Anastrozole is a non-steroidal aromatase-inhibiting, used for treatment of breast cancer. The present study describes the formulation of a controlled release microparticulate drug delivery system containing anastrozole, using poly (D,L lactide-co-glycolide) (PLGA). Microspheres of anastrozole were prepared using the emulsion solvent evaporation technique and effect of critical process parameters and formulation variables were investigated. The parameters such as percentage of initial drug loading, concentration of stabilizer and stirring speed of microsphere preparation were varied to study their effect on the particle size and geometry of the microspheres obtained. The results indicated that the morphology of the anastrozole PLGA microspheres presented a spherical shape with smooth surface, the particle size was distributed from 133 to 89µm and the drug encapsulation efficiency was influenced by homogeneous rotation speed and the polymer concentration in the oil phase and the molecular weight of the polymer. These changes were also reflected in drug release. Selecting an appropriate level of the investigated parameters, spherical microparticles with encapsulation efficiencies higher than 90% and a prolonged anastrozole release over 30 days were obtained.
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