目的:制备一种包封率及载药量较高的载光敏剂微泡,并测定其物理参数。方法:制备加入大豆油载竹红菌素微泡,观察载微泡的形态、结构、观察苏丹黑对微泡的染色,以及超声辐照后苏丹黑的释放情况,测定微泡的包封率、载药量、粒径、电位分布,体外显影效果,兔肝内显影效果。结果:载竹红菌素微泡的浓度为1.4×109/ml至4.5×109/ml,粒径范围为90%以上在1μm至5μm,平均粒径为1.95μm。大豆油微泡竹红菌素的包封率大于95%,载药量为2.38±0.023 mg/ml;Zeta电位为20.3±1.6 mV;苏丹黑染色后光镜下可见大豆油及微泡壁被染成黑色,超声辐照后微泡稀释液变黑加深。结论:采用机械振荡法制备的加入大豆油载竹红菌素微泡,包封率较高,稳定性好,粒径分布好,体内外显像效果尚可,超声辐照能促使微泡中的药物释放,大豆油载药微泡作为一种光敏剂的运载体,有望实现实时监控下的体内定点靶向给药。
Objective: A microbubble loading more hypocrellin was developed as a new cartier for chemotherapeutic drug delivery and its physical parameters were measured. Methods : Hypocrenin was suspended in soybean oil, and then added to an aqueous suspensinn of phospholipids in vials. The headspace of the vials was replaced with perfluorobutane gas. The vials were sealed and agitated on a shaking device. The concentration, size, Zeta potential, drag enluapment effciency and drug - loading amounts of the microbubble containing hypocrellin were studied and the enhancement of ultrasound imaging measured in vitro and in vivo. And the microbubble containing sudan black dye were prnduced to investigate that ultrasound - mediated mierobubbles deliver drug. Results: The microbubbles containing hypocrellin had a mean particle count of approxinkately 1.4 × 10^9 - 4. 5 × 10^9 particles per ml. and a mean size of 1.95μm ailerons. The drug entrapment efficiency was more than 95 % and the drug - loading amounts was 2.38 ±0.023 mg/ml. Fixing amounts of ultrasound energy ruptured the micmbubble and released the drug. The microbubbles containing hypocrellin could nemarkably enhance uhrasound imaging in vitro and the liver imaging of the rabbits was significantly enhanced. Conclusions:Acoustically active microbubble represent a new class of acoustically active photosensitizer delivery vehicles.