姜黄素脂质体粉雾剂的研制和药效学评价

Preparation and pharmacodynamic study of curcumin liposome dry powder inhalation

目的制备姜黄素脂质体粉雾剂并观察其对大鼠急性肺损伤的药效学评价结果。方法用薄膜分散法制备姜黄素脂质体。以乳糖为载体通过喷雾干燥和正交实验设计,筛选姜黄素脂质体粉雾剂的处方及工艺,考察其肺部沉降率。用酸吸入造成大鼠急性肺损伤模型,考察粉雾剂的药效。结果姜黄素脂质体粒径为30 nm,分布均匀,包封率为89.1%,稳定性好。姜黄素脂质体粉雾剂流动性好,体外有效部位沉积率较高,可达46.71%。脂质体粉雾剂与姜黄素混悬液比较,对急性肺损伤的治疗有明显优势。结论姜黄素脂质体粉雾剂可有效治疗急性肺损伤。将难溶性药物制备成脂质体可提高药物在肺部的吸收和疗效。姜黄素脂质体粉雾剂有望成为治疗吸入性肺损伤的有效药物。

Objective To prepare curcumin liposomes for curcumin liposome dry powder inhalation and to observe the efficacy for rat acute lung injury（ALI）.Methods Curcumin liposomes were prepared by the film method.The optimal formulation of curcumin liposome dry powder inhalations（DPIs） was screened by orthogonal design strategy.The inhalation was prepared with lactose as the carrier by spray drying.Rat acute lung injury was made by acid inhaling,which was used to evaluate the effect of inhalation.Results The curcumin liposomes had a tiny size of 30 nm with narrow distribution,high encapsulation of 89.1%,and good stability.The curcumin liposome DPIs had good fluidity and the in vitro deposition test showed that the respirable fraction was 46.71%.Compared with curcumin suspensions,the curcumin liposome DPIs had much better therapeutic effect on rat ALI.Conclusion ALI could be treated using curcumin liposome DPIs and liposomes could improve the insoluble drug＇ absorption and therapeutic efficacy via pulmonary administration.The curcumin liposome dry powder inhalation would be a promising drug for inspiratory lung injury.