Fabrication of potential gastroretentive microspheres of itraconazole for stomach-specific delivery: Statistical optimization and in vitro evaluation
Journal of Applied Pharmaceutical Science
The premise of the study was to develop and optimize multiple unit gastroretentive microspheres of itraconazole to prolong its localization 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 lowdensity shell-forming polymers. The experimental design matrix was prepared using a central composite design to study the effect of various process parameters
... cess parameters over response variables. The optimized microspheres showed a particle size of 285.1µm, drug entrapment efficiency of 86.8%, buoyancy of 51.1%, and cumulative drug release of 77.80%. The experimental responses were in good harmony with the predicted values. The compatibility between drug and excipients was determined by Fourier-transform infrared and differential scanning calorimetry analysis. The results signify 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 an acidic medium for a prolonged period.