载多西紫杉醇的新型超声微泡的制备及性能观察

目的制备携载多西紫杉醇的新型超声微泡,并观察其药物携载能力。方法以PLGA为膜材料,以多西紫杉醇为携载药物,采用复乳化法和冷冻干燥技术,制备载药超声微泡;选择高效液相色谱法测定制剂中药物含量及超声环境下的释放量。结果载药超声微泡样品呈白色粉末状,表面光泽且粒径较均一,载药率和包封率分别可达2.36%和61.40%,且稳定可控;模拟超声环境下药物释放量明显增加。结论所制微泡对多西紫杉醇的携载能力有明显提高,并可在超声环境下稳定释放药物。

Preparation and observation of the capability of docetaxel-loaded ultrasound microbubbles

Objective To prepare a new type of docetaxel-loaded ultrasound microbubbles, and to reveal the discipline of drug release. Methods Docetaxel-loaded microbubbles were prepared with PLGA as the membrane material via multiple emulsion and freeze drying technique. In addition, high performance liquid chromatography (HPLC) was employed for the determination of docetaxel in the samples, as well as the drug release under ultrasound. Results The obtained drug-loaded ultrasound microbubbles were white powders with smooth surface and a narrow size distribution. The drug loading efficiency and encapsulation efficiency was 2.36% and 61.40% with good stability and controllability. Also the drug release was improved obviously with ultrasound irradiation. Conclusion The prepared ultrasound microbubbles can increase drug-loaded capability of docetaxel, and the drug can release stably with ultrasound irradiation.