Optimization of tilianin loaded solid lipid nanoparticles and its absorption and transport study in Caco-2 cell model / 中草药

ABSTRACT

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.