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叶酸修饰的粉防己碱壳聚糖-硬脂酸纳米胶束的制备、表征及体外抗炎活性考察
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| 篇名： | 叶酸修饰的粉防己碱壳聚糖-硬脂酸纳米胶束的制备、表征及体外抗炎活性考察 |
| TITLE： | Preparation，characterization and in vitro anti-inflammatory activity of tetrandrine-loaded chitosan-stearic acid nano micelles modified with folic acid |
| 摘要： | 目的 制备叶酸（FA）修饰的粉防己碱（TET）壳聚糖（CS）-硬脂酸（SA）纳米胶束（简称“FA-CS-SA/TET纳米胶束”），并进行表征和体外抗炎活性考察。方法采用超声法制备FA-CS-SA/TET纳米胶束，以包封率（EE）、载药量（DL）、粒径的综合评分为评价指标，FA-CS-SA与TET质量比、超声功率和超声次数为考察因素，根据正交实验确定最优制备工艺并验证；对以最优工艺制备的FA-CS-SA/TET纳米胶束进行表征，并考察其体外释放性能。以RAW264.7细胞为实验对象，考察其体外抗炎活性。结果最优制备工艺为FA-CS-SA与TET质量比2∶1，超声功率200W，超声200次。以最优工艺制备的FA-CS-SA/TET纳米胶束的EE为（98.86±0.30）%，DL为（28.57±0.34）%，平均粒径为（227.0±9.4）nm，多分散性指数为0.42±0.04，Zeta电位为（12.6±2.3）mV；该纳米胶束呈类圆形且分布均匀，其在0.5%十二烷基硫酸钠溶液中释放较快，72h内的累积释放度为（79.49±3.43）%，且其抗炎作用强于TET原料药。结论本研究成功制备了FA-CS-SA/TET纳米胶束，其载药性能良好，粒径均匀，且具有较好的体外抗炎活性。 |
| ABSTRACT： | OBJECTIVE To prepare tetrandrine （TET）-loaded chitosan（CS）-stearic acid （SA） nano micelles modified with folic acid （FA）（ FA-CS-SA/TET nano micelles）， characterize them and study the anti-inflammatory effect in vitro. METHODS FA- CS-SA/TET nano micelles were prepared by ultrasonic method； the preparation technology was optimized by orthogonal test and validation test was also performed with the mass ratio of FA-CS-SA to TET， ultrasound power and ultrasound times as the factors， using the comprehensive score of entrapment efficiency （EE）， drug loading （DL） and particle size as evaluation index. FA-CS-SA/ TET nano micelles prepared by the optimal technology were characterized， and their release performance in vitro was investigated. RAW264.7 cells were used as subjects to investigate their anti-inflammatory activity in vitro. RESULTS The optimal preparation technology included that the mass ratio of FA-CS-SA to TET was 2∶1， ultrasonic power was 200 W， and the ultrasonic frequency was 200 times. The parameters of FA-CS-SA/TET nano micelles prepared by optimized technology included that EE was （98.86± 0.30）%， DL was （28.57±0.34）%， the average particle size was （227.0±9.4） nm， polydispersity index was 0.42±0.04， and the Zeta potential was（12.6±2.3）mV， respectively. The nano micelles were uniform in appearance and round in shape. The nano micelles were released quickly in 0.5% sodium dodecyl sulfate solution， with a cumulative release rate of （79.49±3.43）% within 72 hours， and its anti-inflammatory effect was stronger than that of TET raw materials. CONCLUSIONS FA-CS-SA/TET nano micelles are prepared successfully in the study， with good drug loading performance， uniform particle size， and good in vitro anti-inflammatory activity. |
| 期刊： | 2024年第35卷第08期 |
| 作者： | 薛飞；杨岚；常金花；刘沛；王汝兴 |
| AUTHORS： | XUE Fei，YANG Lan，CHANG Jinhua，LIU Pei，WANG Ruxing |
| 关键字： | 粉防己碱；纳米胶束；制备工艺；表征；抗炎活性；释放度 |
| KEYWORDS： | tetrandrine； nano micelles； preparation techno- |
| 阅读数： | 4 次 |
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