纳米多孔花形乳糖装载姜黄素干粉吸入剂的制备及体外释药性能研究

目的:制备一种新型的纳米多孔花形乳糖(FL)装载姜黄素(Cur)干粉吸入剂(DPI),为难溶性药物治疗慢性阻塞性肺疾病提供一种安全、高效的肺内递药方式.方法:采用溶液吸附法制备FL微粒装载Cur(Cur-FL)复合粉末.以载药量和吸附率为指标,通过单因素试验优选Cur投药浓度、Cur与FL的投药比例(m/m)和吸附时间...

Preparation and in vitro Release Property Study of Curcumin Dry Powder Inhalation Loaded by Nanoporous Flower-shaped Lactose

OBJECTIVE:To preparea novel Curcumin(Cur)dry powder inhalation(DPI)loaded by nanoporous flower-shaped lactose(FL),and to provide a safe and effective intrapulmonary drug delivery method for the therapy of chronic obstructive pulmonary disease with insoluble drugs.METHODS:FL-loaded Cur(Cur-FL)compound powder was prepared by solution adsorption method.Using drug-loading amount and adsorption rate as indicators,single-factor experiment was used to optimize Cur concentration,Cur-FL ratio(m/m)and adsorption time so as to determine the optimal preparation technology for Cur-FL compound powder.Fourier transform infrared spectroscopy,scanning electron microscope and differential scanning calorimetry were used to characterize the physical and chemical properties of Cur-FL compound powder prepared with optimal technology.The water content and aerodynamic properties were determined;in vitro drug release behavior was investigated by simulating the environment of artificial lung fluid.RESULTS:The optimal preparation technology of Cur-FL compound powder was Cur concentration of 5 mg/mL,Cur-FL ratio of 1∶4,adsorption time of 1 h.The drug-loading amount of compound powder was(23.37±0.43)%,the encapsulation rate was(91.64±0.44)%,and the adsorption rate was(30.50±0.72)%.Cur-FL particles were flower shaped;Cur was physically adsorbed in the pores of FL without chemical changes.The bulk density of Cur-FL compound was(0.21±0.02)g/cm³,tap density was(0.33±0.01)g/cm³,angle of repose was(24.07±0.31)°,average particle size was(3.96±0.80)μm,aerodynamic particle size was(3.33±0.99)μm,water content was(5.63±0.24)%,emptying rate was(92.53±0.87)%,and deposition rate of effective parts in vitro was(45.93±1.77)%.Its 24 h solubility in artificial lung fluid([358.93±1.67)μg/mL]were 3.28 times of Cur,48 h cumulative release ratesin in vitro(90.21%)were 1.63 times of Cur,but Cur+FL physical mixture could not improve the solubility and release of Cur in artificial lung fluid.CONCLUSIONS:Cur-FL compound powder has good in vitro release property,and its powder properties,solubility,water content,fluidity and aerodynamic properties meet the requirements of DPI in Chinese Pharmacopoeia.