ABSTRACT
OBJECTIVE: To prepare luteolin-loaded Solutol hsl5/Poloxamerl88 mixed micelles, evaluate their pharmaceutical property and study their anti-tumor activity. METHODS: The luteolin-loaded mixed micelles were prepared by thin-film hydration method. The particle size was measured by laser granulometry, and the morphology was observed under transmission electron microscope (TEM). The in vitro release behavior was determined by the dialysis method. Cell toxicity and uptake assays were employed to evaluate the anti-tumor activity. The targeting effect was studied by fluorescence labeling. RESULTS: The prepared luteolin-loaded mixed micelles showed spherical and regular shape with an average particle size of 66.43 nm and its entrapment efficiency was more than 80%. The 12 h-accumulated release ratio in vitro was up to 97.42%. The cytotoxicity of luteolin-loaded mixed micelles on human lung adenocarcinoma cell line A549 was significantly stronger than that of free luteolin and the uptake rate was improved. After injecting DiR-loaded mixed micelles into nude mouse, the drug begun to accumulate in tumors after 2 h and reached the highest concentration at 6 h which was significantly higher than that in other tissues. There remained strong drug distribution in the tumors after 12 h. CONCLUSION: The Solutol hs15/Poloxamer188 mixed micelles have small particle size and high entrapment efficiency and can enhance cell toxicity and uptake with certain passive targeting effect. It is a promising delivery system for anti-tumor drug.