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. 2017 May 18;10(5):679-683.
doi: 10.18240/ijo.2017.05.03. eCollection 2017.

Ocular penetration of topically applied 1% tigecycline in a rabbit model

Yasar Sakarya  1 , Rabia Sakarya  1 , Muammer Ozcimen  1 , Sertan Goktas  1 , Serap Ozcimen  2 , Ismail Alpfidan  1 , Ismail Senol Ivacık  1 , Erkan Erdogan  1 , Servet Cetinkaya  3 , Abdulkadir Bukus  1
Affiliations

Ocular penetration of topically applied 1% tigecycline in a rabbit model

Yasar Sakarya et al. Int J Ophthalmol. .

Abstract

Aim: To evaluate ocular penetration of topically applied 1% tigecycline.

Methods: Forty-two New Zealand White rabbits were divided into 3 groups. A 50 µL drop of 1% tigecycline was administered in group 1. In groups 2 and 3, the drop was administered every 15min for 60min (keratitis protocol). Aqueous humor samples in groups 1 and 2 were collected under general anesthesia at 15, 30, 45, 60, 120, and 180min after the last drop. All animals in group 3 were euthanatized. Cornea, vitreous and blood samples were collected 60 and 120min after the last drop. Tigecycline concentrations were measured using high performance liquid chromatography-mass spectrometry (LC-MS/MS).

Results: The peak aqueous humor tigecycline concentration [mean 0.73±0.14 mg/L (SD) and 2.41±0.14 mg/L, respectively] occurred 45min after topical drug application in groups 1 and 2. Group 3 mean values in the cornea, and vitreous, were 3.27±0.50 µg/g, and 0.17±0.10 mg/L at 60min and 3.17±0.77 µg/g and 0.20±0.07 mg/L at 120min, respectively. Tigecycline serum concentrations were negligible.

Conclusion: Tigecycline levels in the aqueous humor in groups 1 and 2, and in the cornea in group 3 exceeded the minimum inhibitory concentrations of most gram-positive organisms that cause bacterial keratitis and endophthalmitis.

Keywords: antibiotic; aqueous humor; cornea; pharmacokinetics; rabbit eyes.

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Figures

Figure 1
Figure 1. Aqueous humor versus time concentration curve of single drop of topical 1% tigecycline (500 µg).
Figure 2
Figure 2. Aqueous humor versus time concentration curve of tigecycline (2 mg) after topical administration according to a keratitis protocol.
See this image and copyright information in PMC

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