Yang Fan, Shang Shang, Wu Kangli, Qi Mengfei, He Yifan, Zhang Yan, Shen Jiayan, Tong Ying, Xiang Yajinjing, Liu Jia, Wu Qing
School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, China.
School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, China.
Int J Biol Macromol. 2025 Jun;314:144339. doi: 10.1016/j.ijbiomac.2025.144339. Epub 2025 May 18.
Supercritical Fluid Extract of Angelica (ASFE) shows potential for treating ulcerative colitis (UC) and colorectal cancer. This study prepared ASFE-quaternized chitosan nanoemulsion (ASFE-QCSNE) using low-energy emulsification with quaternized chitosan as the carrier. The formulation was optimized via pseudo-ternary phase diagrams combined with D-optimal mixture design. The physicochemical properties of ASFE-QCSNE were characterized and evaluated, and its in vitro and in vivo anti-inflammatory activities were investigated. The optimized ASFE-QCSNE was identified as an oil-in-water (O/W) emulsion with a particle size of (23.94 ± 0.53) nm, polydispersity index (PDI) of (0.216 ± 0.02), and Zeta potential of (23.10 ± 0.74) mV. Transmission electron microscopy revealed spherical and uniformly distributed droplets. The encapsulation efficiency and drug loading were (96.10 ± 1.63) % and (2.69 ± 0.05) %, respectively. ASFE-QCSNE demonstrated favorable centrifugal and preliminary storage stability. In simulated gastric fluid and small intestinal fluid, the nanoemulsion maintained structural integrity, whereas the nanostructure was disrupted in simulated colonic fluid. This suggests that ASFE-QCSNE effectively protects active components in ASFE from gastrointestinal degradation and releases them in the colon. In vitro, ASFE-QCSNE inhibited NO secretion at concentrations of 400-800 μg/mL, demonstrating robust anti-inflammatory activity. In a dextran sulfate sodium (DSS)-induced UC mouse model, ASFE-QCSNE significantly alleviated UC symptoms, as evidenced by increased body weight, reduced disease activity index, improved survival rate, and elongated colon length. Histological analysis revealed intact colonic mucosal structure and reduced inflammatory cell infiltration. Immunohistochemistry indicated upregulated expression of tight junction proteins ZO-1 and Occludin, reinforcing intestinal barrier integrity. Serum cytokine levels showed decreased TNF-α and IL-1β and increased IL-10, consistent with its anti-inflammatory effects. In summary, ASFE-QCSNE exhibits promising therapeutic potential for UC, expanding the applications of ASFE in intestinal diseases.
当归超临界流体提取物（ASFE）显示出治疗溃疡性结肠炎（UC）和结直肠癌的潜力。本研究以季铵化壳聚糖为载体，采用低能乳化法制备了ASFE-季铵化壳聚糖纳米乳（ASFE-QCSNE）。通过伪三元相图结合D-最优混合设计对配方进行了优化。对ASFE-QCSNE的理化性质进行了表征和评价，并研究了其体外和体内抗炎活性。优化后的ASFE-QCSNE被鉴定为水包油（O/W）型乳液，粒径为（23.94±0.53）nm，多分散指数（PDI）为（0.216±0.02），Zeta电位为（23.10±0.74）mV。透射电子显微镜显示液滴呈球形且分布均匀。包封率和载药量分别为（96.10±1.63）%和（2.69±0.05）%。ASFE-QCSNE表现出良好的离心稳定性和初步的储存稳定性。在模拟胃液和小肠液中，纳米乳保持结构完整性，而在模拟结肠液中纳米结构被破坏。这表明ASFE-QCSNE能有效保护ASFE中的活性成分不被胃肠道降解，并在结肠中释放。在体外，ASFE-QCSNE在400-8......完整翻译内容请见：https://www.51test.net/show/11034883.html 。
请注意，由于文本较长，完整译文请参考链接内容。如果您还有其他需求，请随时告诉我。
