Targeted liposomes for macrophages-mediated pulmonary fibrosis therapy

Wang, Yujie; Zhao, Fang; Wang, Xiangyu; Zuo, Haojie; Ru, Yiming; Cao, Xi; Wang, Yang

doi:10.1007/s13346-023-01508-3

Cited by 1 publication

(1 citation statement)

References 55 publications

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“…Recently, researchers have increasingly focused on the role of celastrol in weight loss through multiple pathway (e.g., leptin sensitivity, energy expenditure, and appetite control). − However, the potential for the clinical use of celastrol is largely limited by its toxicity and poor water solubility. Fortunately, several pharmaceutic strategies have been developed to circumvent these problems, including liposomes, − nanoencapsulation, polymer drugs, and polymeric micelles. , Various celastrol-loaded carriers greatly improve the bioavailability of celastrol and significantly reduce the adverse reactions of drugs. − …”

Section: Introductionmentioning

confidence: 99%

Cel-CS1K: A Celastrol–Chitosan Conjugate for Treating Diet-Induced Obesity

Zeng,

Tian,

Wang

et al. 2024

Chem. Res. Toxicol.

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Celastrol (Cel), extracted from Tripterygium wilfordii Hook, is a potential antiobesity drug, except for its adverse reactions in clinic. In the present study, we synthesized a promising celastrol–chitosan conjugate (Cel-CS1K) and evaluated its antiobesity effect and biological safety in diet-induced obese mice. Cel-CS1K showed higher drug loading (over 10 wt %), good solubility (18–19 mg/mL) in water, slower peak time (T max = 4 h), and clearance (T 1/2 = 8.97 h) in rats. Cel-CS1K effectively attenuated the cytotoxicity, celastrol-induced apoptosis, and fat accumulation of hepatocytes. Cel-CS1K reduced body weight and dietary amount same as the free Cel but with lower toxicity in blood, liver, and testis. Cel-CS1K improved the glucose homeostasis, HDL-C level, insulin sensitivity, and leptin sensitivity, while it significantly reduced the gene expression levels of LDL-C, TG, and TC in obese mice. Furthermore, the adipose-related gene expression levels provided evidence in support of a role for Cel-CS1K in losing weight by the multimode regulation. Overall, Cel-CS1K provides a translatable therapeutic strategy for the treatment of diet-induced obese humans.

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