FORMULATION AND EVALUATION OF GEL CONTAING AMLEXANOX FOR MOUTH ULCER

Abstract: Objective: To formulate and evaluate mouth gel of amlexanox using an admixture of gelling agent i.e. carbopol p940 and penetration enhancer i.e. propylene glycol. Experimental work: Gel containing amlexanox was prepared by taking carbopol p934 and propylene glycol as penetration enhancer in different ratio. The concentrations of carbopol p934 and propylene glycol were optimized using 3 2 full factorial designs. The parameters determined were pH, drug content, viscosity, spradability, extrudability, in vitro drug release. Results: The pH values of gels were between 6.0 to 7.0. Drug content values were between 89% to 98%. Drug release was dependent on the concentration of carbopol and concentration of propylene glycol. The in vitro drug release time was 3 hr. Drug release from the gels increased with increase in the concentration of propylene glycol up to 10%. However, drug release decreased with further increase in the concentration of the propylene glycol to 20%. Conclusion: Formulation F6 with concentration of carbopol (1%) and concentration of propylene glycol (7%) showing maximum drug release upto 3 hr. was selected as the optimized formulatio

MICROEMULSION BASED NASAL TO BRAIN DELIVERY OF DRUG ACTING ON CNS

Abstract: Background: Fluvoxamine, an antidepressant drug, has absolute bioavailability of only 53% due to high first pass metabolism. Aim: The purpose of this study was to develop and optimize mucoadhesive microemulsion containing Fluvoxamine for intranasal delivery. Materials and Methods: Based on solubility study, Acrysol K150, Tween 20 and polyethylene glycol (PEG) 400 were selected as oil, surfactant and co surfactant respectively. Microemulsions were prepared using water titration method. 2:1% w/w ratio (Tween 20:PEG 400) was selected for formulation development. The prepared microemulsions were optimized for globule size, zeta potential, pH, Viscosity and polydispersity index. The optimized batch was further characterized for% drug content, pH, viscosity and % drug diffusion. Results and Conclusion: All the parameters showed the suitability of microemulsion of Fluvoxamine for intranasal delivery. Carbapol 934P (0.3 % w/w) was used as a polymer for the preparation of mucoadhesive microemulsion to enhance the retention time in the nasal mucosa. Results of nasal toxicity study using excised sheep nasal mucosa showed comparatively no damage to epithelium and so formulation was considered safe for nasal administration. Fluvoxamine mucoadhesive microemulsion showed the highest percentage of diffusion (98.07 ± 0.710 %) after 24h during ex-vivo drug diffusion study through sheep nasal mucosa, followed by Fluvoxamine microemulsion (93.48 ± 0.674%) and finally by Fluvoxamine solution (70.57 ± 0.612%)