The use of targeted liposomes encapsulating chemotherapy drugs enhances the specific targeting of cancer cells, thus reducing the side effects of these drugs and providing patient-friendly chemotherapy treatment. Targeted pegylated (stealth) liposomes have the ability to safely deliver their loaded drugs to the cancer cells by targeting specific receptors overly expressed on the surface of these cells. Applying ultrasound as an external stimulus will safely trigger drug release from these liposomes in a controlled manner. In this study, we investigated the release kinetics of the model drug “calcein” from targeted liposomes sonicated with low-frequency ultrasound (20 kHz). Our results showed that pegylated liposomes were more sonosensitive compared to nonpegylated liposomes. A comparison of the effect of three targeting moieties conjugated to the surface of pegylated liposomes, namely human serum albumin (HSA), transferrin (Tf) and arginylglycylaspartic acid (RGD), on calcein release kinetics was conducted. The fluorescent results showed that HSA-PEG and Tf-PEG liposomes were more sonosensitive (showing higher calcein release following the exposure to pulsed LFUS) compared to the control pegylated liposomes, thus adding more acoustic benefits to their targeting efficacy.

中文翻译：

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聚乙二醇化和靶向部分对超声介导脂质体释药的影响

封装化疗药物的靶向脂质体的使用增强了癌细胞的特异性靶向性，从而降低了这些药物的副作用并提供了对患者友好的化疗方法。靶向的聚乙二醇化（隐身）脂质体具有通过靶向过度表达在这些细胞表面的特定受体，从而将其负载的药物安全地递送至癌细胞的能力。施加超声波作为外部刺激将以受控方式安全地触发药物从这些脂质体释放。在这项研究中，我们研究了用低频超声（20 kHz）超声处理的靶向脂质体中模型药物“钙黄绿素”的释放动力学。我们的结果表明，与未聚乙二醇化的脂质体相比，聚乙二醇化的脂质体对声波的敏感性更高。比较了缀合在聚乙二醇化脂质体表面上的三个靶向部分，即人血清白蛋白（HSA），转铁蛋白（Tf）和精氨酰糖基葡萄糖酸天冬氨酸（RGD）对钙黄绿素释放动力学的影响。荧光结果表明，与对照聚乙二醇化脂质体相比，HSA-PEG和Tf-PEG脂质体对声音更敏感（显示出在暴露于脉冲LFUS后钙黄绿素释放更高），因此在其靶向功效方面增加了更多的声学优势。