Abstract

The present study involves development and optimization of microparticles containing Montelukast Na as anti-asthmatic drug by solvent evaporation method. Montelukast is a leukotriene receptor antagonist (LTRA), it blocks the action of leukotriene D4 (and secondary ligands LTC4 and LTE4) on the cysteinyl leukotriene receptor. This reduces the bronchoconstriction. Results of DSC and FT-IR study have shown that there was no interaction between drug and excipients. M1 to M15 batches were formulated by using different drug polymer ratio of Polycaprolactone and Ethyl cellulose having poly vinyl alcohol as an emulsifying agent supported by response surface methodology using Box-Behnken factorial design. The prepared microparticles were examined for various evaluation parameters like flow properties, % yield, % drug loading, particle size analysis, in vitro drug release at 12 hr. In-vitro release studies were performed in 0.5 % w/v SLS. There was an effect on mean particle size by altering drug polymer ratio and stirring speed. The observed responses were coincided well with the predicted values given by the optimization technique. The optimization of formulation was done by using box-behnken design. The optimized formulations were subjected to stability studies as per ICH guidelines at 40°C temperature and 75% relative humidity. The optimized batch M 19 showed the highest % yield (87.98 %), % drug loading (66.65%), % CDR at 12 hr (99.03 %). The average particle size of optimized batch M19 was 19.25 μm. The result of kinetic models of optimized batch M19 show fickian diffusion kinetics. No significant change was found in drug content by performing stability study on optimized batch M19 as per ICH guidelines.

Keywords

Montelukast Na, Ethyl Cellulose, Polycaprolactone, Solvent Evaporation Method

Cite This Article

Patel, R., Patel, D., Patel, K. N., Patel, P. A., & Nayak, B. S. (2014). Formulation and Evaluation of Microparticles Containing Anti asthmatic Drug. International Journal for Pharmaceutical Research Scholars (IJPRS), 3(2), 242-265.