INSERM U1032, Université de Lyon, 151 Cours Albert Thomas, Lyon, France.
J Drug Target. 2012 Sep;20(8):691-702. doi: 10.3109/1061186X.2012.712129.
Targeted and triggered release of liposomal drug using heat or ultrasound represents a promising treatment modality able to increase the therapeutic-totoxicity ratio of encapsulated drugs.
To study the ability for high-intensity focused ultrasound to induce liposomal drug release mainly by focused inertial cavitation in vitro and in an animal model.
A 1 MHz ultrasound setup has been developed for in vitro and in vivo drug release from a specific liposomal doxorubicin formulation at a target cavitation dose.
Controlled cavitation at 1 MHz was applied within the tumors 48 hours after liposome injection according to preliminary pharmacokinetic study. A small non-significant therapeutic effect of US-liposomal treatment was observed compared to liposomes alone suggesting no beneficial effect of ultrasound in the current setup.
The in vitro study provided a suitable ultrasound setup for delivering a cavitation dose appropriate for safe liposomal drug release. However, when converting to an in vivo model, no therapeutic benefit was observed. This may be due to a number of reasons, one of which may be the difficulty in converting in vitro findings to an in vivo model. In light of these findings, we discuss important design features for future studies.
利用热或超声靶向和触发脂质体药物释放是一种很有前途的治疗方式，能够提高包裹药物的治疗-毒性比。
研究高强度聚焦超声通过聚焦惯性空化在体外和动物模型中诱导脂质体药物释放的能力。
为了在特定的脂质体阿霉素制剂的靶向空化剂量下实现体外和体内药物释放，开发了一种 1 MHz 的超声设备。
根据初步药代动力学研究，在脂质体注射后 48 小时内，将 1 MHz 的控制空化应用于肿瘤中。与单独使用脂质体相比，超声脂质体治疗的小而无统计学意义的治疗效果表明，在当前设置中超声没有有益的效果。
体外研究提供了一种合适的超声设备，可提供适当的空化剂量以安全释放脂质体药物。然而，当转化为体内模型时，没有观察到治疗益处。这可能有很多原因，其中之一可能是将体外研究结果转化为体内模型存在困难。鉴于这些发现，我们讨论了未来研究的重要设计特点。
