ABSTRACT
OBJECTIVE： To prepare insoluble anti-tumor drug-loading polymer micelles， and to increase inhibitive effect of insoluble anti-tumor drug. METHODS： Chitosan （CSO） and stearic acid （SA） were used to prepare blank micelles （CSO-SA）， then modified with mPEG and folic acid （FA） to prepare PEG-CSO-SA and FA-PEG-CSO-SA. Characteristic functional groups of CSO-SA， PEG-CSO-SA and FA-PEG-CSO-SA were detected by infrared spectroscopy. The morphology of micelles was observed by transmission electron microscopy. The particle size and Zeta potential of micelles were measured by laser particle size analyzer. Osthole （OST） was used as the model drug and drug-loading micelles （FA-PEG-CSO-SA/OST） were prepared by dialysis. MTT assay was used to detect the inhibitory rate of FA-PEG-CSO-SA， OST solution and FA-PEG-CSO-SA/OST to human liver cancer cell HepG2. Half inhibitory concentration （IC50） was calculated. RESULTS： FA-PEG-CSO-SA was successfully prepared. CSO-SA， PEG-CSO-SA， FA-PEG-CSO-SA were oval in shape； particle sizes were （96.01±5.99）， （112.93±1.06）， （216.01±4.76） nm （n＝3） and Zeta potentials were （39.30±1.75）， （38.03±2.91）， （15.17±2.10） mV （n＝3）， respectively. Encapsulation efficiency and drug-loading amount of OST in FA-PEG-CSO-SA were （84.47±2.07）％ and （16.01±0.90）％ （n＝3）， respectively. The inhibition rates of FA-PEG-CSO-SA to HepG2 cells were＜20％. IC50 of OST solution and FA-PEG-CSO-SA/OST to HepG2 cells were （62.08±5.21）， （27.49±0.50） μg/mL （n＝3）， respectively. CONCLUSIONS： Prepared FA-PEG-CSO-SA can significantly increase inhibitive effect of insoluble drug OST to HepG2 cells， and it is expected to become a new anti-tumor drug carrier.
ABSTRACT
Objective: To observe the relationship between 1h, 2h post-load plasma glucose (PG) elevation and carotid intima-media thickness (CIMT) in healthy population. Methods: The healthy subjects from normal physical examinations in our hospital from 2013-09 to 2015-05 were selected and oral glucose tolerance test (OGTT) was conducted in them, plasma levels of fasting glucose (FPG), 1hPG and 2hPG were monitored. Finally, 482 subjects with normal fasting glucose, without diabetes were enrolled and divided into 4 groups:①Normal glucose tolerance (NGT) group,n=201,②1hHPG group, the subjects with 1h post-load high and 2h post-load normal glucose,n=83,③2hHPG group, the subjects with 1h post-load normal and 2h post-load high glucose,n=101 and④1hHPG/2hHPG group,n=97. The gender, age, BMI, blood pressure and lipid levels in all subjects were recorded, CIMT was evaluated by Doppler ultrasound; the relationship between 1hHPG, 2hHPG and CIMT were analyzed. Results:①The gender, age, BMI, systemic blood pressure (SBP), DBP and the levels of TC, TG, LDL-C were similar among 4 groups,P>0.05.②For CIMT at both side, both bifurcations and both internal carotid arteries, 1hHPG/2hHPG group was higher than those in 1hHPG group and 2hHPG group; 1hHPG group was higher than 2hHPG group; CIMT in above 3 groups were all higher than NGT group, allP Conclusion: Abnormal 1hHPG and 2hHPG were related to increased CIMT.