Preparation and brain distribution of NMD/TMP-loaded PLGA nanoparticles / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare nimodipine/tetramethylpyrazine-loaded poly[poly (lactic-co-glycolic acid), PLGA] dual-drug nanoparticles (nimodipine/tetramethylpyrazine-PLGA-nanoparticles, NMD/TMP-PLGA-NPs), and investigate the in vitro release behavior and brain distribution. METHODS: NMD/TMP-PLGA-NPs were prepared by optimized emulsion solvent evaporation method with PLGA as a carrier material; the morphology of NMD/TMP-PLGA-NPs was observed by transmission electron microscope; the mean particle size, particle size distribution and Zeta potential were measured by laser particle size analyzer; the entrapment efficiency and drug loading were measured by ultracentrifugation; the in vitro release behavior was studied by dialysis; the brain distribution was compared with NMD-suspension and NMD-PLGA-NPs. RESULTS: The NMD/TMP-PLGA-NPs were spherical; the mean particle size, particle size distribution and Zeta potential of NPs were (631.60±3.20) nm, (0.097±0.007), (-29.25±1.87) mV, respective-ly. The entrapment efficiency and drug loading of NMD were (76.25±1.18)% and (1.24±0.01)%, while those of TMP were (39.30±1.00)% and (6.34±0.11)%, respectively. The profiles of in vitro release had the features of sustained release. The ALC0→t of NMD-suspension, NMD-PLGA-NPs and NMD/TMP-PLGA-NPs were 0.2683, 0.4596 and 0.8815 μg·min·mL-1, and the addition of TMP promoted the reach of highest brain concentration. CONCLUSION: NMD/TMP-PLGA-NPs are prepared successfully and show sustained-release in vitro, and the distribution of NMD into brain was increased significantly with the addition of TMP.