目的 制备灵薏方多组分微乳并对其抗肺癌活性进行研究。方法 以灵芝多糖和薏苡仁多糖水溶液为水相,薏苡仁油为油相,荷载灵芝三萜,采用水滴定法制备灵薏方多组分微乳,测定其粒径、Zeta电位,并考察其稳定性。以Lewis荷瘤小鼠抑瘤率、体质量变化、免疫器官(肝、脾和胸腺)指数以及血浆中肿瘤坏死因子-α(TNF-α)和白细胞介素-6(IL-6)水平为考察指标,结合肿瘤组织病理切片和TUNEL凋亡原位检测,评价灵薏方多组分微乳的抗肺癌活性。结果 制备所得微乳形态圆整,平均粒径为(69.92±8.43)nm,多分散指数(PDI)为0.060±0.008,Zeta电位为(-11.30±1.34)mV。微乳组抑瘤率(57.25%)显著高于混悬液组(45.89%),免疫器官指数和血浆中TNF-α和IL-6水平显著升高,肿瘤组织病理切片和TUNEL凋亡原位检测显示微乳组抗肿瘤效果显著高于混悬液组。结论 灵薏方多组分微乳具有较好的抗肺癌活性。

Objective To prepare Lingyi Formula multicomponent microemulsion and evaluate its anti-lung cancer activity. Methods Lingyi Formula multicomponent microemulsion was prepared by aqueous titration method using polysaccharides solution of Ganoderma lucidum and Coix lachryma-jobi var. ma-yuen as aqueous phase and coix seed oil as oil phase, loading ganoderma triterpenes. The average particle size, Zeta potential, and stability were detected. The results of antitumor efficacy including tumor inhibitory rate, body weight change, immune organ index, and concentration of TNF-α and IL-6 were investigated. Besides, pathological section of tumor tissue and TUNEL labeling were conducted subsequently. Results The prepared microemulsion displayed spherical surface with mean droplet size of (69.92 ± 8.43) nm, polydispersity (PDI) of 0.060 ± 0.008, and Zeta potential of (-11.30 ± 1.34) mV. Tumor inhibitory rate of microemulsion (57.25%) was significantly higher than that of suspension (45.89%), immune tissue index as well as the concentration of TNF-α and IL-6 were increased significantly. TUNEL labeling and pathological section of tumor tissue showed that the antitumor activity of microemulsion was significantly effective compared with that of suspensions. Conclusion Lingyi Formula multicomponent microemulsion has a good anti-lung cancer activity.

国家自然科学基金资助项目(81373979);江苏省中医药领军人才项目(LJ200913);江苏省自然科学基金资助项目(BK20141058)