辛夷挥发油鼻腔醇质体喷雾剂的制备及其质量评价

目的 研究剔除a-松油醇后的辛夷挥发油（VOMF）醇质体喷雾剂的最佳制备处方，并考察其性质和鼻黏膜纤毛毒性。方法 采用注入法制备5% VOMF醇质体，以包封率和载药量为考察指标，采用正交设计法对VOMF醇质体的制备处方进行优化，并对醇质体形态、粒径大小分布、Zeta电位、稳定性等进行评价；以在体蟾蜍口腔上腭纤毛在药物溶液作用下持续摆动时间（PVD）和持续运动率（PPV）评价不同组给药后的鼻黏膜纤毛毒性。结果 最优处方组合为大豆磷脂用量1.5%，胆固醇用量0.15%，乙醇用量36%。质量评价结果表明醇质体圆整均匀，Zeta电位为（-55.9±2.1）mV，喷雾后醇质体平均粒径下降，包封率基本无变化。鼻黏膜纤毛毒性研究表明该制剂基本无鼻黏膜纤毛毒性。结论 注入法制备的剔除a-松油醇后的VOMF醇质体工艺简单、可靠，产品稳定性好，基本无鼻黏膜纤毛毒性，表明该制剂可用于鼻腔给药。

Preparation of nasal ethosome sprays of volatile oil in Magnoliae Flos and evaluation of its quality

Objective To study the optimal preparation process of nasal ethosome sprays of volatile oil in Magnoliae Flos after removing a-terpineol alcohol (VOMF) and to investigate its characteristics and mucociliotoxicity. Methods The 5% VOMF ethosome was prepared with ultrasonic injection method, and the orthogonal test was used to design the formulations of VOMF ethosome which was evaluated by entrapment efficiency and drug loading as indexes. Quality evaluation included appearance, particle diameter distribution, Zeta potential, entrapment efficiency (EE), and stability. The persistent vibration duration (PVD) and percentage of persistent vibration (PPV) in situ toad oral palate cilia were observed to evaluate the mucociliotoxicity administered by various constituents. Results The optimal preparation was 1.5% of phospholipid, 0.15% of cholesterol, and 36% of ethyl alcohol. The quality evaluation showed that the ethosome was round and uniform, while the mean Zeta potential was (-55.9 ± 2.1) mV. The average particle diameter was getting smaller, the EE had no change, and no mucociliotoxicity was found after spraying. Conclusion Ultrasonic injection method used to prepare VOMF ethosome is rational and stable and it can be used for nasal administration.