Design, Development, Evaluation and Optimization of Microballoons of Telmisartan

Abstract

In present study an attempt was made to prepare microballoons of Telmisartan by emulsion solvent diffusion technique for sustained delivery by using polymers like Ethyl cellulose to extend the drug release for about 12 hours in the upper GIT, which may result in enhanced absorption and there by improved bioavailability. Formulation optimization of Telmisartan loaded microballoons was carried out by using different concentration of Polyvinyl alcohol (PVA) and Ethyl cellulose. Total 9 batches were formulated. All 9 batches were evaluated for entrapment efficiency (EE) and buoyancy. Among all batches DP4 shows maximum entrapment efficiency (EE) and buoyancy and was considered as optimized formulation. DP4 batch was further used for process optimization. The process optimization was carried out at three different stirring speeds i.e. 1300, 1500 and 1700 rpm for three different stirring time period i.e. 1hr, 2hr and 3 hr and another 9 batches were formulated. Out of all the batches DP13 showed the spherical shape of microballoons without formation of flakes. Optimized batch DP13 was evaluated for Zeta Potential, Particle Size Distribution which show - 41.8mV and 1.344 μm particle size, SEM, XRD Analysis. Batch DP13 was charged for stability and were placed in glass vials container and stored at ICH storage condition (2°C - 4°C Refrigeration condition , 30 ± 2°C / 60% ± 5% RH , 40 ± 2°C / 75% ± 5% RH ) for a period of 30 days. The samples were analyzed for physical appearance, buoyancy and for the drug release after 30 days. After 1 months samples were withdrawn and microballoons showed no change in physical appearances, buoyancy and drug release, which indicate that the microballoons were stable.