Preparation of baicalin-berberine complex nanocrystal enteric microspheres and pharmacodynamic evaluation of ulcerative colitis treatment in rats.
10.19540/j.cnki.cjcmm.20250331.301
- Author:
Xiao-Chao HUANG
1
;
Yi-Wen HU
1
;
Peng-Yu SHEN
1
;
Rui-Hong JIAN
1
;
Dong-Li QI
1
;
Zhi-Dong LIU
1
;
Jia-Xin PI
1
Author Information
1. State Key Laboratory of Chinese Medicine Modernization, Tianjin University of Traditional Chinese Medicine Tianjin 301617, China State Key Laboratory of Component-based Chinese Medicine, Tianjin University of Traditional Chinese Medicine Tianjin 301617, China Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine Tianjin 301617, China.
- Publication Type:Journal Article
- Keywords:
baicalin;
berberine;
enteric microspheres;
in vitro release;
ulcerative colitis
- MeSH:
Animals;
Colitis, Ulcerative/metabolism*;
Rats;
Nanoparticles/chemistry*;
Microspheres;
Male;
Berberine/administration & dosage*;
Flavonoids/administration & dosage*;
Rats, Sprague-Dawley;
Drugs, Chinese Herbal/administration & dosage*;
Humans;
Particle Size;
Tumor Necrosis Factor-alpha/immunology*;
Drug Liberation;
Drug Compounding
- From:
China Journal of Chinese Materia Medica
2025;50(15):4263-4274
- CountryChina
- Language:Chinese
-
Abstract:
To enhance the therapeutic efficacy of the baicalin-berberine complex(BA-BBR) in the treatment of ulcerative colitis(UC), BA-BBR nanocrystal microspheres(BA-BBR NC MS) were prepared using the dropping method. The microspheres were characterized in terms of morphology, particle size, differential scanning calorimetry(DSC), and powder X-ray diffraction(XRD). The release profiles of BA and BBR from the microspheres were measured, and the drug release mechanism was investigated. A rat model of UC was induced by 5% dextran sodium sulfate(DSS) and treated continuously for 7 days to evaluate the therapeutic effects of different formulations. The results showed that the prepared BA-BBR MS and BA-BBR NC MS were uniform gel spheres with particle sizes of(1.77±0.16) mm and(1.67±0.08) mm, respectively. After drying, the gels collapsed inward and exhibited a rough surface. During the preparation process, the BA-BBR nanocrystals(BA-BBR NC) were uniformly encapsulated within the microspheres. The release profiles of the microspheres followed a first-order kinetic model, and the 12-hour cumulative release of BA and BBR from BA-BBR NC MS was higher than that from BA-BBR MS. Compared with BA-BBR, BA-BBR NC, and BA-BBR MS, BA-BBR NC MS further alleviated UC symptoms in rats, most significantly reducing the levels of TNF-α, IL-1β, IL-6, and MPO, while increasing the level of IL-4 in colon tissues. These results indicate that BA-BBR NC MS, based on a "nano-in-micro" design, can deliver BA-BBR to the intestine and exert significant therapeutic effects in a UC rat model, suggesting it as a promising new strategy for the treatment of UC.
