Effect of external aqueous phase composition on the physicochemical properties of goserelin acetate PLGA microspheres
Objective To determine the effect of sodium chloride and mannitol in the outer aqueous phase on the physicochemical properties of the goserelin acetate PLGA microspheres.Methods Goserelin acetate PLGA microspheres were prepared by W/O/Wand O/W emulsion-solvent evaporation methods.The effects of different concentrations of sodium chloride and mannitol on the microspheres were evaluated in terms of surface morphology,internal morphology,particle size,drug loading,in vitro release,structure and crystal form.Results For microspheres prepared by W/O/W method,an increase in the concentration of both sodium chloride and mannitol in the outer aqueous phase resulted in an increase in drug loading,a decrease in particle size and burst release,and a reduction in surface pores.Sodium chloride instead of mannitol reducted the internal pores of the microspheres.For microspheres prepared by the O/W method,an increase in the concentration of both additives resulted in an increase in drug loading,a decrease in particle size and burst release,and a reduction in both surface and internal pores of the microspheres.Conclusion By increasing the concentration of sodium chloride and mannitol in the outer aqueous phase,the structure and properties of goserelin acetate PLGA microspheres are effectively improved.