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用于肺部靶向的载头孢喹肟聚乳酸-乙醇酸共聚物微球的制备与测试

Preparation and testing of cefquinome-loaded poly lactic-co-glycolic acid microspheres for lung targeting.

作者信息

Qu Shaoqi, Zhao Li, Zhu Jiajia, Wang Chunmei, Dai Cunchun, Guo Hui, Hao Zhihui

机构信息

a Agricultural Bio-Pharmaceutical Laboratory, Qingdao Agricultural University , Qingdao , China and.

b National-Local Joint Engineering Laboratory of Agricultural Bio-Pharmaceutical Technology , Qingdao , China.

出版信息

Drug Deliv. 2017 Nov;24(1):745-751. doi: 10.1080/10717544.2017.1321058.

Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5668/8241178/8f0cc27a0f74/IDRD_A_1321058_F0001_B.jpg

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