目的 制备并优化田蓟苷固体脂质纳米粒（T-SLNs），对其理化性质及体外吸收和转运进行考察。方法 采用高剪切乳化超声法制备了T-SLNs，利用星点设计-效应面法（CCD-RSM）对其制备工艺进行了优化，并对其平均粒径、多分散性指数（PDI）、Zeta电位、形态、包封率及体外释放等特性进行了考察，使用Caco-2细胞模型模拟小肠上皮细胞，对T-SLNs在Caco-2细胞中的吸收和转运进行了考察。结果 T-SLNs的最佳制备工艺：药脂比（质量比）0.11，大豆卵磷脂与脂质质量比1.26，聚山梨酯-80用量50.5 mg/mL，所制备的T-SLNs外观呈球形或类球形，大小相近，分散均匀，平均粒径为（86.40±0.62）nm，PDI为0.165±0.080，Zeta电位为（-24.2±0.6）mV，包封率为（89.81±1.07）%，在磷酸盐缓冲溶液（pH 6.8）中48 h累积释放率为（98.72±1.57）%。T-SLNs在Caco-2细胞模型中的吸收和转运均高于田蓟苷组。结论 高剪切乳化超声法制备T-SLNs的工艺稳定可行，制备的T-SLNs具有较小的粒径和较高的包封率，相同浓度下T-SLNs在Caco-2细胞模型中的吸收和转运均高于田蓟苷组。

Objective To prepare and optimize tilianin loaded solid lipid nanoparticles (T-SLNs), and investigate the physicochemical properties, absorption and transport behavour of T-SLNs in vitro. Methods T-SLNs were prepared by high shear homogenization followed by ultrasonication and optimized by central composite design and response surface methodology. In the study, the physicochemical properties of T-SLNs including size, polydispersity (PDI), Zeta potential, shape, entrapment efficiency and release profile in vitro were investigated, the absorption and transport behavour of T-SLNs in Caco-2 cell model were also measured. Results The optimum formulation of T-SLNs consisted of: drug/lipid of 0.11, soy lecithin/lipid of 1.26, and content of tween-80 was 5.05%. The prepared T-SLNs were spherical and uniform with the mean particle diameter at (86.40±0.62) nm, PDI (0.165±0.080) and Zeta potential of (-24.2±0.6) mV, respectively. The average EE was (89.81±1.07)%, and the release in vitro showed that tilianin was released about (98.72±1.57)% in 48 h. Besides, the absorption and transport assays of T-SLNs in Caco-2 cells model indicated that T-SLNs had a higher absorption and transport than tilianin. Conclusion The method of high shear homogenization followed by ultrasonication is suitable for T-SLNs preparation. The optimal T-SLNs have a smaller particle size and high EE. Moreover, in the same concentration of tilianin, the absorption and transport amounts of T-SLNs in Caco-2 cell model were higher than tilianin.

自治区高技术研究发展计划（201517109）；自治区研究生科研创新项目（XJGRI2015053）