Formulation Development of Ketoconazole Ophthalmic Formulation

The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid precorneal elimination of drug may be overcome by the use of ophthalmic gel systems. The purpose of the present study was to develop ophthalmic gel formulations of ketoconazole. Intraocular delivery of topically applied drugs such as ketoconazole is hampered by elimination of the solution due to tear turnover, so an mucoadhesive gel was formulated. Ketoconazole gels were prepared using sodium carboxymethylcellulose (NaCMC) as a mucoadhesive polymer and xanthan gum as a viscosity increasing agent. Gels were evaluated for various parameters like appearance, pH, drug content, gel strength, bioadhesion, viscosity, In-vitro drug release, isotonisity, sterility, antifungal activity, ocular irritancy and stability studies. The gel strength, bioadhesion and isotonisity shown quality parameter for ophthalmic formulation. The optimized formulation containing 1% w/v Na CMC and 0.2% w/v xanthan gum have shown 97.66% drug release up to 8 hrs. This is sufficient for antifungal activity. Diffusion studies have shown that a Korsmeyers-peppas is the best-fit model. This study found that an optimized formulation having improved viscosity and better mucoadhesive property may improve the bioavaibility of ocular administration of ketoconazole in gel form and can be alternative to the conventionally administered oral formulation and effectively used to prolong residence time.