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雷公藤红素白蛋白纳米粒的制备及抗类风湿性关节炎药效评价
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| 篇名： | 雷公藤红素白蛋白纳米粒的制备及抗类风湿性关节炎药效评价 |
| TITLE： | Preparation of celastrol-loaded albumin nanoparticles and their efficacy against rheumatoid arthritis |
| 摘要： | 目的 制备雷公藤红素白蛋白纳米粒（CLT-AN），并考察其体内抗类风湿性关节炎（RA）活性。方法采用超声法制备CLT-AN，以粒径、分散指数（PDI）和稳定性为评价指标，以CLT投药量、大豆油用量和超声功率为考察因素，通过单因素实验优化处方工艺。利用透射电镜、激光粒度测定仪等考察CLT-AN的理化性质，并研究其体外稳定性和体外释放特性。构建佐剂诱导关节炎大鼠模型，考察CLT-AN对模型大鼠关节肿胀、血清中炎症因子[肿瘤坏死因子α（TNF-α）和白细胞介素1β（IL-1β）]水平以及关节组织病理状态的影响。结果优化的处方为CLT6.5g、大豆油45mg、超声功率490W、超声时间8min。按最佳处方制备的CLT-AN外观形态圆整，平均粒径为（96.8±1.1）nm，PDI为0.174±0.020，Zeta电位为（－18.6±1.7）mV，包封率为（94.61±0.46）%，载药量为（2.42±0.21）%。在室温条件下，CLT-AN储存5d内的粒径、PDI、Zeta电位和包封率均无显著变化。CLT-AN体外释放缓慢，72h的累积释放量可达到73.56%；与游离CLT相比，CLT-AN可明显抑制模型大鼠的关节肿胀，降低其血清中TNF-α、IL-1β水平，并且显著改善炎症关节组织的病理状态。结论超声法制备的CLT-AN粒径适中、稳定性良好，具有显著的缓释特征和优良的抗RA活性。 |
| ABSTRACT： | OBJECTIVE To prepare celastrol -loaded albumin nanoparticles （CLT-AN），and to investigate their activity against rheumatoid arthritis （RA）in vivo . METHODS CLT-AN was prepared by ultrasonic method . The formulation technology was optimized by single -factor test by taking particle size ，polydispersity index （PDI）and stability as indexes ，with the dosage of CLT ， the dosage of soybean oil and the ultrasonic power as factors . The physical and chemical properties of CLT -AN were investigated by transmission electron microscopy （TEM）and laser particle size analyzer ；in vitro stability and release profile were studied . A rat model of adjuvant -induced arthritis was constructed to investigate the effects of CLT -AN on joint swelling ，the levels of serum inflammatory factors [tumor necrosis factor α（TNF-α）and interleukin -1β（IL-1β）] and pathological state of joint tissue . RESULTS The optimized formulation was CLT 6.5 g，soybean oil 45 mg，ultrasonic power 490 W，ultrasonic time 8 min. CLT- AN prepared by the best formulation showed uniform and spherical morphology . Its particle size ，PDI，Zeta potential were （96.8± 1.1）nm，0.174±0.020，and（－18.6±1.7）mV，respectively. The encapsulation efficiency and drug -loading efficiency were （94.61±0.46）% and（2.42±0.21）%. There were no significant changes in particle size ，PDI，Zeta potential and encapsulation efficiency of CLT -AN within 5 days of storage at room temperature . CLT-AN was slowly released in vitro ，and the cumulative release reached 73.56% in 72 h. Compared with CLT ，CLT-AN could significantly inhibit the joint swelling of model rats ，reduced the levels of inflammatory factors TNF -α and IL -1β in serum ，and improved the pathological state of inflammatory joint tissue . CONCLUSIONS CLT-AN prepared by ultrasonic method has the appropriate particle size ，good stability ，significant sustained - release characteristics ，and excellent therapeutic efficacy against RA . |
| 期刊： | 2022年第33卷第21期 |
| 作者： | 闫汉语，张永萍，徐剑，刘耀，曹国琼，汪祖华，宋信莉，郭玲 |
| AUTHORS： | YAN Hanyu，ZHANG Yongping，XU Jian，LIU Yao，CAO Guoqiong，WANG Zuhua，SONG Xinli，GUO Ling |
| 关键字： | 雷公藤红素白蛋白纳米粒；处方工艺；理化性质；类风湿性关节炎 |
| KEYWORDS： | celastrol-loaded albumin nanoparticles ；for- mulation technology ；physicochemical properties ；rheumatoid arthr itis |
| 阅读数： | 199 次 |
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