Preparation and Characterization of Lung-targeting Cefquinome-loaded PLGA Microspheres  

作　　者：张瑞丽 HAO Zhihui DING Zhaopeng 吕志华 

机构地区：[1]School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China [2]Agricultural Bio-pharmaceutical Laboratory, Qingdao Agricultural University, Qingdao 266109, China

出　　处：《Journal of Wuhan University of Technology(Materials Science)》2017年第2期494-499,共6页武汉理工大学学报（材料科学英文版）

基　　金：Funded by the national key research and development plan(No.2016YFD0501309);the National Natural Science Foundation of China(31402256);the High-level Talent Research Foundation of Qingdao Agricultural University,China(631206)

摘　　要：We developed poly lactic-co-glycolic acid（PLGA） microspheres loaded with cefquinome and tested their effectiveness in a mouse model. The microspheres were prepared by optimizing several key parameters such as PLGA molecular weight, drug/polymer ratio, internal water volume and ethyl acetate. Drug loading efficiency, stability, in vitro release and tissue distribution in mouse were evaluated. The average particle size of the microspheres was 27.84 μm. The drug loading efficiency was 64.57%. The in vitro release of cefquinome from microspheres after 4 h was about 40% compared with over 90% for the drug alone. The concentration of cefquinome in lung reached 25 μg/g 0.25 h after injection, and kept at 10 μg/g 4 h after injection. However, the concentration of cefquinome was very low in other organs even 0.25 h after injection. In conclusion, Cefquinome-loaded PLGA microspheres are compatible as an effective lung-targeting drug delivery system and have a good sustained release efficacy.We developed poly lactic-co-glycolic acid（PLGA） microspheres loaded with cefquinome and tested their effectiveness in a mouse model. The microspheres were prepared by optimizing several key parameters such as PLGA molecular weight, drug/polymer ratio, internal water volume and ethyl acetate. Drug loading efficiency, stability, in vitro release and tissue distribution in mouse were evaluated. The average particle size of the microspheres was 27.84 μm. The drug loading efficiency was 64.57%. The in vitro release of cefquinome from microspheres after 4 h was about 40% compared with over 90% for the drug alone. The concentration of cefquinome in lung reached 25 μg/g 0.25 h after injection, and kept at 10 μg/g 4 h after injection. However, the concentration of cefquinome was very low in other organs even 0.25 h after injection. In conclusion, Cefquinome-loaded PLGA microspheres are compatible as an effective lung-targeting drug delivery system and have a good sustained release efficacy.

关 键 词：PLGA microspheres cefquinome lung-targeting sustained release size mouse 

分 类 号：TQ465[化学工程—制药化工]