Qian PENG, Xi LAN, Jing-Yi CHEN, Jing-Yang LI, Li CHEN, Li ZHANG, Ling ZHANG; Preparation and Evaluation of Baicalin-Loaded PLGA Microspheres In Vitro and In Vivo; Advanced Nano-Bio-Materials and Devices; 2017:1(4):191-203

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Here, the Baicalin-loaded PLGA microspheres (BC-MS) were prepared, and their properties in vitro and in vivo were evaluated. The microspheres were prepared using the solvent evaporation method based on O/W emulsion. The HPLC method was established in the determination of the content of baicalin in the microspheres. The surface and particle size were observed by the inverted microscopy, and the characteristics of in vitro release of BC-MS were investigated by dynamic dialysis method. After that, the microspheres were in vivo evaluated in rats. It was observed that the microspheres had an average particle size of 1.89μm, the drug loading was 12.79%, and the encapsulation rate was 85.40%. Moreover, the microspheres were spherical in shape and smooth surface with a uniform distribution. The release profiles of BC-MS agreed with Ritger-Peppas equation. The plasma concentration-time curves of BC-MS were fitted with two-compartment model. The results of pharmacodynamics in rats showed that: the elimination half-life of baicalin solution (BC-S) and Baicalin-loaded PLGA microspheres (BC-MS) were respectively 1.27 h and 258.98 h, mean residence time (MRT) were 0.88 h and 373.01 h, respectively. As the above result shows, BC-MS has the slow-release effect. Thus, the Baicalin-loaded PLGA microspheres have been successfully prepared.