right eye. The intravitreal drug levels were determined in 25 animals from each group by high-performance liquid chromatography (HPLC). The potential for toxicity associated with the intravitreal triamcinolone injections was evaluated in five randomly selected animals from each group by electroretinography (ERG) and by light microscopy. Results: Median intravitreal concentrations of TA-BA (g/ml) were 1903.1, 1213.0, 857.8, 442.0, 248.6 at 3, 7, 14, 21 and 28 days after injection. Intravitreal concentrations of TA-PF (g/ml) were 1032.9, 570.1, 516.6, 347.9, 102.8 at 3, 7, 14, 21 and 28 days after injection. The median intravitreal triamcinolone concentration was significantly higher in the TA-BA compared to the TA-PF group at 7 days post-injection (p<0.05). There was no significant difference between the two groups in median triamcinolone concentration at the other time points evaluated. There was no evidence of toxic effects on the retina in either group based on ERG or histological analyses. Conclusions: Following a single intravitreal injection, the median concentration of triamcinolone acetonide is significantly higher in the TA-BA compared to the TA-PF group at 7 days post-injection. No toxic reactions in the retina were observed in either group.

Original languageEnglish (US)
Pages (from-to)55-61
Number of pages7
JournalCurrent Eye Research
Volume37
Issue number1
DOIs
StatePublished - Jan 1 2012

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Triamcinolone Acetonide
Intravitreal Injections
Triamcinolone
Pharmacokinetics
Rabbits
Electroretinography
Safety
Retina
Injections
Poisons
Benzyl Alcohol
Microscopy
High Pressure Liquid Chromatography
Light
Pharmaceutical Preparations

All Science Journal Classification (ASJC) codes

  • Ophthalmology
  • Sensory Systems
  • Cellular and Molecular Neuroscience

Cite this

Oliveira, R. C., Messias, A., Siqueira, R. C., Bonini-Filho, M. A., Haddad, A., Damico, F. M., ... Jorge, R. (2012). Vitreous pharmacokinetics and retinal safety of intravitreal preserved versus non-preserved triamcinolone acetonide in rabbit eyes. Current Eye Research, 37(1), 55-61. https://doi.org/10.3109/02713683.2011.593722
Oliveira, Rafael C. ; Messias, André ; Siqueira, Rubens C. ; Bonini-Filho, Marco A. ; Haddad, Antnio ; Damico, Francisco M. ; Maia-Filho, Alfredo ; Crispim, Pedro Tb ; Saliba, Juliana B. ; Ribeiro, Jefferson A.S. ; Scott, Ingrid U. ; Cunha-Jr, Armando S. ; Jorge, Rodrigo. / Vitreous pharmacokinetics and retinal safety of intravitreal preserved versus non-preserved triamcinolone acetonide in rabbit eyes. In: Current Eye Research. 2012 ; Vol. 37, No. 1. pp. 55-61.
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abstract = "Purpose: To compare the intravitreal pharmacokinetic profile of a triamcinolone acetonide formulation containing the preservative benzyl alcohol (TA-BA) versus a preservative-free triamcinolone acetonide formulation (TA-PF), and evaluate potential signs of toxicity to the retina. Methods: A total of 60 New Zealand male white rabbits, divided into two groups, were studied. In the TA-BA group, 30 rabbits received an intravitreal injection of TA-BA (4mg/0.1ml) into the right eye. In the TA-PF group, 30 rabbits received an intravitreal injection of TA-PF (4mg/0.1ml) into the right eye. The intravitreal drug levels were determined in 25 animals from each group by high-performance liquid chromatography (HPLC). The potential for toxicity associated with the intravitreal triamcinolone injections was evaluated in five randomly selected animals from each group by electroretinography (ERG) and by light microscopy. Results: Median intravitreal concentrations of TA-BA (g/ml) were 1903.1, 1213.0, 857.8, 442.0, 248.6 at 3, 7, 14, 21 and 28 days after injection. Intravitreal concentrations of TA-PF (g/ml) were 1032.9, 570.1, 516.6, 347.9, 102.8 at 3, 7, 14, 21 and 28 days after injection. The median intravitreal triamcinolone concentration was significantly higher in the TA-BA compared to the TA-PF group at 7 days post-injection (p<0.05). There was no significant difference between the two groups in median triamcinolone concentration at the other time points evaluated. There was no evidence of toxic effects on the retina in either group based on ERG or histological analyses. Conclusions: Following a single intravitreal injection, the median concentration of triamcinolone acetonide is significantly higher in the TA-BA compared to the TA-PF group at 7 days post-injection. No toxic reactions in the retina were observed in either group.",
author = "Oliveira, {Rafael C.} and Andr{\'e} Messias and Siqueira, {Rubens C.} and Bonini-Filho, {Marco A.} and Antnio Haddad and Damico, {Francisco M.} and Alfredo Maia-Filho and Crispim, {Pedro Tb} and Saliba, {Juliana B.} and Ribeiro, {Jefferson A.S.} and Scott, {Ingrid U.} and Cunha-Jr, {Armando S.} and Rodrigo Jorge",
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Oliveira, RC, Messias, A, Siqueira, RC, Bonini-Filho, MA, Haddad, A, Damico, FM, Maia-Filho, A, Crispim, PT, Saliba, JB, Ribeiro, JAS, Scott, IU, Cunha-Jr, AS & Jorge, R 2012, 'Vitreous pharmacokinetics and retinal safety of intravitreal preserved versus non-preserved triamcinolone acetonide in rabbit eyes', Current Eye Research, vol. 37, no. 1, pp. 55-61. https://doi.org/10.3109/02713683.2011.593722

