1.Preparation and in vitro Release Property Study of Curcumin Dry Powder Inhalation Loaded by Nanoporous Flower-shaped Lactose
Nan LI ; Xu LI ; Peng CHENG ; Lingyu KONG ; Renrui FENG ; Songwen TAN
China Pharmacy 2021;32(7):794-801
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 son- (45.93 ± 1.77)% . Its 24 h solubility in artificial lung gwen.tan@csu.edu.cn 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.