Comparative intraocular penetration of 4 fluoroquinolones after topical instillation

Jae Lim Chung, Eun Hye Lim, Sang Wroul Song, Byung Yeop Kim, Joon H. Lee, Francis S. Mah, Kyoung Yul Seo

Research output: Contribution to journalArticle

22 Citations (Scopus)

Abstract

Purpose: To compare the intraocular penetration of 4 fluoroquinolone eye drops after topical instillation into rabbit eyes. Methods: The tested drugs were levofloxacin 1.5% (LVFX), gatifloxacin 0.3%, moxifloxacin 0.5% (MFLX), and besifloxacin 0.6% (BFLX). Forty-eight New Zealand white rabbits were randomly assigned into 2 groups. For group 1 (40 rabbits, 80 eyes), single instillation was performed, and tissue samples were acquired after 0.5, 1, 2, 4, and 6 hours. For group 2 (8 rabbits, 16 eyes), repeated instillation was performed (4 times, every 15 minutes), and tissues were acquired 1 hour after the fourth instillation. The drug concentrations in ocular tissues (cornea, aqueous, conjunctiva, and trisected vitreous) were analyzed with high-performance liquid chromatography. Results: The AUC0-6 h (area under the curve, in microgram.hour/ gram) in group 1 and the mean concentration (in micrograms/gram) in group 2 for LVFX, gatifloxacin 0.3%, MFLX, and BFLX, respectively, were 22.97, 6.44, 13.54, and 3.29 and 22.60, 6.99, 13.69, and 1.91 in cornea; 5.66, 1.43, 3.38, and 0.42 and 5.52, 1.29, 2.47, and 0.19 in aqueous humor; 2.33, 0.91, 2.17, and 9.83 and 4.51, 0.78, 1.48, and 2.09 in bulbar conjunctiva; 0.243, 0.051, 0.134, and 0.018 and 0.182, 0.055, 0.122, and 0.015 in anterior vitreous; none of the drugs achieved enough concentration in equatorial and posterior vitreous. Repeated instillation resulted in approximately 2.1 times greater penetration than single instillation. Conclusions: LVFX and MFLX demonstrated good intraocular penetration particularly in cornea, aqueous humor, and anterior vitreous, and they may be considered the penetrative fluoroquinolones. BFLX showed high concentration in bulbar conjunctiva and may be considered the retentive fluoroquinolone.

Original languageEnglish
Pages (from-to)1046-1051
Number of pages6
JournalCornea
Volume32
Issue number7
DOIs
Publication statusPublished - 2013 Jul 1

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Fluoroquinolones
Levofloxacin
Conjunctiva
Cornea
Rabbits
Aqueous Humor
Pharmaceutical Preparations
Ophthalmic Solutions
Area Under Curve
High Pressure Liquid Chromatography
7-(3-aminohexahydro-1H-azepin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
moxifloxacin
gatifloxacin

All Science Journal Classification (ASJC) codes

  • Ophthalmology

Cite this

Chung, J. L., Lim, E. H., Song, S. W., Kim, B. Y., Lee, J. H., Mah, F. S., & Seo, K. Y. (2013). Comparative intraocular penetration of 4 fluoroquinolones after topical instillation. Cornea, 32(7), 1046-1051. https://doi.org/10.1097/ICO.0b013e31828d6d9e
Chung, Jae Lim ; Lim, Eun Hye ; Song, Sang Wroul ; Kim, Byung Yeop ; Lee, Joon H. ; Mah, Francis S. ; Seo, Kyoung Yul. / Comparative intraocular penetration of 4 fluoroquinolones after topical instillation. In: Cornea. 2013 ; Vol. 32, No. 7. pp. 1046-1051.
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title = "Comparative intraocular penetration of 4 fluoroquinolones after topical instillation",
abstract = "Purpose: To compare the intraocular penetration of 4 fluoroquinolone eye drops after topical instillation into rabbit eyes. Methods: The tested drugs were levofloxacin 1.5{\%} (LVFX), gatifloxacin 0.3{\%}, moxifloxacin 0.5{\%} (MFLX), and besifloxacin 0.6{\%} (BFLX). Forty-eight New Zealand white rabbits were randomly assigned into 2 groups. For group 1 (40 rabbits, 80 eyes), single instillation was performed, and tissue samples were acquired after 0.5, 1, 2, 4, and 6 hours. For group 2 (8 rabbits, 16 eyes), repeated instillation was performed (4 times, every 15 minutes), and tissues were acquired 1 hour after the fourth instillation. The drug concentrations in ocular tissues (cornea, aqueous, conjunctiva, and trisected vitreous) were analyzed with high-performance liquid chromatography. Results: The AUC0-6 h (area under the curve, in microgram.hour/ gram) in group 1 and the mean concentration (in micrograms/gram) in group 2 for LVFX, gatifloxacin 0.3{\%}, MFLX, and BFLX, respectively, were 22.97, 6.44, 13.54, and 3.29 and 22.60, 6.99, 13.69, and 1.91 in cornea; 5.66, 1.43, 3.38, and 0.42 and 5.52, 1.29, 2.47, and 0.19 in aqueous humor; 2.33, 0.91, 2.17, and 9.83 and 4.51, 0.78, 1.48, and 2.09 in bulbar conjunctiva; 0.243, 0.051, 0.134, and 0.018 and 0.182, 0.055, 0.122, and 0.015 in anterior vitreous; none of the drugs achieved enough concentration in equatorial and posterior vitreous. Repeated instillation resulted in approximately 2.1 times greater penetration than single instillation. Conclusions: LVFX and MFLX demonstrated good intraocular penetration particularly in cornea, aqueous humor, and anterior vitreous, and they may be considered the penetrative fluoroquinolones. BFLX showed high concentration in bulbar conjunctiva and may be considered the retentive fluoroquinolone.",
author = "Chung, {Jae Lim} and Lim, {Eun Hye} and Song, {Sang Wroul} and Kim, {Byung Yeop} and Lee, {Joon H.} and Mah, {Francis S.} and Seo, {Kyoung Yul}",
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Chung, JL, Lim, EH, Song, SW, Kim, BY, Lee, JH, Mah, FS & Seo, KY 2013, 'Comparative intraocular penetration of 4 fluoroquinolones after topical instillation', Cornea, vol. 32, no. 7, pp. 1046-1051. https://doi.org/10.1097/ICO.0b013e31828d6d9e