Vitreous pharmacokinetics and retinal safety of intravitreal preserved versus non-preserved triamcinolone acetonide in rabbit eyes. / Oliveira, Rafael C.; Messias, André; Siqueira, Rubens C.; Bonini-Filho, Marco A.; Haddad, Antnio; Damico, Francisco M.; Maia-Filho, Alfredo; Crispim, Pedro Tb; Saliba, Juliana B.; Ribeiro, Jefferson A.S.; Scott, Ingrid U.; Cunha-Jr, Armando S.; Jorge, Rodrigo.

In: Current Eye Research, Vol. 37, No. 1, 01.01.2012, p. 55-61.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Vitreous pharmacokinetics and retinal safety of intravitreal preserved versus non-preserved triamcinolone acetonide in rabbit eyes

AU - Oliveira, Rafael C.

AU - Messias, André

AU - Siqueira, Rubens C.

AU - Bonini-Filho, Marco A.

AU - Haddad, Antnio

AU - Damico, Francisco M.

AU - Maia-Filho, Alfredo

AU - Crispim, Pedro Tb

AU - Saliba, Juliana B.

AU - Ribeiro, Jefferson A.S.

AU - Scott, Ingrid U.

AU - Cunha-Jr, Armando S.

AU - Jorge, Rodrigo

PY - 2012/1/1

Y1 - 2012/1/1

N2 - Purpose: To compare the intravitreal pharmacokinetic profile of a triamcinolone acetonide formulation containing the preservative benzyl alcohol (TA-BA) versus a preservative-free triamcinolone acetonide formulation (TA-PF), and evaluate potential signs of toxicity to the retina. Methods: A total of 60 New Zealand male white rabbits, divided into two groups, were studied. In the TA-BA group, 30 rabbits received an intravitreal injection of TA-BA (4mg/0.1ml) into the right eye. In the TA-PF group, 30 rabbits received an intravitreal injection of TA-PF (4mg/0.1ml) into the right eye. The intravitreal drug levels were determined in 25 animals from each group by high-performance liquid chromatography (HPLC). The potential for toxicity associated with the intravitreal triamcinolone injections was evaluated in five randomly selected animals from each group by electroretinography (ERG) and by light microscopy. Results: Median intravitreal concentrations of TA-BA (g/ml) were 1903.1, 1213.0, 857.8, 442.0, 248.6 at 3, 7, 14, 21 and 28 days after injection. Intravitreal concentrations of TA-PF (g/ml) were 1032.9, 570.1, 516.6, 347.9, 102.8 at 3, 7, 14, 21 and 28 days after injection. The median intravitreal triamcinolone concentration was significantly higher in the TA-BA compared to the TA-PF group at 7 days post-injection (p<0.05). There was no significant difference between the two groups in median triamcinolone concentration at the other time points evaluated. There was no evidence of toxic effects on the retina in either group based on ERG or histological analyses. Conclusions: Following a single intravitreal injection, the median concentration of triamcinolone acetonide is significantly higher in the TA-BA compared to the TA-PF group at 7 days post-injection. No toxic reactions in the retina were observed in either group.

AB - Purpose: To compare the intravitreal pharmacokinetic profile of a triamcinolone acetonide formulation containing the preservative benzyl alcohol (TA-BA) versus a preservative-free triamcinolone acetonide formulation (TA-PF), and evaluate potential signs of toxicity to the retina. Methods: A total of 60 New Zealand male white rabbits, divided into two groups, were studied. In the TA-BA group, 30 rabbits received an intravitreal injection of TA-BA (4mg/0.1ml) into the right eye. In the TA-PF group, 30 rabbits received an intravitreal injection of TA-PF (4mg/0.1ml) into the right eye. The intravitreal drug levels were determined in 25 animals from each group by high-performance liquid chromatography (HPLC). The potential for toxicity associated with the intravitreal triamcinolone injections was evaluated in five randomly selected animals from each group by electroretinography (ERG) and by light microscopy. Results: Median intravitreal concentrations of TA-BA (g/ml) were 1903.1, 1213.0, 857.8, 442.0, 248.6 at 3, 7, 14, 21 and 28 days after injection. Intravitreal concentrations of TA-PF (g/ml) were 1032.9, 570.1, 516.6, 347.9, 102.8 at 3, 7, 14, 21 and 28 days after injection. The median intravitreal triamcinolone concentration was significantly higher in the TA-BA compared to the TA-PF group at 7 days post-injection (p<0.05). There was no significant difference between the two groups in median triamcinolone concentration at the other time points evaluated. There was no evidence of toxic effects on the retina in either group based on ERG or histological analyses. Conclusions: Following a single intravitreal injection, the median concentration of triamcinolone acetonide is significantly higher in the TA-BA compared to the TA-PF group at 7 days post-injection. No toxic reactions in the retina were observed in either group.

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