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Oscar Olvera Montaño, Yussett Contreras, Leopoldo Martin Baiza-Duran, Paloma Marquez, Iliana Hernández Pérez, Fernando Castellanos Chang, Juan D Quintana-Hau, Humberto Figueroa; Ocular distribution and safety of the pazufloxacin 0.6% ophthalmic solution in rabbits. Invest. Ophthalmol. Vis. Sci. 2015;56(7 ):5742.
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© ARVO (1962-2015); The Authors (2016-present)
To evaluate ocular distribution and safety of pazufloxacin ophthalmic solution 0.6% after instillation to New Zealand White rabbits eyes.
Sixtytwo healthy male New Zealand White rabbits were used in the studies. Thirtytwo animals (64 eyes) were used in the ocular distribution study, splited into 8 groups of 4. Pazufloxacin ophthalmic solution 0.6% (Laboratorios Sophia S.A. de C.V., Zapopan, JAL, México) was instilled (30 μL) in both eyes. After a single instillation pazufloxacin levels were measured in conjunctiva, cornea and aqueous humor, at the following time points: 0.25, 1, 3, 4, 6, 8, 12 and 24 h. At the predetermined times, animals in each group were euthanized and tissues were collected and then analyzed by high performance liquid chromatography. Thirty animals (60 eyes) were used for the safety study, wich were randomly divided into three groups. Animals in group 1 were instilled pazufloxacin ophthalmic solution; animals in group 2 were instilled moxifloxacin ophthalmic solution 0.5% (Vigamoxi®, Alcon Laboratories Inc., Fort Worth, TX, USA) and the animals in group 3 were instilled gatifloxacin ophthalmic solution 0.5% (Zymar®, Allergan Inc. Irvine, CA, USA), all treatmens were administered in both eyes. Doses were given 7 times daily for 30 days. Slit lamp examination, fluorescein and lisamine green staining were performed on days 2, 7, 10, 15, 20, 25 and 30. On day 31 rabbits were euthanized and eyes enucleated for histopathologic assessment. Conjunctival hyperemia, chemosis, corneal staining and conjunctival discharge were assessed as clinical toxicity and safety criteria.
After a single instillation the highest maximum concentration was found in conjunctiva (21659 ng/g), followed by cornea (11651 ng/g) and aqueous humor (1707 ng/g). Cmax in all tissues were higher than the minimal inhibition concentration for pseudomonas aeuriginosa (422 ng/g)<br /> No statistically significant differences between groups were found. In the histopathologic report no differences were encountered between groups and there were no signs of cellular toxicity.
Pazufloxacin ocular distribution and safety profile, make it a viable option for topical treatment of ocular infections. Further studies are granted to assess and compare efficacy of pazufloxacino and other quinolones.
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