首页|基于缓释递药系统的姜酮混合胶束构建及其评价

基于缓释递药系统的姜酮混合胶束构建及其评价

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目的:研究混合胶束包载姜酮后的药物性能以及对治疗非酒精性脂肪肝(NAFLD)的影响。方法:采用薄膜分散法制备姜酮/F68/F127/TPGS混合胶束(Z-TPGS-Ms),通过单因素试验筛选最优处方,观察胶束形态,测定粒径、包封率及载药量,考察胶束稳定性。通过体外释放实验和体内药动学考察Z-TPGS-Ms释放效果,并建立非酒精性脂肪肝细胞模型,考察抗NAFLD作用。结果:Z-TPGS-Ms粒径为(20。78±1。32)nm,包封率和载药量分别为(98。01%± 0。17%)和(6。47%±1。06%)。Z-TPGS-Ms稳定性良好,体外累积释放率明显高于原料药,实现姜酮在体内缓慢释放。与姜酮相比,Z-TPGS-Ms治疗NAFLD效果明显改善。结论:基于缓释递药系统制备的姜酮混合胶束稳定、均一、载药量高,可实现缓释递药,提高体外治疗NAFLD效果。
Preparation and Evaluation of Zingerone Mixed Micelles Based on Sus-tained-release Delivery System
Objective:To investigate the drug properties of mixed micelles encapsulating zingerone and their effects on the treatment of nonalcoholic fatty liver disease.Methods:Zingerone/F68/F127/TPGS mixed micelles(Z-TPGS-Ms)were prepared by thin film dispersion,and the optimal prescription was screened by univariate tests.Micelles were observed on aspects of morphology,particle size,encapsulation rate,drug load and stability.The release effects of Z-TPGS-Ms were investigated by release experiments in vitro and pharmacokinetics in vivo,and a non-alcoholic fatty liver(NAFLD)cell model was established to investigate the anti-NAFLD effects.Results:The particle size of Z-TPGS-Ms was(20.78±1.32)nm,the encapsulation rate and drug load were(98.01%±0.17%)and(6.47%±1.06%),respectively.Z-TPGS-Ms had good stabili-ty,the cumulative release rates were significantly higher than those of zingerone,and the micelles realized slow release of zingerone in vivo.The results of treatment of NAFLD showed that Z-TPGS-Ms had signifi-cantly improved effects on NAFLD compared with zingerone in vitro.Conclusion:Based on the sustained-release delivery system,stable and uniform zingerone mixed micelles with good encapsulation rate and drug load were successfully prepared,which achieved sustained-release drug delivery and improved in vitro treatment of NAFLD.

MicellesSustained releaseNon-alcoholic fatty liverZingerone

葛竹妹、李冉、顾晨露、商勋、赵小超

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宿迁市中医院 药学部,宿迁 223800

江苏大学 药学院,镇江 212000

盐城工业技术学院 药品与健康学院,盐城 224000

胶束 缓释 非酒精性脂肪肝 姜酮

宿迁市科技计划

K202201

2024

药学与临床研究
江苏省药学会

药学与临床研究

CSTPCD
影响因子:0.95
ISSN:1673-7806
年,卷(期):2024.32(2)
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