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Three series of novel compounds derived from 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid bearing piperazine carboxamides, (5-(substituted phenyl)-1,3,4-oxadiazol-2-yl) and (5-(alkylthio)-1,3,4-oxadiazol-2-yl) substitutions at the 4-position were synthesized. Synthesized compounds were characterized by 1 H NMR, 13 C NMR and mass spectral analysis and evaluated for their antimicrobial activities. Interestingly, most of the compounds exhibit moderate to good activities against tested Gram-positive, Gram-negative bacterial strains as well as fungal strains. ª 2015 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

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Background: Voriconazole (VCZ) is a lipophilic candidate, effective against fungal infections like ocular keratitis and endopthalmitis. Objective: The purpose to develop, optimize and characterize voriconazole microemulsion as sustained medication for ophthalmic application. Methods: The pseudo-ternary phase diagrams were developed using oleic acid, isopropyl myristate and isopropyl palmitate (oil phases), tween 80 (surfactant), propylene glycol (co-surfactant), distilled water (aqueous phase) and modified chitosan (Mod.CH) as mucoadhesive polymer. The optimum composition of oil, Smix and water was selected on the basis of phase diagrams and as mucoadhesive polymer Mod.CH was used in the formulations. All the formulations were evaluated for thermodynamic stability/dispersibility, physicochemical parameters (droplet size, polydispersity index, zeta potential, drug content, viscosity, pH and conductivity), in vitro, ex vivo and in vivo studies. Results: All formulations showed droplet size below 250 nm, positive zeta potential and polydispersity index below 0.5. The in vitro drug release study performed on selected formulations showed maximum sustained release than marketed formulation. The in vitro transcorneal permeation experiment of formulations suggests that optimized formulations showed better permeation. The selected formulation of voriconazole microemulsion was able to produce maximum antifungal activity against Candida albicans when compared to marketed formulation. In vivo study performed on rabbit eyes, found more drug concentration in aqueous humor of optimized formulation; the AUC0→t of IPMVM-11 was approximately 6.84-fold higher than VOZOLE and efficiently enhanced the corneal bioavailability. Conclusion: The modified chitosan based on voriconazole loaded microemulsion was promising novel carrier for sustained action in ophthalmic medication.