目的: 制备纳米级的载紫杉醇促黄体激素释放激素(luteinising-hormone releasing hormone,LHRH)靶向脂质微泡超声造影剂并评价其理化特性。方法: 通过旋转蒸发法、机械震荡法及生物素-亲和素法制备LHRH靶向脂质微泡。Malvern检测仪检测其粒径及表面电位,超声下观察其体外显影情况,高效液相色谱法检测紫杉醇的载药量及包封率,流式细胞仪检测二抗分别与靶向微泡、非靶向微泡的结合率。结果: 靶向脂质微泡外观圆整,分布均匀,在室温下保存14 d后,微泡的一般特性与制备初比较,差异无统计学意义(P＞0.05)。靶向微泡及非靶向微泡与二抗的结合率分别为(97.76±2.18)%、(6.48±0.71)%,二者比较差异具有统计学意义(P＜0.05)。结论: 成功制备纳米级载紫杉醇靶向脂质微泡,此微泡粒径较小,稳定性较高,且LHRH的靶连接率较高。
Objective: To prepare the targeted lipid-microbubble ultrasonographic contrastagent loaded with paclitaxel LHRH, and to evaluate its physical and chemical properties,Methods:LHRH targeted lipid-microbubble was prepared by Co-evaporating method, mechanical vibration method and biotin-avidin method. The size and surface electric potential were detected by Malvern detector and the imaging was observed by ultrasonography. The drug-loading capacity and encapsulation rate were determined by high performance liquid chromatography (HPLC). The connection rates of secondary antibody with targeted and non-targeted lipid-microbubble were detected by flow cytometry (FCM).Results: The targeted lipid- microbubble had complete appearance and even distribution. After being kept at room temperature for 14 days, there was no significant difference of general properties ( P＞0.05). The binding rates of secondary antibody with targeted and non-targeted lipid-microbubble were 97.76±2.18 % and 6.48±0.71 % respectively, which had significant difference (P＜0.05).Conclusion: The targeted lipid-microbubble loaded with paclitaxel is successfully prepared, with smaller size and higher stability. It has a high connection rate of LHRH.
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