Huo Dongjie, Deng Shuhai, Li Lingbing, Ji Jianbo
Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhuaxi road, Shandong, 250012 Jinan, PR China.
Int J Pharm. 2005 Jan 31;289(1-2):63-7. doi: 10.1016/j.ijpharm.2004.10.017. Epub 2004 Dec 19.
Lung-targeting cisplatin-loaded poly(lactic-co-glycolic) acid microspheres (CDDP-PLGA-MS) were prepared by a solvent evaporation method. The uniform design was used to optimize the technology of preparation, the appearance and size distribution were examined by scanning electron microscope, and the aspects such as in vitro release characteristics, stability, drug loading, loading efficiency, pharmacokinetics and tissue distribution in rabbit were studied. The experimental results showed that the microspheres were globular in appearance and dispersed well. The average particle size was 12.8 microm with 98% of the microspheres being in the range of 5-30 microm. The drug loading and loading efficiency were 17.68 and 53.2%, respectively. The in vitro release behavior could be expressed by the following equation: 1-Q=0.424e(-0.360t)+0.474e(-0.001t). After i.v. administration (15 min), the drug concentration of microspheres group in lung in rabbits was 212 microg/g, while that of controlled group was 1.37 microg/g. CDDP-PLGA-MS showed a combination of lung-targeting and sustained drug release in experiments on rabbits.
采用溶剂蒸发法制备了肺靶向顺铂聚乳酸-乙醇酸共聚物微球（CDDP-PLGA-MS）。运用均匀设计法优化制备工艺，通过扫描电子显微镜考察其外观及粒径分布，并研究其体外释放特性、稳定性、载药量、包封率、药代动力学以及在兔体内的组织分布等方面。实验结果表明，微球外观呈球形，分散性良好。平均粒径为12.8微米，98%的微球粒径在5-30微米范围内。载药量和包封率分别为17.68%和53.2%。体外释放行为可用以下方程表示：1-Q = 0.424e(-0.360t)+0.474e(-0.001t)。静脉注射（15分钟后），兔体内微球组肺组织中的药物浓度为212微克/克，而对照组为1.37微克/克。在兔实验中，CDDP-PLGA-MS表现出肺靶向与缓释相结合的特性。
