《Table 2–Pharmacokinetic parameters of formulations.》

《Table 2–Pharmacokinetic parameters of formulations.》   提示:宽带有限、当前游客访问压缩模式
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《The accelerated blood clearance phenomenon of PEGylated nanoemulsion upon cross administration with nanoemulsions modified with polyglycerin》


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aAREA under curve from time 0 to 60 min.bThe mean retention time from time 0 to 60 min.

For evaluating the effect of PG610-DSPE on the induction of the ABC phenomenon in rats,rats were treated with the 1%GE-B,3%GE-B,9%GE-B and 9%PE-B at 5μmol phospholipid/kg as the first dose respectively.7 d later,the rats were injected with the9%PE(5μmol phospholipid/kg).The result of Fig.3A showed that,the plasma concentrations of the second dose of the 9%PEdecrease.Compared with control group which pretreated with5%glucose,rats pretreated with the 1%GE-B induce the rapidly clearance of the 9%PE(AUC (0–60 min)values,5723.06±85.14 and1236.65±27.23μg/ml/min,respectively,**P<0.01,Table 2) .The decreasing extends from strong to weak are 1%GE>3%GE>9%GE(MRT (0–60)(min),19.45±1.54,22.48±2.12,23.49±2.76 min respectively) .This suggests that the ABC phenomenon is induced by the nanoemulsion coated with PG610-DSPE.This is the first report that the GE induces the ABC phenomenon of the second dose of the 9%PE.As shown in the Table 2,pharmacokinetic parameters reveal that rats pretreated with the 9%PE-B can induce stronger ABC phenomenon than the 1%GE-B(AUC (0–60 min)values,204.15±9.38 and 1236.65±27.23μg/ml/min,respectively) .The parameters between the control group and the group pretreated with the 1%GE-B are compared.The differences in parameters between these two groups are significant(**P<0.01)(Table 2) .The Fig.2B shows that the liver and spleen accumulations are increased due to the induction of the ABCphenomenon.As we all know,PEG endows the nanoparticles“stealth”.Some researchers think that the reason why the PEGylated nanoemulsion induces the ABC phenomenon is that the long lifetime of nanoparticles trigger the immune system[40].However,from the results of our work,the ABC phenomenon is also induced by the nanocarriers in short circulation.