恩诺沙星聚合物胶束的制备及体外释放

Preparation and in vitro release of enrofloxacin-polymeric micelles

通过比较3种不同质量比的两嵌段共聚物制备的聚合物胶束,优化恩诺沙星聚合物胶束的制备工艺,并考察该胶束的理化性质和体外释药特性。以自乳化溶剂挥发法制备恩诺沙星聚合物胶束,并采用单因素法优化处方;HPLC法测定其载药量、包封率、体外释药特性,激光粒度仪测定其粒径及分布,红外分光光度法(IR)确证含药胶束特征。结果显示,采用PLA16000-mPEG2000(聚乳酸-聚乙二醇单甲醚)共聚物为载体,以丙酮为有机溶剂,所制备胶束平均粒径为(117.2±8.2)nm,载药量为(3.3±0.17)%,包封率为(32.3±1.70)%;相对于另外2种材料制备的胶束有较好的载药量,且IR确证药物已被包封在胶束中。恩诺沙星胶束体外释药试验表明其具有一定的缓释特性。

To optimize the preparation method of the enrofloxacin-polymeric micelles by comparing with three different proportionality of D,L-lactide and mPEG,and investigate its properties and release behavior in vitro.The enrofloxacin-polymeric micelles were prepared by modified spontaneous emulsification solvent diffusion method.The method by examining the single factor was used to optimize the preparation procedure.The drug loading and encapsulation were determined by HPLC.The mean diameter and distribution of the particle size were also assayed.The formulation of drug loading micelles was confirmed by IR.The results showed that the micelles were prepared with the polymer with the proportion of PLA16000-mPEG2000 as carrier,acetone as organic solvent,which had the better drug loading.The mean diameter was（117.2±8.2） nm,and drug loading as well as the encapsulation efficiency were（3.3±0.17）% and（32.3±1.7）%,respectively.Enrofloxacin was found to be encapsulated in the micelles.In vitro,enrofloxacin could be released sustainably from the micelles.