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bioRxiv · 10.1101/620898

Preparation and pharmacokinetics of genistein MePEG-PLGA copolymer micelles

Smith, J.·Swartz, M.
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Abstract

In this report, we demonstrated a novel technique to prepare genistein (GEN) MePEG-PLGA copolymer micelles. Initial stability and pharmacokinetic behavior in rats after intravenous administration were investigated. The micelles were prepared by modified self-emulsifying solvent evaporation method. The morphology, encapsulation efficiency, drug loading, particle size and Zeta potential were investigated. The release behavior was investigated by dynamic membrane dialysis technique. The micelles were stored in a refrigerator at 4 {degrees}C, and samples were taken after 1 d, 10 d, 1 month, 3 months, and 6 months, and the encapsulation efficiency and drug loading were examined. The GEN micelles were injected into the tail vein of healthy rats. The blood concentration of GEN in rats was determined by HPLC. The plasma concentration data was processed by DAS 2.0 software. The main pharmacokinetic parameters were statistically analyzed by SPSS 17.0 software. Results The encapsulation efficiency of the prepared micelles was (84.43+/-2.93) %, the drug loading was (2.63+/-0.91) %, and the particle size was (63.75+/-4.12) nm. The release behavior of GEN micelles was in line with the Weibull model. The 6-month leakage rate of GEN micelles was 2.45%, and the drug loading decreased by 0.18%. The main pharmacokinetic parameters AUC0-t after GEN micelles and GEN emulsion 40 mg{middle dot}kg-1 were injected into the tail vein of rats. They were (99.46+/- 4.77) mg {middle dot} L-1 {middle dot}h and (57.51+/-1.37) mg{middle dot}L-1 {middle dot}h, and t1/2 were (7.48+/-1.15)h and (4.95+/- 1.15)h, respectively, and Cmax was (16.03+/-1.20) mg{middle dot}L-1 and (16.73+/-1.10) mg{middle dot}L-1, CL are (0.36+/-0.02) L{middle dot}h-1 {middle dot}kg-1 and (0.67+/-0.02)L{middle dot}h-1 {middle dot}kg-1.

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Smith, J., Swartz, M.. 2019-04-27. Preparation and pharmacokinetics of genistein MePEG-PLGA copolymer micelles. https://doi.org/10.1101/620898

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