Preparation，optimization and antibacterial activity of luteolin nanostructured lipid carriers / 中国药科大学学报

ABSTRACT

@#To prepare and optimize luteolin nanostructured lipid carriers (Lut-NLCs) and investigate their antibacterial activity in vitro. Lut-NLCs were prepared by hot melt emulsification-ultrasonic method. The solid lipid concentration (X1),liquid lipid concentration (X2) and surfactant concentration (X3) were used as independent variables,with the average particle size (Y1) and the encapsulation efficiency (Y2) as the dependent variables. The optimal formulation of Lut-NLCs was obtained through Box-Behnken experiment design. The microstructure of Lut-NLCs was observed by transmission electron microscopy(TEM). The in vitro release characteristics of Lut-NLCs were investigated. Furthermore, the in vitro antibacterial activities of luteolin and Lut-NLCs were compared. The formulation composition of Lut-NLCs was optimized as follows:the concentration of the solid lipid, liquid lipid and surfactant were 13.0 mg/mL,15.0 mg/mL,and 15.0 mg/mL,respectively. Three batches of Lut-NLCs were prepared with an average particle size of (210.4±17.3) nm,and an encapsulation efficiency of (88.4±1.2)%. Lut-NLCs were observed to be spheroidal,with a smooth surface and a uniform particle size distribution by TEM. The drug release profiles of Lut-NLCs showed a bursting release in the early stage and a slow and stable release in the later stage. Moreover, the cumulative release amount of drug reached 95% in 12 hours. The results of antibacterial circle experiment showed that the antibacterial effect of Lut-NLCs on Staphylococcus aureus and Escherichia coli was higher than that of luteolin raw materials. In this study,the formulation of Lut-NLCs prepared by simple preparation process is reasonable,and Lut-NLCs also exhibited the significant in vitro antibacterial activity. It is expected to be an effective way for external application of luteolin.