Comparison of cytotoxicity of fluoroquinolone antimicrobial eye drops and its effect on their bioavailability
- Authors: Hintuba T.S.1, Takhtaev Y.V.2, Okolov I.N.3, Motyleva V.A.1, Shlyakman R.B.2
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Affiliations:
- North-Western State Medical University named after I.I. Mechnikov
- Academician I.P. Pavlov First St Petersburg State Medical University of the Ministry of Healthcare of Russia
- S. Fyodorov Eye Microsurgery Federal State Institution
- Issue: Vol 10, No 1 (2017)
- Pages: 77-86
- Section: Articles
- URL: https://journals.rcsi.science/ov/article/view/6319
- DOI: https://doi.org/10.17816/OV10177-86
- ID: 6319
Cite item
Abstract
In addition to the breadth of activity of antibacterial medications as well as to their pharmacokinetic and pharmacodynamic properties, their safety and bioavailability represent an important aspect. Currently, there is no consensus on fluoroquinolone toxicity.
The aim of the present study was to compare the total cytotoxic effect on corneal epithelium and bioavailability of three antibacterial fluoroquinolone eye drops, registered in the Russian Federation: 1) Oftaquix™ (levofloxacin 5 mg/ml; preservative benzalkonium chloride (BAC) 0.05 mg/ml; produced by Santen Oy, Finland), hereafter “levofloxacin (original)”; 2) Signicef® (levofloxacin 5 mg/ml; preservative BAC 0.1 mg/ml; produced by Sentiss Pharma Pvt. Ltd., India), hereafter “levofloxacin (generic)”; 3) Vigamox® (moxifloxacin® 5 mg/ml; preservative-free; produced by Alcon Laboratories, Inc., USA) hereafter “moxifloxacin” - using in vivo methods and determining the possible effect of preservative presence (in different concentration) or of its absence on reaching the minimal threshold concentrations of the antibiotic in the anterior chamber fluid, using the high-yield liquid chromatography combined with mass-spectrometric detection. The study showed that tested antibacterial medications could exert a cytostatic effect on the corneal epithelium at in vivo conditions and differ in their cytotoxic potential. Benzalkonium chloride presence in Signicef in a concentration twice as high than that of the main medication (Oftaquix) causes a proven by confocal microscopy effect on the corneal epithelium, and this may influence the bioavailability of the medication.
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##article.viewOnOriginalSite##About the authors
Tamara S. Hintuba
North-Western State Medical University named after I.I. Mechnikov
Author for correspondence.
Email: khintubatamara@gmail.com
ophthalmologist, research resident, Department of Ophthalmology
Russian Federation, Saint PetersburgYuri V. Takhtaev
Academician I.P. Pavlov First St Petersburg State Medical University of the Ministry of Healthcare of Russia
Email: ytakhtaev@gmail.com
MD, Prof. of the Ophthalmology department
Russian Federation, Saint PetersburgIgor N. Okolov
S. Fyodorov Eye Microsurgery Federal State Institution
Email: ytakhtaev@gmail.com
PhD, Head of the Clinical Bacteriological Laboratory
Russian Federation, Saint PetersburgVera A. Motyleva
North-Western State Medical University named after I.I. Mechnikov
Email: ytakhtaev@gmail.com
ophthalmologist, research resident, Department of Ophthalmology
Russian Federation, Saint PetersburgRoman B. Shlyakman
Academician I.P. Pavlov First St Petersburg State Medical University of the Ministry of Healthcare of Russia
Email: ytakhtaev@gmail.com
ophthalmologist, research resident, Department of Ophthalmology
Russian Federation, Saint PetersburgReferences
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