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Journal of Pharmaceutical Negative Results
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Year : 2011  |  Volume : 2  |  Issue : 1  |  Page : 24-27

EDTA decreases in vitro transcorneal permeation of fluconazole in phosphate buffer through excised sheep cornea

1 Gurukul College of Pharmacy, Suratgarh, Rajasthan, India
2 Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar, Haryana, India

Correspondence Address:
Sunil Thakral
5-M-24, Jawahar Nagar, Sri Ganganagar, Rajasthan
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Source of Support: None, Conflict of Interest: None

DOI: 10.4103/0976-9234.82986

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Introduction: According to the World Health Organization, corneal diseases are a major cause of vision loss and blindness, second only to cataract in overall importance. Fungal keratitis is a major blinding eye disease in Asia. In epithelia, calcium has been implicated in the maintenance of intercellular matrix and therefore may be a key factor determining the size of potential paracellular routes for drug transport. Although the effects of chelating agents such as EDTA on the permeability of inorganic and organic solutes have been well documented in other epithelia, as well as the corneal endothelium, no definitive studies examining the effects of these compounds upon corneal epithelia have been reported. Materials and Methods: The corneal permeation studies were conducted using freshly excised sheep cornea, mounted between donor and receptor chambers of an all glass-modified Franz diffusion cell, containing 11 ml of ringer bicarbonate (pH 7.4, 34 o±1 o C). At the end of the experiment, each cornea (freed from sclera) was weighed, soaked in 1 ml of methanol, dried overnight at 90΀C and reweighed. From the difference in weights corneal hydration was calculated Results: Fluconazole ophthalmic solutions (0.2% w/v, pH 6.0) containing EDTA shows significant difference in P app 1.51×10 6 (cm/s) as compared to fluconazole ophthalmic solutions (0.2% w/v, pH 6.0) without EDTA showing 2.37×10 6 (cm/s). Conclusions: Use of ethylene diamine tetraacetate as chelating agent in fluconazole ophthalmic solutions significantly decreased the corneal permeability of fluconazole.

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