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聚乙二醇修饰姜黄素固体脂质纳米粒吸入微粉的制备、表征及组织分布研究
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| 篇名： | 聚乙二醇修饰姜黄素固体脂质纳米粒吸入微粉的制备、表征及组织分布研究 |
| TITLE： | Preparation，characterization and tissue distribution of polyethylene glycol-modified Curcumin solid lipid nanoparticle inhalable micropowder |
| 摘要： | 目的 制备吸入用聚乙二醇（PEG）修饰的花形乳糖（FL）装载姜黄素（Cur）固体脂质纳米粒（SLN）吸入微粉（简称“PEG-Cur-FL”）。方法采用溶剂乳化扩散-低温固化法制备PEG-Cur-FL，并对其包封率和载药量、粉体学性质、空气动力学粒径、体外沉积性质和体外释放特性进行表征。将小鼠分为Cur-SLN-FL（未经PEG修饰）组和PEG-Cur-FL组，每组55只。两组小鼠均单次经气管吸入相应药物微粉5mg/kg（以Cur计），分别于给药后0.25、0.5、1、2、4、6、8、12、24、48、72h时摘眼球取血并分离其气管、肺、肝和肾组织，测定小鼠血浆和各组织样品中Cur的质量浓度，分析药物的组织分布和滞留情况。结果PEG-Cur-FL的包封率和载药量分别为（86.2±1.8）%和（4.2±0.2）%，松密度和振实密度分别为（0.24±0.01）g/cm3和（0.30±0.01）g/cm3，空气动力学粒径为（2.74±0.64）μm，体外有效部位沉积率（二级药物沉积率）为（45.07±2.79）%。与Cur原料药比较，Cur-SLN-FL和PEG-Cur-FL在漏槽和非漏槽条件下均具有缓释作用，且PEG-Cur-FL在人工肺液中的释放更平缓，释药特征符合Weibull模型。体内分布结果显示，PEG-Cur-FL组小鼠给药后1h的肺组织药物浓度显著低于同期Cur-SLN-FL组，而4～48h各时间点的肺组织药物浓度均显著高于同期Cur-SLN-FL组（P＜0.05）；PEG-Cur-FL组0.25～12h各时间点的血浆药物浓度均显著低于同期Cur-SLN-FL组，肝、肾组织药物浓度亦低于同期Cur-SLN-FL组（P＜0.05）。结论成功制备PEG-Cur-FL；该吸入微粉具有良好的可吸入性能和释放性能；经气管内给药后可提高Cur在肺组织的药物有效浓度，同时降低其血浆药物浓度和非靶器官的药物分布浓度。 |
| ABSTRACT： | OBJECTIVE To prepare polyethylene glycol （PEG）-modified flower lactose （FL） loaded Curcumin （Cur） solid lipid nanoparticle （SLN） inhalable micropowder （referred to as “PEG-Cur-FL”）. METHODS PEG-Cur-FL was prepared by the solvent emulsification diffusion low-temperature solidification method， and its encapsulation efficiency， drug loading capacity， powder properties， aerodynamic particle size， in vitro deposition properties， and in vitro release characteristics were characterized. The mice were divided into Cur-SLN-FL （unmodified with PEG） group and PEG-Cur-FL group， with 55 mice in each group. Both groups of mice were given a single inhalation of 5 mg/kg （calculated as Cur） of the corresponding drug micropowder through an air tube. At 0.25， 0.5， 1， 2， 4， 6， 8， 12， 24， 48 and 72 hours after administration， eyeballs were removed to collect blood and tracheal， lung， liver and kidney tissues were separated. The mass concentration of Cur in mouse plasma and various tissue samples was measured， and the tissue distribution and retention of the drug were analyzed. RESULTS The encapsulation efficiency and drug loading capacity of PEG-Cur-FL were （86.2±1.8）% and （4.2±0.2）%， respectively； the bulk density and tap density were （0.24±0.01） g/cm3 and （0.30±0.01） g/cm3， respectively； the aerodynamic particle size was （2.74±0.64） μm； the in vitro effective site deposition rate （secondary drug deposition rate） was （45.07±2.79）%. Compared with Cur raw materials， Cur-SLN- FL and PEG-Cur-FL had sustained release effects under both leakage and non-leakage conditions， and PEG-Cur-FL had a smoother sustained release in artificial lung fluid， with release characteristics consistent with the Weibull model. The results of in vivo distribution showed that the drug concentration in the lung tissue of PEG-Cur-FL group was significantly lower than that of Cur- SLN-FL group during the same period after 1 hour of administration， while the drug concentration in the lung tissue at 4 to 48 hours was significantly higher than that of Cur-SLN-FL group during the same period （P＜0.05）； the plasma drug concentrations of the PEG-Cur-FL group at all time points from 0.25 to 12 hours were significantly lower than those of the Cur-SLN-FL group during the same period （P＜0.05）， and the drug concentrations in liver and kidney tissues were also lower than those of the Cur-SLN-FL group during the same period （P＜0.05）. CONCLUSIONS PEG-Cur-FL is prepared successfully； the inhalable micropowder has good inhalability and release performance； after administration through the trachea， the effective concentration of Cur in lung tissue can be increased， while reducing its plasma drug concentration and drug distribution concentration in non-target organs. |
| 期刊： | 2025年第36卷第19期 |
| 作者： | 李楠；王梓；郝迪；孔令钰；李旭 |
| AUTHORS： | LI Nan，WANG Zi，HAO Di，KONG Lingyu，LI Xu |
| 关键字： | 姜黄素；聚乙二醇；固体脂质纳米粒；吸入微粉；吸入给药；体外释放；组织分布 |
| KEYWORDS： | curcumin； polyethylene glycol； solid lipid nanoparticles； inhalable micropowder； inhalation administration； in |
| 阅读数： | 3 次 |
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