两性霉素B聚乳酸普鲁兰纳米胶束的制备及评价

Preparation and in vitro characterization of amphotericin B poly(dl-lactide)-pullulan micelles

目的制备两性霉素B聚乳酸普鲁兰(PLA-pullulan)纳米胶束,并进行体外评价。方法以新型两亲性高分子PLA-pullulan为载体材料,采用薄膜水化法制备两性霉素B纳米胶束,并分别采用透射电镜、激光粒径仪和zeta电位分析仪对胶束的形态、粒径和表面电位进行表征,测定其包封率、载药量和体外释放动力学,考察其药物分散状态和溶血毒性。结果所制备的两性霉素B聚乳酸普鲁兰纳米胶束溶液外观透明,电镜下呈圆整的球形,平均粒径为152.1 nm,包封率为71.1%,载药量达10.9%,24 h的累积释放量为10.01%,溶血毒性低于两性霉素B去氧胆酸钠胶束。结论聚乳酸普鲁兰胶束是两性霉素B潜在的优良纳米载体,具有良好的应用价值。

Objective To prepare and characterize the amphotericin B(Am B) loaded poly(dl-lactide) pullulan(PLA-pullulan) nanomicelles in vitro. Methods PLA-pullulan, a new amphiphilic polymer, was used for loading Am B with thin film dispersion method. The morphology, diameter and surface potential of the micelles were characterized by transmission electron microscopy, size and zeta potential analyzer. The drug loading content, entrapment efficiency and in vitro release of Am B loaded micelles were determined. The relative aggregation state of the encapsulated Am B and hemolytic toxicity were studied. Results The micelle was clear and transparent, globular shaped. The average particle size, drug loading content and entrapment efficiency were 152.1 nm with narrow distribution, 71.1% and 10.9%, respectively. The cumulative release amount of micelle within 24 h is 10.01%. Am B loaded micelles showed lower hemolysis than Am B solutions. Conclusions PLA-pullulan micelles, used as nanocarrier of amphotericin B, has a very good application prospect.