Objective: To prepare nanostructured lipid carriers modified with mPEG2000-DSPE(mPEG2000-DSPE-NMD-NLC) and investigate its properties and in vivo pharmacokinetics in rats. Method: mPEG2000-DSPE-NMD-NLC were prepared by melt ultrasonication method

morphology was observed by TEM

particle size

entrapment efficiency

drug loading and Zeta potential were determined

in vitro release was examined.Plasma concentrations of nimodipine at different time point in rats were determined by HPLC

with nimodipine injection as control

pharmacokinetics parameters of mPEG2000-DSPE-NMD-NLC in rats were calculated. Result: Prepared mPEG2000-DSPE-NMD-NLC showed spherical with uniform size and rounded surface;Particle size was about 85 nm

Zeta potential was (-12.77±0.15) mV

entrapment efficiency and drug loading were (97.66±0.45)% and (3.36±1.53)%

respectively;Cumulative release of mPEG2000-DSPE-NMD-NLC was 20.03% within 0-6 h

and 43.06% at 24 h.Pharmacokinetic parameters were as follows:t1/2=21.65 h

MRT=21.09 h

CL=557.30 mL·h-1·kg-1

AUC(0-t)=6 411.96 μg·h2·L-1. Conclusion: Particle size distribution of mPEG2000-DSPE-NMD-NLC was uniform

its showed obvious in vitro and in vivo sustained-release characteristic.This study could lay foundation for improving clinical efficacy of nimodipine.