Comparative intraocular penetration of 4 fluoroquinolones after topical instillation. / Chung, Jae Lim; Lim, Eun Hye; Song, Sang Wroul; Kim, Byung Yeop; Lee, Joon H.; Mah, Francis S.; Seo, Kyoung Yul.

In: Cornea, Vol. 32, No. 7, 01.07.2013, p. 1046-1051.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Comparative intraocular penetration of 4 fluoroquinolones after topical instillation

AU - Chung, Jae Lim

AU - Lim, Eun Hye

AU - Song, Sang Wroul

AU - Kim, Byung Yeop

AU - Lee, Joon H.

AU - Mah, Francis S.

AU - Seo, Kyoung Yul

PY - 2013/7/1

Y1 - 2013/7/1

N2 - Purpose: To compare the intraocular penetration of 4 fluoroquinolone eye drops after topical instillation into rabbit eyes. Methods: The tested drugs were levofloxacin 1.5% (LVFX), gatifloxacin 0.3%, moxifloxacin 0.5% (MFLX), and besifloxacin 0.6% (BFLX). Forty-eight New Zealand white rabbits were randomly assigned into 2 groups. For group 1 (40 rabbits, 80 eyes), single instillation was performed, and tissue samples were acquired after 0.5, 1, 2, 4, and 6 hours. For group 2 (8 rabbits, 16 eyes), repeated instillation was performed (4 times, every 15 minutes), and tissues were acquired 1 hour after the fourth instillation. The drug concentrations in ocular tissues (cornea, aqueous, conjunctiva, and trisected vitreous) were analyzed with high-performance liquid chromatography. Results: The AUC0-6 h (area under the curve, in microgram.hour/ gram) in group 1 and the mean concentration (in micrograms/gram) in group 2 for LVFX, gatifloxacin 0.3%, MFLX, and BFLX, respectively, were 22.97, 6.44, 13.54, and 3.29 and 22.60, 6.99, 13.69, and 1.91 in cornea; 5.66, 1.43, 3.38, and 0.42 and 5.52, 1.29, 2.47, and 0.19 in aqueous humor; 2.33, 0.91, 2.17, and 9.83 and 4.51, 0.78, 1.48, and 2.09 in bulbar conjunctiva; 0.243, 0.051, 0.134, and 0.018 and 0.182, 0.055, 0.122, and 0.015 in anterior vitreous; none of the drugs achieved enough concentration in equatorial and posterior vitreous. Repeated instillation resulted in approximately 2.1 times greater penetration than single instillation. Conclusions: LVFX and MFLX demonstrated good intraocular penetration particularly in cornea, aqueous humor, and anterior vitreous, and they may be considered the penetrative fluoroquinolones. BFLX showed high concentration in bulbar conjunctiva and may be considered the retentive fluoroquinolone.

AB - Purpose: To compare the intraocular penetration of 4 fluoroquinolone eye drops after topical instillation into rabbit eyes. Methods: The tested drugs were levofloxacin 1.5% (LVFX), gatifloxacin 0.3%, moxifloxacin 0.5% (MFLX), and besifloxacin 0.6% (BFLX). Forty-eight New Zealand white rabbits were randomly assigned into 2 groups. For group 1 (40 rabbits, 80 eyes), single instillation was performed, and tissue samples were acquired after 0.5, 1, 2, 4, and 6 hours. For group 2 (8 rabbits, 16 eyes), repeated instillation was performed (4 times, every 15 minutes), and tissues were acquired 1 hour after the fourth instillation. The drug concentrations in ocular tissues (cornea, aqueous, conjunctiva, and trisected vitreous) were analyzed with high-performance liquid chromatography. Results: The AUC0-6 h (area under the curve, in microgram.hour/ gram) in group 1 and the mean concentration (in micrograms/gram) in group 2 for LVFX, gatifloxacin 0.3%, MFLX, and BFLX, respectively, were 22.97, 6.44, 13.54, and 3.29 and 22.60, 6.99, 13.69, and 1.91 in cornea; 5.66, 1.43, 3.38, and 0.42 and 5.52, 1.29, 2.47, and 0.19 in aqueous humor; 2.33, 0.91, 2.17, and 9.83 and 4.51, 0.78, 1.48, and 2.09 in bulbar conjunctiva; 0.243, 0.051, 0.134, and 0.018 and 0.182, 0.055, 0.122, and 0.015 in anterior vitreous; none of the drugs achieved enough concentration in equatorial and posterior vitreous. Repeated instillation resulted in approximately 2.1 times greater penetration than single instillation. Conclusions: LVFX and MFLX demonstrated good intraocular penetration particularly in cornea, aqueous humor, and anterior vitreous, and they may be considered the penetrative fluoroquinolones. BFLX showed high concentration in bulbar conjunctiva and may be considered the retentive fluoroquinolone.

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