Corneal deposits after the topical use of ofloxacin in two children with vernal keratoconjunctivitis

Claerhout, Ilse; Kestelyn, Philippe; Meire, F; Remon, J.P.; Decaestecker, Tineke; Bocxlaer, Jan Van

doi:10.1136/bjo.87.5.646

Cited by 15 publications

(10 citation statements)

References 7 publications

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“…This finding may be because liposomes were prepared at pH 7.4, and ofloxacin has pH dependent solubility, and it has minimum solubility at this pH (4 mg/ml); this will increase the unionized fraction of ofloxacin, which is lipophilic in nature (8). Due to the fact that MLVs contain multiple lamellae capable of loading a higher mass of lipophilic drug than REVs (46), EE% had higher values in the case of MLVs than REVs of the same composition and molar ratio.…”

Section: Factors Affecting Encapsulation Efficiencymentioning

confidence: 99%

“…The marketed eye drop has pH equal to 6.4 (6), and the average pH of tear is 7.2-7.4. Therefore, increasing the pH of ofloxacin solution from 6.4 to 7.2 will increase the unionized fraction of ofloxacin, which exceeds the solubility of drug in water at this pH (less than 4 mg/ ml), as a result of a white crystalline deposit on cornea which is one of major side effect of ofloxacin ophthalmic solution (8).…”

Section: Introductionmentioning

confidence: 99%

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Preparation and Evaluation of Thermosensitive Liposomal Hydrogel for Enhanced Transcorneal Permeation of Ofloxacin

Hosny

2009

AAPS PharmSciTech

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Abstract. Ofloxacin, available as ophthalmic solution, has two major problems: first, it needs frequent administration every 4 hours or even every 1 hour to treat severe eye infection; second, there is formation of white crystalline deposit on cornea due to its pH-dependent solubility, which is very low at pH of corneal fluid. In order to provide a solution to previous problems, ofloxacin in this study is prepared as topically effective in situ thermosensitive prolonged release liposomal hydrogel. Two preparation procedures were carried out, leading to the formation of multilamellar vesicles (MLVs) and reverse-phase evaporation vesicles (REVs) at pH 7.4. Effects of method of preparation, lipid content, and charge inducers on encapsulation efficiency were studied. For the preparation of in situ thermosensitive hydrogel, chitosan/β-glycerophosphate system was synthesized and used as carrier for ofloxacin liposomes. The effect of addition of liposomes on gelation temperature, gelation time, and rheological behaviors of the hydrogel were evaluated. In vitro transcorneal permeation was also determined. MLVs entrapped greater amount of ofloxacin than REVs liposomes at pH 7.4; drug loading was increased by including charge-inducing agent and by increasing cholesterol content until a certain limit. The gelation time was decreased by the addition of liposomes into the hydrogel. The prepared liposomal hydrogel enhances the transcorneal permeation sevenfold more than the aqueous solution. These results suggested that the in situ thermosensitive ofloxacin liposomal hydrogel ensures steady and prolonged transcorneal permeation, which improves the ocular bioavailability, minimizes the need for frequent administration, and decreases the ocular side effect of ofloxacin.

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Section: Factors Affecting Encapsulation Efficiencymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Thermosensitive Liposomal Hydrogel for Enhanced Transcorneal Permeation of Ofloxacin

Hosny

2009

AAPS PharmSciTech

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“…Sparfloxacin drug deposition was demonstrated in a patient with previous corneal graft by Gokhale,6 which resolved after stopping the drug therapy. Claerhout et al 9 have shown crystalline deposition of ofloxacin after use in two children with vernal keratoconjunctivitis. Norfloxacin crystal deposition was noted in three patients treated for bacterial keratitis reported by Castillo et al 7.…”

Section: Discussionmentioning

confidence: 99%

Sparfloxacin-associated corneal epithelial toxicity

2014

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Sparfloxacin is a broad-spectrum fluoroquinolone antibiotic commonly used for various bacterial corneal infections. Topical use of fluoroquinolones is considered to be safe leading to their widespread use. Common indications include blepharitis, conjunctivitis and corneal ulcers. However, unsupervised prolonged use is associated with deposition of crystalline material in the epithelial and anterior stromal layers of the cornea. These may be associated with significant visual symptoms including diminution of vision and glare/photophobia. We present a case of a 40-year-old man who was treated with topical 0.3% sparfloxacin unsupervised for a long time. The patient developed significant visual impairment due to diffuse epitheliopathy. Cessation of the drug was slowly followed by reversal of manifestations and normalisation of corneal morphology.

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“…Corneal deposits of fluoroquinolones have been observed in up to 17.6% of people during the treatment of bacterial keratitis . Corneal deposits are most commonly reported after the topical use of ciprofloxacin, but norfloxacin‐ and ofloxacin‐related corneal deposits have also been reported in humans . Corneal deposits have antimicrobial activity and can serve as drug reservoirs .…”

Section: Discussionmentioning

confidence: 99%

Corneal plaque containing levofloxacin in a dog

Park

Kang²,

Lim³

et al. 2015

Veterinary Ophthalmology

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A 13-year-old castrated male Yorkshire terrier developed a corneal ulcer 2 weeks after intracapsular lens extraction (ICLE) in the right eye. The corneal ulcer was treated with levofloxacin eye drops. A plaque with a white luster developed in the central cornea 2 weeks after treatment with levofloxacin eye drops. The corneal plaque was surgically removed under inhalant anesthesia. The corneal plaque displayed antimicrobial activity against Escherichia coli. Furthermore, levofloxacin content in the plaque was confirmed by matrix-assisted laser desorption/ionization time-of-flight/time-of-flight (MALDI-TOF/TOF) mass spectrometry (MS). The corneal ulcer completely resolved 2 weeks after the surgical removal of the corneal lesion and replacement of levofloxacin eye drops with tobramycin eye drops. Although the topical use of levofloxacin is unlikely to lead to corneal chemical deposits due to the high water solubility of the drug compared to other topical fluoroquinolones, this patient developed corneal plaque of the antibiotic drop.

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Corneal deposits after the topical use of ofloxacin in two children with vernal keratoconjunctivitis

Cited by 15 publications

References 7 publications

Preparation and Evaluation of Thermosensitive Liposomal Hydrogel for Enhanced Transcorneal Permeation of Ofloxacin

Preparation and Evaluation of Thermosensitive Liposomal Hydrogel for Enhanced Transcorneal Permeation of Ofloxacin

Sparfloxacin-associated corneal epithelial toxicity

Corneal plaque containing levofloxacin in a dog

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