使用声触发全氟戊烷乳剂递送氯苯丁酸。
Delivery of chlorambucil using an acoustically-triggered perfluoropentane emulsion.
机构信息
Department of Biomedical Engineering, University of Michigan, Ann Arbor, MI, USA.
出版信息
Ultrasound Med Biol. 2010 Aug;36(8):1364-75. doi: 10.1016/j.ultrasmedbio.2010.04.019.
Abstract
Ultrasound-mediated delivery systems have mainly focused on microbubble contrast agents as carriers of drugs or genetic material. This study uses micron-sized, perfluoropentane (PFP) emulsions as carriers of chlorambucil (CHL), a lipophilic chemotherapeutic. The release of CHL is achieved via acoustic droplet vaporization (ADV), whereby the superheated emulsion is converted into gas bubbles using ultrasound. Emulsions were made using an albumin shell and soybean oil as the CHL carrier. The ratio of the PFP to soybean oil phases in the droplets and the fraction of droplets that vaporize per ultrasound exposure were shown to correlate with droplet diameter. A 60-min incubation with the CHL-loaded emulsion caused a 46.7% cellular growth inhibition, whereas incubation with the CHL-loaded emulsion that was exposed to ultrasound at 6.3 MHz caused an 84.3% growth inhibition. This difference was statistically significant (p < 0.01), signifying that ADV can be used as a method to substantially enhance drug delivery.
摘要
超声介导的递送系统主要集中在微泡造影剂作为药物或遗传物质的载体。本研究使用微米级的全氟戊烷 (PFP) 乳剂作为氯苯丁酸 (CHL) 的载体，CHL 是一种亲脂性化疗药物。CHL 的释放是通过声致液滴汽化 (ADV) 实现的，即通过超声将过热的乳液转化为气泡。乳液使用白蛋白壳和大豆油作为 CHL 载体。乳滴中 PFP 与大豆油相的比例以及每超声暴露时汽化的乳滴分数与液滴直径相关。用负载 CHL 的乳液孵育 60 分钟导致细胞生长抑制率为 46.7%，而用在 6.3 MHz 下暴露于超声的负载 CHL 的乳液孵育则导致 84.3%的生长抑制。这种差异具有统计学意义 (p < 0.01)，表明 ADV 可用作大幅增强药物递送的方法。
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