Preparation, characterization and brain targeting efficiency in mice of huperzine A-PLGA nanoparticle / 国际药学研究杂志

ABSTRACT

Objective: To prepare huperzine A (HupA) -poly (lactic-co-glycolic acid)(PLGA) nanoparticles (HupA-PLGA-NP) and to study their distribution property in mice. Methods: HupA-PLGA-NP were prepared by emulsion solvent evaporation method with PLGA as the carrier material, and the formulations were optimized by orthogonal design test. Nanoparticles were characterized by transmission electron microscopy (TEM) and laser particle diameter analyzer. Encapsulation efficiency (EE) was detected by HPLC. Distribution of nanoparticles in mice was evaluated by in nivo imaging system. Results The nanoparticles prepared by the optimal preparation were uniform spherical particles by TEM. Mean diameter, polydisperse index and Zeta potential of nanoparticles were (46.49 ± 1.37) nm, (0.31 ± 0.01) and (- 38.3 ± 1.56) mV, respectively. EE was (28.45 ± 1.52) %. The verifying experiments indicated that the repeatibility of the experiment was satisfactory. Results: of in vivo imaging confirmed that nanoparticles with the diameter of about 50 nm could cross blood-brain barrier into brain and had good sustained-release effect. Conclusion: HupA-PLGA-NP are found to have smaller particle size, sustained release of HupA and elevated drug concentration in brain.