The grail of the study was to design, develop and characterize sustained release mucoadhesive microspheres of acyclovir and to optimize the drug release profile using response surface methodology by applying Box–Behnken design (BBD) which was equipped with three levels and three factors. Microspheres were prepared from Methocel K15M and Ethocel Standard 45 Premium using the emulsification solvent evaporation technique. The independent factors were the amounts of Methocel K15M (X1), amount of Ethocel Standard 45 Premium (X2), and RPM (X3). The dependent variables were cumulative percentage drug release (CDR) at 8 hour (Y1), bond strength (Y2), and swelling at 4 hour (Y3). To understand the effects of different factor level combinations on the responses, various response surface graphs and contour plots were prepared. Predicted values and experimental values for optimized formulation (X1 = 600 mg, X2 = 500 mg, and X3 = 336.57) was found to be in close agreement. Dhaka Univ. J. Pharm. Sci. 18(1): 1-2, 2019 (June)
The present investigation was designed to prepare controlled release microspheres of carbamazepine using two polymers of different solubility and permeability characteristics, Ethocel standard 45 premium and Eudragit RL 100. The drug release profile was optimized with the aid of design of experiments (DoE). Microspheres of combined polymers were designed according to 2 2 factorial central composite design (CCD), taking drug loading and polymeric ratio as the independent variables. Total thirteen batches were prepared. The dependent variables were percentage of drug released in 3 hours and 6 hours and mean dissolution time (MDT). The regression parameters of the developed model and graphical interpretation for each response with statistical significance were calculated by using Minitab 17. The relationship between the experimental variables and responses were evaluated by generating response surface plots. Increased amount of Eudragit RL 100 had impact on surface morphology of prepared microspheres. It produced larger holes on the surface due to its higher permeability characteristics. Polynomial mathematical models generated for various response variables using multiple linear regression analysis, were found to be statistically significant (p < 0.05). One optimum formulation (O1) was selected based on USP specification and the second optimum formulation (O2) was selected for the maximization of MDT (hours). Batch O1 showed 22.85 % and 48.78 % drug release after 3 and 6 hours, respectively which were found to be in close agreement with those predicted by the mathematical model. Another optimum formulation, batch O2 showed MDT as 160.61 hours.
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