外水相组成对醋酸戈舍瑞林PLGA微球理化性质的影响

Effect of external aqueous phase composition on the physicochemical properties of goserelin acetate PLGA microspheres

目的 采用W/O/W和O/W乳化溶剂挥发法制备醋酸戈舍瑞林PLGA微球,考察在外部水相中加入不同浓度的氯化钠和甘露醇对所制备微球理化性质的影响。方法 醋酸戈舍瑞林PLGA微球采用W/O/W和O/W乳化溶剂挥发法制备,以微球的表面形态、内部形态、粒径、载药量、体外累计释放行为、结构和晶型来评价不同浓度的添加剂对两种制备方法所制得微球的影响。结果 采用W/O/W制备的微球增加外水相中氯化钠的浓度,微球载药量增加、粒径减小、突释量降低、微球表面及内部孔洞减少;增加外水相中甘露醇的浓度,微球载药量增加、粒径减小,突释量降低、微球表面孔洞减少,内部孔洞未减少;O/W法制备的微球增加水相中氯化钠和甘露醇的浓度,微球载药量增加、粒径减小、突释量降低、微球表面及内部孔洞减少。结论 通过增加外部水相中添加剂的浓度,有效改善了醋酸戈舍瑞林PLGA微球的结构和性质。

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/W and 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.