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姜黄素纳米胶束的制备、表征及抗酒精性肝病体外活性评价
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| 篇名： | 姜黄素纳米胶束的制备、表征及抗酒精性肝病体外活性评价 |
| TITLE： | Preparation and characterization of curcumin nanomicelles and evaluation of in vitro hepatoprotective activity against alcohol liver disease |
| 摘要： | 目的 制备并表征姜黄素纳米胶束（简称“Cur/mPEG-PBLA胶束”），并评价其抗酒精性肝病的体外活性。方法以聚乙二醇-聚天冬氨酸苄酯嵌段共聚物（mPEG-PBLA）为载体，采用透析法制备Cur/mPEG-PBLA胶束；观察其外观和显微形态，检测其粒径、多分散性指数、Zeta电位、包封率及载药量，并进行体外释放、pH稳定性、热稳定性、稀释稳定性、储存稳定性、血浆稳定性考察和溶血实验。以人肝癌细胞、正常肝细胞为对象，以Cur对照品溶液为参照，采用无水乙醇干预建立酒精性肝病细胞模型，评价Cur/mPEG-PBLA胶束对酒精性肝病的体外预防和改善作用。结果所制Cur/mPEG-PBLA胶束显淡黄色乳光，呈圆球形且分布均匀，平均粒径约140nm，多分散性指数＜0.3，Zeta电位为（－8.15±0.05）mV；包封率及载药量分别为（73.26±3.16）%、（4.87±0.42）%。Cur对照品在10h时的累积释放率接近80%；Cur/mPEG-PBLA胶束在8h时的累积释放率仅为28.94%，在48h时的累积释放率才达48.25%。Cur/mPEG-PBLA胶束的pH稳定性、热稳定性均优于Cur对照品溶液，稀释稳定性、储存稳定性、血浆稳定性均较好，且不会引发溶血现象。Cur对照品溶液和Cur/mPEG-PBLA胶束对2种细胞的酒精性损伤均有不同程度的体外预防和改善作用；且作用48h时，Cur/mPEG-PBLA胶束的上述作用均显著优于同质量浓度的Cur对照品溶液（P＜0.05）。结论Cur/mPEG-PBLA胶束可提高Cur的pH稳定性、热稳定性，延缓其释放速度，同时具有更强的体外抗酒精性肝病活性。 |
| ABSTRACT： | OBJECTIVE To prepare and characterize curcumin nanomicelles （hereinafter referred to as Cur/mPEG-PBLA micelles）， and to evaluate the in vitro hepatoprotective activity against alcohol liver disease （ALD）. METHODS Cur/mPEG-PBLA micelles were prepared with the dialysis method using methoxy-poly（ethylene glycol）-poly（β-benzyl-L-aspartate） （mPEG-PLGA） as the carrier. The appearance and microscopic morphology of Cur/mPEG-PBLA micelles were observed， and particle size， polydispersity index， Zeta potential， encapsulation efficiency and drug loading content were all detected. The in vitro release， pH stability， thermal stability， dilution stability， storage stability， plasma stability tests， and hemolysis experiments were all performed. The cell model of ALD was established with anhydrous ethanol intervention using human liver cancer cells and normal liver cells as objects， Cur reference solution as reference， to evaluate in vitro preventive and ameliorative effects of Cur/mPEG- PBLA micelles on ALD. RESULTS The prepared Cur/mPEG-PBLA micelles exhibited a pale-yellow milky light， with a spherical shape and uniform distribution. The average particle size was about 140 nm， and the polydispersity index was less than 0.3. Zeta potential was （－8.15±0.05） mV； the encapsulation efficiency was （73.26±3.16）%， and the drug loading content was （4.87± 0.42）%. The cumulative release of Cur reference substance was close to 80% at 10 h； the cumulative release of Cur/mPEG-PBLA micelles at 8 h was 28.94% and only 48.25% at 48 h. pH stability and thermal stability of Cur/mPEG-PBLA micelles were better than those of Cur reference solution； Cur/mPEG-PBLA micelles showed good dilution stability， storage stability and plasma stability， and would not cause hemolysis. Cur reference solution and Cur/mPEG-PBLA micelles had varying degrees of in vitro preventive and ameliorative effects on ALD in two types of cells； after 48 h of application， the above effects of Cur/mPEG-PBLA micelles were significantly better than those of Cur reference solution at the same mass concentration （P＜0.05）. CONCLUSIONS Cur/mPEG-PBLA micelles can improve pH stability and thermal stability of Cur， delayits degradation rate， and have better in vitro hepatoprotective activity against ALD. |
| 期刊： | 2024年第35卷第10期 |
| 作者： | 李禄辉；耿广平；徐磊；张志坤；蒲晓辉 |
| AUTHORS： | LI Luhui，GENG Guangping，XU Lei，ZHANG Zhikun，PU Xiaohui |
| 关键字： | 姜黄素；纳米胶束；酒精性肝病；预防；改善；体外活性 |
| KEYWORDS： | curcumin； nanomicelles； alcohol liver disease； prevention； improvement； in vitro activity |
| 阅读数： | 59 次 |
| 本月下载数： | 0 次 |
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