目的 制备磷脂复合物-壳聚糖微球干粉吸入剂，探讨其用于肺部吸入给药的可行性。方法 以姜黄素为模型药物，采用喷雾干燥法制备磷脂复合物-壳聚糖微球。考察工艺因素对微球载药量、流动性、吸湿性、空气动力学径和体外沉积的影响，利用扫描电子显微镜(SEM)观察、X射线衍射分析(XRD)和差示扫描量热法(DSC)对微球进行表征。结果 磷脂与壳聚糖的比例对微球性质有很大影响。优化的姜黄素磷脂复合物-壳聚糖微球为表面光滑的完整球形，载药量为(11.79±0.82)%，空气动力学径为(3.93±0.53)μm，体外肺部沉积率可达(59.36±5.17)%，排空率为(98.55±0.60)%。微球吸湿性小但流动性较差。DSC和XRD显示，姜黄素在磷脂复合物微球中的存在状态并非游离态而是保持了与磷脂的复合状态。结论 喷雾干燥法制备的磷脂复合物壳聚糖微球有望用于肺部吸入给药。

Objective To prepare a dry powder inhalation based on phytosomes-chitosan microspheres and to investigate the possibility for pulmonary delivery. Methods Curcumin was selected to be model drug. The curcumin-phytosomes loaded chitosan microspheres (Cur-PS-CMs) were prepared by spray-drying method. The technology was optimized using drug loading, angle of repose, moisture uptake, theoretical aerodynamic diameter, and aerodynamic behavior in vitro as evaluation indexes. The optimized Cur-PS-CMs were characterized by SEM, DSC, and X-ray diffraction. Results The drug loading of optimized Cur-PS-CMs was (11.79 ± 0.82)%, and the theoretical aerodynamic diameter was (3.93 ± 0.53) μm. The fine particle fraction and emitted dose were (59.36 ± 5.17)% and (98.55 ± 0.60)%, respectively. The humidity uptake was less than 10% but the powder flowability was poor. SEM showed that Cur-PS-CMs were spherical with smooth surface. DSC and X-ray diffraction verified that Cur was not released from PS in CMs. Conclusion The PS-CMs prepared by spray-drying method may have a potential to be used as a dry powder inhalation for pulmonary delivery.

重庆市自然科学基金项目（cstc2011jj10010）；西南大学博士基金项目（SWU111065）；西南大学“国家大学生创新性实验计划”项目（201310635016）