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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 the phospholipid complex - chitosan microsphere dry powder inhaler to investigate the feasibility of its inhalation for pulmonary inhalation. Methods With curcumin as model drug, the phospholipid complex - chitosan microspheres was prepared by spray drying method. The effects of technological factors on drug loading, fluidity, hygroscopicity, aerodynamic diameter and in vitro deposition of microspheres were investigated. The effects of technological factors on the drug loading, microstructure and morphology were investigated by scanning electron microscopy (SEM), X-ray diffraction (XRD) and differential scanning calorimetry DSC) microspheres were characterized. Results The ratio of phospholipid to chitosan has a great influence on the properties of microspheres. Optimized curcumin phospholipid complex - chitosan microspheres with a smooth spherical surface, drug loading (11.79 ± 0.82)%, aerodynamic diameter (3.93 ± 0.53) μm, lung deposition rate up to (59.36 ± 5.17)%, the emptying rate was (98.55 ± 0.60)%. Microspheres have low hygroscopicity but poor fluidity. DSC and XRD showed that the presence of curcumin in the phospholipid complex microspheres was not free state but maintained the complex state with the phospholipid. Conclusion Spray drying method prepared phospholipid complex chitosan microspheres is expected to be used for pulmonary inhalation.