Qu Shaoqi, Zhao Li, Zhu Jiajia, Wang Chunmei, Dai Cunchun, Guo Hui, Hao Zhihui
a Agricultural Bio-Pharmaceutical Laboratory, Qingdao Agricultural University , Qingdao , China and.
b National-Local Joint Engineering Laboratory of Agricultural Bio-Pharmaceutical Technology , Qingdao , China.
Drug Deliv. 2017 Nov;24(1):745-751. doi: 10.1080/10717544.2017.1321058.
The aim of this study was to prepare cefquinome-loaded poly lactic-co-glycolic acid (PLGA) microspheres and to evaluate their in vitro and in vivo characteristics. Microspheres were prepared using a spry drier and were characterized in terms of morphology, size, drug-loading coefficient, encapsulation ratio and in vitro release. The prepared microspheres were spherical with smooth surfaces and uniform size (12.4 ± 1.2 μm). The encapsulation efficiency and drug loading of cefquinome was 91.6 ± 2.6 and 18.3 ± 1.3%, respectively. In vitro release of cefquinome from the microspheres was sustained for 36 h. In vivo studies identified the lung as the target tissue and the region of maximum cefquinome release. A partial lung inflammation was observed but disappeared spontaneously as the microspheres were removed through in vivo decay. The sustained cefquinome release from the microspheres revealed its applicability as a drug delivery system that minimized exposure to healthy tissues while increasing the accumulation of therapeutic drug at the target site. These results indicated that the spray-drying method of loading cefquinome into PLGA microspheres is a straightforward method for lung targeting in animals.
本研究的目的是制备载有头孢喹肟的聚乳酸-乙醇酸共聚物（PLGA）微球，并评估其体外和体内特性。使用喷雾干燥器制备微球，并对其形态、大小、载药系数、包封率和体外释放进行表征。制备的微球呈球形，表面光滑，大小均匀（12.4±1.2μm）。头孢喹肟的包封率和载药量分别为91.6±2.6%和18.3±1.3%。头孢喹肟从微球中的体外释放持续36小时。体内研究确定肺为靶组织以及头孢喹肟释放最多的区域。观察到部分肺部炎症，但随着微球在体内降解而自行消失。微球中头孢喹肟的持续释放表明其作为一种药物递送系统的适用性，该系统可最大程度减少对健康组织的暴露，同时增加治疗药物在靶部位的蓄积。这些结果表明，将头孢喹肟载入PLGA微球的喷雾干燥法是一种用于动物肺部靶向的直接方法。
