In Vitro Effects of Fluoroquinolone and Aminoglycoside Antibiotics on Human Keratocytes

Leonardi, Andrea; Papa, Vincenzo; Fregona, I.; Russo, P.; Franchis, G. De; Milazzo, Giovanni

doi:10.1097/01.ico.0000164782.10667.ed

Cited by 13 publications

(5 citation statements)

References 30 publications

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“…Some earlier studies compared the cytotoxicity between FQs, ofloxacin and the aminoglycoside, netilmicin. [35][36][37] They concluded that netilmicin was significantly less toxic than ofloxacin to human keratocytes, 37 to intact and mechanically damaged rabbit eyes, 36 and to rabbit corneal epithelial cells. 35 Mallari et al 38 also found an increased risk of corneal perforation after FQ treatment for bacterial keratitis, compared with treatment with fortified antibiotics (cephazolin 5% and tobramycin 1.36%).In our study, preservative-free fortified gentamicin and cefazolin were less cytotoxic to corneal epithelium cells than all the other FQ solutions tested.…”

Section: Discussionmentioning

confidence: 99%

Comparison of fluoroquinolones: cytotoxicity on human corneal epithelial cells

Tsai

Chen

2009

Eye

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Purpose To compare the cytotoxicity of different fluoroquinolones (FQs) towards human corneal epithelial cells (HCECs). Methods HCECs were incubated with FQs (norfloxacin, ciprofloxacin, ofloxacin, levofloxacin, moxifloxacin, and gatifloxacin), both as commercial ophthalmic formulations and as unpreserved solutions. Cells incubated in different formulations of gentamicin, cefazolin, and benzalkonium chloride (BAC) were also compared. A cell viability assay, using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) assay, was used to evaluate the drug effects on cell viability after five incubation times (30 min, 1 h, 4 h, 8 h, and 24 h). Transepithelial electrical resistance (TEER) was measured with a voltohmmeter to help understand changes in paracellular permeability at five time points (4 h, 8 h, 12 h, 24 h, and 48 h). Cell morphology was observed with an inverted fluorescence microscope, with multiple stage position and in time-lapse mode. Results The preserving solutions and BAC at concentrations above 0.005% significantly decreased cell viability, when assayed by MTS. Increased paracellular permeability and decreased membrane integrity were also observed by TEER measurements and inverted fluorescence microscopy. Ofloxacin and levofloxacin were both free of preservatives and showed the least cytotoxicity towards HCECs in commercial FQ eye drops. Conclusions The cytotoxicity observed with FQ eye drops seems to be caused mainly by the preservative, which induced a significant decrease in membrane integrity and increased paracellular permeability. We found the new generation of FQs (moxifloxacin and gatifloxacin) no less cytotoxic towards HCECs than the old generation ones.

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Section: Discussionmentioning

confidence: 99%

Comparison of fluoroquinolones: cytotoxicity on human corneal epithelial cells

Tsai

Chen

2009

Eye

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“…Netilmicin is a broad spectrum, third generation aminoglycoside with excellent in vitro activity against the most common bacterial ocular pathogens, including Pseudomonas spp 14,27–29. Netilmicin is noncytotoxic and does not interfere with physiological healing, and is therefore able to provide good protection against bacterial infections during the wound repair process 12,13,15…”

Section: Discussionmentioning

confidence: 99%

“…This gel has no preservative and contains two natural biopolymers (xanthan gum and sodium hyaluronate) in addition to netilmicin. Hyaluronate is well known for promoting physiological wound healing by stimulating corneal epithelial cell migration and proliferation,9–11 whereas netilmicin is an effective, safe, and noncytotoxic antibiotic that is able to provide good protection against bacterial infections during the process of wound repair 12–15…”

mentioning

confidence: 99%

A new eye gel containing sodium hyaluronate and xanthan gum for the management of post-traumatic corneal abrasions

