中国中药杂志2025，Vol.50Issue(15)：4263-4274,12.DOI:10.19540/j.cnki.cjcmm.20250331.301
黄芩苷-小檗碱复合物纳米晶肠溶微球的研制及其抗溃疡性结肠炎的药效学评价
Preparation of baicalin-berberine complex nanocrystal enteric microspheres and pharmacodynamic evaluation of ulcerative colitis treatment in rats
摘要
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.关键词
溃疡性结肠炎/黄芩苷/小檗碱/肠溶微球/体外释放Key words
ulcerative colitis/baicalin/berberine/enteric microspheres/in vitro release引用本文复制引用
黄小超,胡艺雯,沈鹏宇,蹇瑞鸿,祁东利,刘志东,皮佳鑫..黄芩苷-小檗碱复合物纳米晶肠溶微球的研制及其抗溃疡性结肠炎的药效学评价[J].中国中药杂志,2025,50(15):4263-4274,12.基金项目
天津市教委科研计划项目(2021ZD008) （2021ZD008）
