Study of influence of formulation and process variables on entrapment efficiency and particle size of floating microballoons of clopidogrel bisulphate by doe

Microparticulate drug delivery is a prominent method of oral delivery of drugs which is more beneficial than the single unit dosage forms. A prior approach to increase the gastric retention time of the drug through multiparticulate drug delivery is by formulating floating microballoons. They result in more reproducible drug absorption and reduced risk of local irritation, thereby improving the bioavailability of the drug. In the current research work, clopidogrel, a BCS class - II drug was formulated as controlled release microballoons using ethyl cellulose as polymer and span 80 as the surfactant to improve the gastric retention of the drug. Box - Benhken design was selected to design the experiment and the study of effect of various formulation and process parameters like concentration of surfactant, volume of solvent, volume of internal phase, concentration of polymer, speed of rotation on the drug entrapment efficiency and particle size of the microballoons were carried out. The highest drug entrapment efficiency was found to be 93.1% in the F14 formulation. The smallest particle size of the microballoons was found to be 183.9μm in the F32 formulation. Buoyancy studies showed all the formulations have good floating characteristics. The maximum yield of microballoons was found in the F7 formulation with 93.1% yield. The final results were statistically treated using ANOVA and were found to be significant. (p - value < 0.05).