Preparation and Evaluation of Microemulsion Based Formulations for Rapid-Onset Intranasal Delivery of Zonisamide
Abstract:The purpose of present study was to develop intranasal microemulsions of Zonisamide (ZNS) for direct brain drug delivery. A peceol based oil in water microemulsion (ME) with labrasol as surfactant and transcutol as cosurfactant (2:1) was developed. Phase behaviour and solubilization capacity of the ME systems were studied and were further characterized for drug content, globule size, zeta potential, viscosity, and pH. In vitro drug diffusion studies of developed ME based formulation were carried out through sheep nasal mucosa using Franz diffusion cell. The effect of mucoadhesive agent and different penetration enhancers were also evaluated in the diffusion studies. In vitro drug diffusion study revealed that the ME has significantly increased the drug diffusion across the nasal mucosa. ME containing 1% citric acid as permeation enhancer and 0.5% carbopol 934p as mucoadhesive agent further enhances drug delivery across the mucosa. The safety and efficacy of the optimized formulation is supported by histopathology study which suggests that the formulation does not impart any toxicity to the nasal mucosa. The results of the present investigation suggest that the developed ME system is a promising approach for effective intranasal delivery of ZNS which can enhance its brain delivery for successful treatment of epilepsy.
Document Type: Research Article
Publication date: December 1, 2010
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