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Novel Carboxylated Chitosan-Based Triptolide Conjugate for the Treatment of Rheumatoid Arthritis.

Authors :
Zhang, Lan
Yan, Min
Chen, Kun
Tian, Qikang
Song, Junying
Zhang, Zijuan
Xie, Zhishen
Yuan, Yong
Jia, Yaquan
Zhu, Xin
Zhang, Zhenqiang
Wu, Xiangxiang
Zeng, Huahui
Source :
Pharmaceutics; Mar2020, Vol. 12 Issue 3, p202, 1p
Publication Year :
2020

Abstract

A new platform for triptolide (TP) delivery was prepared by conjugating TP to a carboxylmethyl chitosan (CMCS). Compared with the natural TP, the TP-conjugate (TP-CMCS) containing TP of ~5 wt% exhibited excellent aqueous solubility (>5 mg/mL). Results of in vitro experiments showed that TP-CMCS could relieve TP-induced inhibition on RAW264.7 cells and apoptosis, respectively. Compared with the TP group, TP-CMCS could effectively alleviate the toxicity injury of TP and decreased the mortality rate of the mice (p < 0.05). TP-CMCS did not cause much damage to the liver (AST and ALT) and kidney (BUN and CRE) (p < 0.05). After administration, the levels of IL-6, IL-1β, and TNF-α decreased, and the arthritis detumescence percentages increased significantly, and the bony erosion degree was distinctly decreased in the TP-CMCS groups and TP group. Our results suggested that TP-CMCS was a useful carrier for the treatment of RA, which enhanced aqueous solubility of free TP and reduced drug toxicity in vitro and in vivo. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
19994923
Volume :
12
Issue :
3
Database :
Complementary Index
Journal :
Pharmaceutics
Publication Type :
Academic Journal
Accession number :
142495504
Full Text :
https://doi.org/10.3390/pharmaceutics12030202