Hao Shilei, Wang Yazhou, Wang Bochu, Deng Jia, Zhu Liancai, Cao Yang
Key Laboratory of Biorheological Science and Technology, Ministry of Education, College of Bioengineering, Chongqing University, Chongqing 400030, China.
Key Laboratory of Biorheological Science and Technology, Ministry of Education, College of Bioengineering, Chongqing University, Chongqing 400030, China.
Mater Sci Eng C Mater Biol Appl. 2014 Jun 1;39:113-9. doi: 10.1016/j.msec.2014.02.014. Epub 2014 Feb 15.
In the present study, the electrospray deposition was successfully applied to prepare the porous poly(lactic-co-glycolic acid) (PLGA) microparticles by one-step processing. Metronidazole was selected as the model drug. The porous PLGA microparticles had high drug loading and low density, and the porous structure can be observed by scanning electron microscope (SEM) and transmission electron microscopy (TEM). The production time has been shortened considerably compared with that of the traditional multi-emulsion method. In addition, no chemical reaction occurred between the drug and polymer in the preparation of porous microparticles, and the crystal structure of drug did not change after entrapment into the porous microparticles. The porous microparticles showed a sustained release in the simulated gastric fluid, and the release followed non-Fickian or case II transport. Furthermore, porous microparticles showed a slight cytotoxicity in vitro. The results indicated that electrospray deposition is a good technique for preparation of porous microparticles, and the low-density porous PLGA microparticles has a potential for the development of gastroretentive systems or for pulmonary drug delivery.
在本研究中，电喷雾沉积法成功地用于一步制备多孔聚乳酸-乙醇酸共聚物（PLGA）微粒。选择甲硝唑作为模型药物。多孔PLGA微粒具有高载药量和低密度，其多孔结构可通过扫描电子显微镜（SEM）和透射电子显微镜（TEM）观察到。与传统的多重乳液法相比，生产时间大幅缩短。此外，在制备多孔微粒过程中药物与聚合物之间未发生化学反应，药物包封于多孔微粒后其晶体结构未改变。多孔微粒在模拟胃液中呈现缓释特性，且释放遵循非菲克扩散或Ⅱ型转运。此外，多孔微粒在体外表现出轻微的细胞毒性。结果表明，电喷雾沉积法是制备多孔微粒的一种良好技术，低密度多孔PLGA微粒在胃滞留系统或肺部药物递送的开发方面具有潜力。
