Objective: To prepare a nano-carrier based on combining bacterial outer membrane vesicles (OMV) with three block polymer pluronic F127 (PEO100-PPO65-PEO100) (OMV-F127) and to investigate its immunological activity. Methods: Attenuated salmonella (sal) was cultivated. OMV were separated by centrifugal ultrafiltration or ultrasonication, and OMV-F127 was prepared by mechanical extrudation method. The protein contents and compositions were tested with BCA and SDS-PAGE; the morphology of OMV, F127 and OMV-F127 were observed with FM and TEM; the particle sizes and their zeta potential were determined with DLS. Mouse macrophage RAW246.7 cells were treated with OMV-F127 (50 μg/mL, 100 μg/mL) in vitro, and the concentrations of IL-12, TNF-α and IFN-γ in culture supernatant were measured with ELISA kits. Results: The contents of protein in separated OMV by centrifugal ultrafiltration and ultrasonication were 2.8 mg/mL and 2.7 mg/mL, respectively. SDS-PAGE showed the marker protein OmpF/C in OMV. Under the FM and TEM, ball-like structure of F127 and OMV-F127 was observed. Size analysis revealed that the diameters of OMV, F127 and OMV-F127 were 72±2 nm, 90±3 nm and 92±2 nm, respectively. ELISA tests revealed that OMV-F127 significantly stimulated the secretion of IL-12, TNF-α and IFN-γ in RAW246.7 cells. Conclusion: A nano-carrier based on bacterial outer membrane vesicles has been prepared, which can stimulate the secretion of cytokines and may have immunomodulatory effects.
目的: 设计制备三种瑞戈非尼环糊精包合物，以改善瑞戈非尼的溶解度、溶出度和生物利用度。
方法: 采用重结晶、饱和水溶液等方法对瑞戈非尼—环糊精包合物的制备方法进行研究，通过傅里叶红外光谱、热重分析、X射线粉末衍射、核磁共振、核欧佛豪瑟效应频谱等方法对瑞戈非尼—环糊精包合物进行结构分析。并采用SW620结肠癌细胞荷瘤裸鼠模型考察其体内抑瘤效果。
结果: 瑞戈非尼被环糊精包合后溶解性能明显改善，溶出度从大到小依次为：瑞戈非尼-β-环糊精包合物 > 瑞戈非尼—羟丙基-β-环糊精 > 瑞戈非尼-γ-环糊精包合物。优选包合及溶出效果最好的瑞戈非尼-β-环糊精包合物进行裸鼠体内抑瘤试验，结果表明，瑞戈非尼-β-环糊精包合物抑瘤效果比瑞戈非尼明显提高。
结论: 难溶性药物瑞戈非尼被环糊精包合后其溶解度和溶出度改善，从而提高瑞戈非尼的生物利用度。