The premise of the study was to develop and optimize multiple unit site specific gastroretentive microspheres of itraconazole to prolong the localisation of drug in the stomach and analyzed using response surface methodology. The emulsion solvent diffusion evaporation method was used to prepare hollow microsphere of ethyl cellulose and Eudragit RS100 as low density shell forming polymers. The experimental design matrix was prepared by using central composite design to study the effect of various process parameters over response variables. The optimized microspheres showed particle size 285.1µm, drug entrapment efficiency of 86.8%, buoyancy 51.1% and cumulative drug release 77.80 %. The experimental responses were in good harmony with the predicted values. The drug and excipients compatibility was determined by differential scanning calorimetry and Fourier transform-infrared analysis. The results signifies that gastroretentive hollow microspheres are a promising vehicle to extend the retention time of itraconazole in the upper GI tract and it can be floated in acidic medium for prolonged period of time.
Key words: Hollow microspheres, Eudragit RS100, Ethylcellulose, optimization, Central Composite Design.
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