Preparation, characteristic and in vivo study of H102 loaded PEG-PLGA nanoparticles / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare H102 loaded PEG-PLGA nanoparticles (H102-NP) and investigate its properties in vitro and in vivo. METHODS: Orthogonal design was used to optimize the formulation. The nanoparticles were characterized in terms of morphology, size, Zeta potential, drug encapsulation efficiency, in vitro release and stability. H102 concentrations in plasma and brain following tail vein injection of H102-NP in mice were measured by LC-MS. RESULTS: H102-NP were spherical and of regular size. The average size, Zeta potential and encapsulation efficiency of H102-NP were found to be around 137 nm, -38 mV and 64%. The cumulative release of H102-NP in pH 7.4 PBS and plasma at 12 d is 93% and 95%, respectively. Incubated in plasma and brain homogenate at 37°C for 12 h, the degradation of H102 encapsulated in nanoparticles was only 5%. Compared with H102 solution which was eliminated rapidly in blood with low concentration in brain, H102-NP was eliminated slowly in blood with higher concentration and longer duration in brain after intravenous administered in mice. The AUC of H102-NP was 245 times and 11 times higher in plasma and brain than that of H102 solution. CONCLUSION: H102-loaded nanoparticles are successfully prepared with good properties in vitro and in vivo, which showed a prospect for the treatment of Alzheimer's disease.