FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF VENLAFAXINE HCL
Journal Title: International Research Journal of Pharmacy (IRJP) - Year 2011, Vol 2, Issue 4
Abstract
The objective of the present investigation was to formulate and evaluate the mucoadhesive Venlafaxine HCl microspheres using Hydroxy propyl methyl cellulose K4M as polymer. Venlafaxine HCl is a new generation serotonin reuptake inhibitor drug showing effective antidepressant properties, having a short bioavailability of 12.6% and biological half-life of 5 hours. Venlafaxine HCl microspheres were prepared by simple emulsification phase separation technique using glutaraldehyde as a crosslinking agent. Fifteen preliminary trail batches A1-A15 of microspheres were prepared by using different volume (10ml to 50ml) of glutaraldehyde (25% v/v aqueous solution) as crosslinking agent, crosslinking time of 1 to 3 hours and the polymer to drug in 3:1 ratio. From those fifteen preliminary trial batches, the optimized formulation was selected based on the percentage of mucoadhesion and sphericity of microspheres. On the basis of the preliminary trials, 32 full factorial design was employed to study the effect of independent variable X1 (polymer-to- drug ratio 1:1, 3:1 and 6:1) and the stirring speed X2 (500, 1000 and 1500rpm) on the dependent variables like percentage mucoadhesion, drug entrapment efficiency, particle size and t80. The drug polymer compatibility studies were carried out using FTIR. The stability studies were conducted for the optimized formulation. The optimized formulation exhibited a high drug entrapment efficiency of 70% and a swelling index 1.57, % mucoadhesion after 1hour was 91% and the drug release was also sustained for more than 12 hours. As the concentration of glutaraldehyde increased, the mucoadhesiveness decreases and there was no significant effect in time. Stirring speed has negative effect on t80.
Authors and Affiliations
Senthil Adimoolam , Hardik Kumar Thakkar , Mehulkumar Dave , Tejas Lad , Bhagya Battu
Keywords
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