ABSTRACT
OBJECTIVE: To prepare puerarin-loaded PEG-PE nano-micelles and explore its tissue distribution in acute myocardial ischemia model mice. METHODS: Puerarin-loaded PEG-PE nano-micelles were prepared by thin-film hydration method. Sixty KM mice were randomly divided into two groups (30 in each group). Both were given puerarin-loaded PEG-PE nano-micelles at a dose of 20 mgkg-1. After 5 min of medication, the mice in one group were treated with ligation of coronary artery to establish acute myocardial ischemia, and the other one group was taken as the control. The animals were executed at 30, 60, 90, 120, 150 and 180 min, then the heart, liver, spleen, lung, and kidney were extracted. The content of puerarin in the organ tissue was determined by HPLC. RESULTS: The drug loading and drug encapsulation of puerarin-loaded PEG-PE nano-micelles were (5.8±1.3)% and (78.6±5.7)%, respectively, and the diameters and Zeta potential were 25 nm and -3 mV, respectively. The AUCs of tissue distribution of puerarin-loaded PEG-PE nano-micelles in the control group were in the sequence of liver>kidney>heart >spleen>lung>brain. While the AUCs of tissue distribution of PEGylated puerarin in acute myocardial ischemia model mice were in the sequence of liver≈heart>kidney>lung>spleen>brain. The AUCheart of puerarin-loaded PEG-PE nano-micelles in acute myocardial ischemia model mice was 1.9 times of that of the control mice (P<0.05). CONCLUSION: Puerarin-loaded PEG-PE nano-micelles show excellent drug loading capabilities. It has good heart-targeting property in early myocardial infarction area and can accumulate in the ischemic myocardium. This study provides important information for further development of prepamiceion.