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目的:制备鼻用干粉吸入剂,探讨以壳聚糖为载体的黄芩苷纳米粒组装成微球的制备方法及其体外释放性能、鼻黏膜渗透性。方法:采用离子交联法制备黄芩苷壳聚糖纳米粒,利用喷雾干燥法将纳米粒组装成微球。利用扫描电镜、差示扫描量热及X射线衍射等对微球进行表征,考察其在人工鼻电解质液中的体外释放性能及模拟人鼻黏膜条件下的鼻黏膜渗透性。结果:黄芩苷纳米粒(一级粒子)平均粒径(170.5±2.3)nm,纳米粒经喷雾干燥后形成平均粒径(6.8±0.4)μm的微球(二级粒子),药物以无定形态分布于载体材料中,微球比流动能(5.46±0.37)m J·g-1。在正应力15 k Pa时,空气以2 mm·s-1的速度通过微球粉末时气压降值0.323 k Pa。该粒子遇人工鼻电解质溶液后能重新分散,释放出一级粒子。体外释放表明微球33 h累积释放率(78.85±2.71)%,体外释药过程符合Riger-Peppas模型。微球在7 h时单位面积累计释放量为黄芩苷原料药的1.77倍。结论:制备的黄芩苷微球能够释放出一级粒子,具有较好的流动性、透气性和一定缓释作用,可提高黄芩苷的透鼻黏膜性。
OBJECTIVE: To prepare a nasal dry powder inhaler for the preparation of microspheres assembled with chitosan nanoparticles loaded with chitosan and its in vitro release properties and nasal mucosa permeability. Methods: Baicalin chitosan nanoparticles were prepared by ion-crosslinking method. The nanoparticles were assembled into microspheres by spray drying. The microspheres were characterized by scanning electron microscopy, differential scanning calorimetry and X-ray diffraction. Their in vitro release properties in artificial nasal electrolyte and nasal mucosal permeability in the simulated human nasal mucosa were investigated. Results: The average particle size of baicalin nanoparticles (primary particles) was (170.5 ± 2.3) nm. After the nanoparticles were spray dried, the microspheres (secondary particles) with the mean particle diameter of 6.8 ± 0.4 μm were formed. Morphology distribution in the carrier material, microspheres than the mobile energy (5.46 ± 0.37) m J · g-1. At normal pressure of 15 kPa, the air pressure drops by 0.323 kPa when the air passes through the microsphere powder at the speed of 2 mm-s-1. The particles are redispersed after the artificial nasal electrolyte solution is released, releasing a first-order particle. The in vitro release showed a 33 h cumulative release rate of microspheres (78.85 ± 2.71)%, in vitro release process in line with the Riger-Peppas model. The accumulated release per unit area of microspheres at 7 h was 1.77 times of the baicalin bulk drug. CONCLUSION: The prepared baicalin microspheres can release first-grade particles with better fluidity, air permeability and certain sustained-release effect, which can improve the nasal mucosa of baicalin.