烟台大学学报（自然科学与工程版）2026，Vol.39Issue(1)：32-41,10.DOI:10.13951/j.cnki.37-1213/n.250103
siRNA-阳离子脂质体干粉吸入剂的制备与评价
Preparation and Evaluation of a Cationic Liposome/siRNA Dry Powder for Inhalation
摘要
Abstract
To address the low delivery efficency of conventional siRNA systems in KRAS-targeted drug develop-ment,we developed a cationic liposome-based siRNA dry powder inhaler(siRNA-LP-DPI)to enhance pulmonary drug targeting efficiency.Key parameters—including apparent morphology,particle size distribution,Zeta poten-tial,and redispersibility—were systematically evaluated to optimize process conditions,such as cryoprotectant type and pre-freezing temperature.Using 5%mannitol as the cryoprotectant and a pre-freezing temperature of-80℃,we obtained a white,fluffy siRNA-LP-DPI powder after drying.The optimized formulation exhibited excellent redis-persibility and minimal hygroscopicity,with a redispersed particle size of(98.66±2.61)nm and a Zeta potential of(4.98±0.45)mV,demonstrating favorable physical stability.In vitro cytotoxicity assays revealed that both siRNA-LP and siRNA-LP-DPI significantly reduced A549 tumor cell viability compared to free siRNA controls,with no loss of siRNA bioactivity after lyophilization.Cellular uptake studies further confirmed that siRNA-LP-DPI substantially enhanced siRNA uptake efficiency in A549 cells.This study provides an effective lung-targeted antitu-mor strategy,offering a promising and safe therapeutic approach for non-small cell lung cancer patients.关键词
KRAS/siRNA/阳离子脂质体/冷冻干燥/干粉吸入剂/非小细胞肺癌Key words
KRAS/siRNA/cationic liposome/freeze drying/dry powder inhaler/non-small cell lung cancer分类
医药卫生引用本文复制引用
LI Xiao,LU Yanxiu,LU Kerui,YU Xiaoyu,LIU Sha..siRNA-阳离子脂质体干粉吸入剂的制备与评价[J].烟台大学学报（自然科学与工程版）,2026,39(1):32-41,10.基金项目
山东省自然科学基金资助项目(ZR2023MH318). （ZR2023MH318）
