目的 制备白及多糖/甘草酸共稳定的青藤碱纳米乳（sinomenine nanoemulsion，Sin-NE），并系统表征其性质，考察其稳定性与释药行为，进而通过体外实验评价其抗炎效果。方法 采用超声乳化法制备Sin-NE，观测其形貌、粒径、多分散指数（polydispersity index，PDI）、ζ电位，单因素实验和正交试验筛选最佳处方并进行处方验证，测量其pH值、浊度、黏度、包封率和载药量，进行稳定性考察，探究其体外释药行为。构建RAW264.7细胞炎症模型，验证Sin-NE对一氧化氮（nitric oxide，NO）、白细胞介素-6（interleukin-6，IL-6）、肿瘤坏死因子-α（tumor necrosis factor-α，TNF-α）的影响。结果 Sin-NE的最优处方为薏苡仁油用量3%，联合表面活性剂用量0.5%，白及多糖与甘草酸质量比1∶9，超声处理时间10 min，超声功率325 W。该处方所制备的Sin-NE平均粒径为（145.30±2.35）nm，ζ电位为（-39.51±0.43）mV，PDI为0.095±0.022，pH值为3.990±0.033。其包封率达到88.78%，载药量为26.14 mg/g。此外，Sin-NE在离心、储存、稀释及加热条件下均表现出良好的稳定性，并具备缓释特性，在体外能显著抑制炎症细胞中NO的释放，有效降低炎症因子IL-6和TNF-α的水平。结论 Sin-NE显著提高了青藤碱的生物利用度和抗炎活性，为新型中药纳米乳制剂的开发提供了实验依据。

Objective To prepare sinomenine nanoemulsion (Sin-NE) co-stabilized by Bletilla striata polysaccharide and glycyrrhizic acid, systematically characterize its properties, investigate its stability and drug release behavior, and further evaluate its anti-inflammatory effects through in vitro experiments. Methods The Sin-NE was prepared using the ultrasonic emulsification method. Its morphology, particle size, polydispersity index (PDI), and ζ potential were observed and determined. Optimal formulation parameters were screened via single-factor and orthogonal experiments, followed by formulation validation. pH value, turbidity, viscosity, encapsulation efficiency, and drug loading capacity were measured. Stability was investigated under centrifugation, storage, dilution, and heating conditions was evaluated, and in vitro drug release behavior was investigated. A RAW264.7 cell inflammation model was established to validate the effects of the Sin-NE on nitric oxide (NO), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α). Results The optimized formulation comprised 3% Coicis Semen oil, 0.5% combined emulsifiers, a 1∶9 mass ratio of Bletilla striata polysaccharide to glycyrrhizic acid, 10 min of ultrasonic treatment, and 325 W ultrasonic power. The resulting Sin-NE exhibited an average particle size of (145.30 ±2.35) nm, ζ potential of (-39.51 ±0.43) mV, PDI of 0.095 ±0.022, and pH value of 3.990 ±0.033. Encapsulation efficiency and drug loading capacity reached 88.78% and 26.14 mg/g, respectively. The nanoemulsion demonstrated excellent stability under centrifugation, storage, dilution, and heating conditions and displayed sustained-release characteristics. In vitro, it significantly inhibited NO release and effectively reduced IL-6 and TNF-α levels in inflamed cells. Conclusion The Sin-NE significantly enhances sinomenine’s bioavailability and anti-inflammatory activity, providing experimental evidence for developing novel traditional Chinese medicine nanoemulsion formulations.

R283.6

国家自然科学基金项目(82360852);贵州省科技计划项目(黔科合基础-ZK[2023]重点046);贵州省现代中药创制全省重点实验室(黔科合平台[2025]019);贵州中医药大学纳米药物技术研究中心(贵中医ZX合字[2024]070)