ACS Biomater Sci Eng. 2020 Jan 13;6(1):48-57. doi: 10.1021/acsbiomaterials.8b01301. Epub 2019 Jul 3.
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.
靶向脂质体包裹化疗药物可增强癌细胞的靶向性，从而降低这些药物的副作用，并为患者提供更友好的化疗治疗。靶向聚乙二醇化（隐形）脂质体能够通过靶向这些细胞表面过度表达的特定受体，将其负载的药物安全地递送到癌细胞中。应用超声作为外部刺激，可以安全地以可控的方式从这些脂质体中触发药物释放。在这项研究中，我们研究了低频超声（20 kHz）处理后的靶向脂质体中模型药物“钙黄绿素”的释放动力学。结果表明，与非聚乙二醇化脂质体相比，聚乙二醇化脂质体的超声敏感性更高。比较了三种靶向部分修饰在聚乙二醇化脂质体表面的效果，即人血清白蛋白（HSA）、转铁蛋白（Tf）和精氨酸-甘氨酸-天冬氨酸（RGD），对钙黄绿素释放动力学的影响。荧光结果表明，与对照组聚乙二醇化脂质体相比，HSA-PEG 和 Tf-PEG 脂质体的超声敏感性更高（在暴露于脉冲 LFUS 后显示出更高的钙黄绿素释放），从而为其靶向效果增加了更多的声效益处。