Faraldi¹,

Papa²,

Santoro³

et al. 2012

OPTH

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PurposeThe aim of this study was to investigate the effects of an ophthalmic gel containing sodium hyaluronate and xanthan gum in addition to the antibiotic netilmicin in the management of traumatic corneal abrasions.Patients and methodsPatients with traumatic corneal abrasions were randomly treated as follows: Group A (n = 20) with an occlusive patching for 12 hours plus one drop of an eye gel containing 0.15% sodium hyaluronate, 1% xanthan gum and 0.3% netilmicin qid for 5 days; and Group B (n = 20) with an occlusive patching for 2–3 days plus one application of 0.3% netilmicin ophthalmic ointment qid for 5 days. All patients were evaluated after the third and seventh day by slit-lamp examination, fluorescein staining, and corneal defect photograph in order to assess corneal re-epithelialization. Conjunctival hyperaemia, lid oedema, subjective symptoms of discomfort, and conjunctival swabs were also evaluated.ResultsNo statistically significant difference was observed between the groups in terms of the extent of corneal healing after 3 days of treatment. Both treatments were also highly effective in decreasing the erosion score and the conjunctival hyperemia (P < 0.0001, P < 0.005, respectively) without any significant difference between the two types of treatment. Subjective symptoms of discomfort and conjunctival swabs were also evaluated.ConclusionIn the management of traumatic corneal abrasions, the administration of an eye gel containing sodium hyaluronate and xanthan gum is able to reduce the length of occlusive patching. In addition, the presence of netilmicin guarantees good antibiotic prophylaxis during the wound repair process.

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“…26 Topically applied fluoroquinolones have been considered to be more toxic to the corneal epithelium than other antibiotic agents. 27,28 However, in a recently published study levofloxacin did not negatively influence epithelial wound healing. 29 Moreover, levofloxacin was shown to be less cytotoxic on human corneal keratocytes and epithelial cells than other fluoroquinolones, including gatifloxacin, moxifloxacin, ciprofloxacin and ofloxacin.…”

Section: Pharmacokinetic and Toxicological Propertiesmentioning

confidence: 92%

Effectiveness of Levofloxacin Eye Drops – A Microbiological Perspective

Kresken¹,

Kreutzer²,

Kaspar³

2009

European Ophthalmic Review

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Levofloxacin is a later-generation antibacterial agent of the fluoroquinolone class that exhibits a broad spectrum of in vitro activity. It has been demonstrated to be effective in the treatment of a wide range of community-and hospital-associated infections. 1 This review presents a microbiological perspective of the use of levofloxacin for topical treatment of bacterial external ocular infections, presenting in vitro, pharmacokinetic and clinical trials data. Levofloxacin eye drops were launched in several European countries in 2002. The widespread use of levofloxacin in ophthalmology can be attributed to its appropriate antibacterial spectrum and good corneal penetration. The main indications for treatment are bacterial blepharitis and conjunctivitis, bacterial keratitis -especially when associated with contact lenses -and endophthalmitis, where it is provided as an additional therapeutic agent. Furthermore, levofloxacin eye drops are used as prophylaxis to reduce the bacterial conjunctival flora prior to intraocular surgery. In a healthy eye the conjunctival bacterial flora primarily consists of Staphylococcus spp. (mainly S. epidermidis), Corynebacterium spp. and, to a lesser degree, Streptococcus spp. and various Gram-negative rods. 2 The predominant bacterial organisms isolated from patients with acute bacterial conjunctivitis are S. aureus, S. pneumoniae and Haemophilus influenzae, the latter being frequently recovered from children. 3,4 S. aureus is also considered the primary pathogen of chronic blepharoconjunctivitis. The leading organisms causing bacterial keratitis are Staphylococcus spp., Streptococcus spp., Pseudomonas aeruginosa and enteric Gram-negative rods. 5,6 Gram-negative bacilli account for most cases of contact-lensassociated bacterial keratitis. Pharmacodynamic Properties of LevofloxacinLevofloxacin is the L-isomer of the racemic drug ofloxacin. The antibacterial activity of ofloxacin resides almost entirely in the L-isomer. Therefore, levofloxacin is, by its nature, twice as active as ofloxacin per unit of mass. 7

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In Vitro Effects of Fluoroquinolone and Aminoglycoside Antibiotics on Human Keratocytes

Cited by 13 publications

References 30 publications

Comparison of fluoroquinolones: cytotoxicity on human corneal epithelial cells

Comparison of fluoroquinolones: cytotoxicity on human corneal epithelial cells

A new eye gel containing sodium hyaluronate and xanthan gum for the management of post-traumatic corneal abrasions

Effectiveness of Levofloxacin Eye Drops – A Microbiological Perspective

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