Preparation of celastrol-loaded albumin nanoparticles and their efficacy against rheumatoid arthritis
- VernacularTitle: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
- Author:
Hanyu YAN
1
;
Yongping ZHANG
1
;
Jian XU
1
;
Yao LIU
1
;
Guoqiong CAO
1
;
Zuhua WANG
1
;
Xinli SONG
1
;
Ling GUO
1
Author Information
1. School of Pharmacy/National Engineering Technology Research Center of Miao Medicine/Guizhou Engineering Technology Research Center for Processing and Preparation of Traditional Chinese Medicine and Ethnic Medicine，Guizhou University of Traditional Chinese Medicine，Guiyang 550025，China
- Publication Type:Journal Article
- Keywords:
celastrol-loaded albumin nanoparticles;
for- mulation technology;
physicochemical properties;
rheumatoid arthr itis
- From:
China Pharmacy
2022;33(21):2597-2602
- CountryChina
- Language:Chinese
-
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 .
