Objective: To prepare and characterize poly(lactic-co-glycolic acid) (PLGA)-crebanine nanoparticles (PLGA-Cre-NPs)

and evaluate its in vitro release. Method: PLGA-Cre-NPs was prepared by emulsion-solvent diffusion method with PLGA as carrier material.Central composite design-response surface methodology was applied to optimize the preparation procedure of the nanoparticles based on the evaluation indexes of encapsulation rate

particle size and polydispersity index (PDI).The in vitro release kinetics of the nanoparticles was investigated by dynamic dialysis system. Result: The optimized preparation procedure was as follows:volume of organic phase-aqueous phase of 3:10

acetone-ethanol (8:2)

PLGA amount of 90 mg.The encapsulation rate of PLGA-Cre-NPs was (84.69±2.54)% with the particle size of (155.3±14.2) nm and PDI of 0.095±0.018

and it showed a regular spherical structure by scanning electron microscopy.Meanwhile

the release profile of PLGA-Cre-NPs could be well described by two phase dynamic equation

0-24 h was closer to Weibull equation

24-168 h was closer to Higuchi equation

and its half life (t1/2) was 18.06 h

the cumulative release rate was 78.77% at 168 h. Conclusion: PLGA-Cre-NPs has high encapsulation rate and uniform size

which will be expected to become a sustained-release preparation.