Yan F, Tang S, Fu Q
Department of Oncology, Changhai Hospital of Shanghai, Shanghai, People's Republic of China.
Arzneimittelforschung. 2012 Apr;62(4):176-80. doi: 10.1055/s-0031-1299745. Epub 2012 Jan 23.
Paclitaxel(PTX)-loaded microspheres composed of poly(D,L-lactide-co-glycolide) (PLGA) were prepared by an O/W emulsion solvent evaporation method. This study was designed to investigate the preparation, in vitro release, in vivo pharmacokinetics and tissue distribution of a PTX-loaded microspheres system. Microspheres are characterized according to drug loading, size and shape. With a dynamic light scattering sizer and a transmission electron microscopy, it is shown that the PTX-loaded microspheres had a mean size of approximately 10.24 µm with narrow size distribution and a spherical shape. The in vitro release profiles indicate that the release of PTX from the microspheres exhibit a sustained release behavior. A similar phenomenon is observed in a pharmacokinetic study in rats, in which AUC of the microspheres formulation were 3.7-fold higher than that of PTX injection. The biodistribution study in mice showed that the PTX-loaded microspheres not only decreased drug uptake by liver, but also increased distribution of drug in lung. These results suggest that PTX-loaded microspheres may efficiently load, protect and retain PTX in both in vitro and in vivo environments, and could be a useful drug carrier for i. v. administration of PTX.
采用水包油乳液溶剂蒸发法制备了聚（D，L-丙交酯-共-乙交酯）（PLGA）负载紫杉醇（PTX）的微球。本研究旨在考察PTX负载微球系统的制备、体外释放、体内药代动力学及组织分布。微球根据载药量、大小和形状进行表征。通过动态光散射粒度仪和透射电子显微镜显示，PTX负载微球的平均大小约为10.24 µm，粒径分布窄且呈球形。体外释放曲线表明，PTX从微球中的释放呈现出缓释行为。在大鼠药代动力学研究中也观察到类似现象，其中微球制剂的AUC比PTX注射剂高3.
