In-SituGellingOphthalmicFormulationsforSustainedRelease andEnhanced OcularDelivery ofFluconazole
Journal Title: IOSR Journal of Pharmacy and Biological Sciences (IOSR-JPBS) - Year 2016, Vol 11, Issue 2
Abstract
: The present work describes formulation and evaluation of ophthalmic delivery systems of an effective anti-fungal named fluconazole (FLZ) based on the concept of temperature-triggered in-situ gelation using poloxamer 407 (P407) and ion-activated in-situ gelation employing sodium alginate (ALG) in purpose of easy eye instillation as drops that form gels in the eye providing sustained drug release, prolonged eye contact, and improved ocular delivery. Plain in-situ gelling ophthalmic formulations were prepared using different concentrations of the utilized polymers to optimize the gelling capacity. FLZ formulations with good gelling capacity were evaluated regarding viscosity, pH, drug content, in-vitro release, and stability for 6 months at different temperatures. The optimized formula that provided a sustained release and the highest shelf life was then assessed with respect to its ocular bioavailability in rabbits. All formulations possessed pH tolerable by the eye, acceptable viscosity values and drug contents complying with pharmacopeial limits. In-vitro release results indicated a sustained drug release without any burst effect and non-Fickian release mechanism. The optimized in-situ gel based on P407 (15% w/v) and HPMC (2% w/v) significantly improved FLZ ocular bioavailability in rabbits compared to its solution as a control. Therefore, this formulation may be represented as a potential drug delivery system of FLZ with a sustained release and an enhanced ocular delivery.
Authors and Affiliations
Nabil A. A. Khatera, Osama A. Soliman, Elham A. Mohamed
Keywords
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