Pharmacokinetics of emodin liposomes mixed with different forms of PEG in rats

SHEN Li-ping; YAN Dong-xue; ZHAO Shan-ke; YIN Mei-lin; SUN Yu-qi

Abstract：Objective:To study the pharmacokinetics of emodin liposomes mixed with mPEG2000,DSPEPEG2000 or Chol-PEG2000 in rats.Methods:mPEG-Emo-Lip,DSPE-Emo-Lip and Chol-Emo-Lip were prepared by film-ultrasonic dispersion.The emodin liposomes were injected to rats through caudal vein.HPLC method was established to determine the concentrations of emodin in plasma samples,and then the kinetic equations were used to fit the pharmacokinetics of emodin liposomes in rats.The long-circulation effects of the three forms of emodin liposomes were compared.Results:Compared to Emo-Lip,the elimination half-lives (t1/2) of mPEG-Emo-Lip,DSPE-Emo-Lip and Chol-Emo-Lip were extended by (2.29 ± 0.32),(4.25 ± 0.76) and (3.36 ± 0.47) folds,the mean residence time (MRT) was increased by (1.72 ± 0.26),(3.52 ± 0.61) and (2.42 ± 0.31) folds,the areas under the concentration-time curve (AUC) were increased by (2.23 ± 0.06),(5.30 ± 0.28) and (3.83 ± 0.34) folds,and the clearance (CL) in plasmas was decreased by (0.44 ±0.01),(0.19 ±0.01) and (0.26 ± 0.02) folds,respectively.Conclusion:Emodin liposomes mixed with mPEG2000,DSPE-PEG2000 or Chol-PEG2000 can prolong the t1/2 and MRT,which demonstrate long-circulation effects.The DSPE-Emo-Lip shows more obvious long-circulation effect.