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超声敏感的 cRGD 修饰脂质体作为一种新型药物传递系统。

Ultrasound-sensitive cRGD-modified liposomes as a novel drug delivery system.

机构信息

Department of Chemical Engineering, College of Engineering, American University of Sharjah, Sharjah, United Arab Emirates.

Materials Science and Engineering Program, American University of Sharjah, Sharjah, United Arab Emirates.

出版信息

Artif Cells Nanomed Biotechnol. 2022 Dec;50(1):111-120. doi: 10.1080/21691401.2022.2074439.

DOI:10.1080/21691401.2022.2074439
PMID:35543613
Abstract

Targeted liposomes enable the delivery of encapsulated chemotherapeutics to tumours by targeting specific receptors overexpressed on the surfaces of cancer cells; this helps in reducing the systemic side effects associated with the cytotoxic agents. Upon reaching the targeted site, these liposomes can be triggered to release their payloads using internal or external triggers. In this study, we investigate the use of low-frequency ultrasound as an external modality to trigger the release of a model drug (calcein) from non-targeted and targeted pegylated liposomes modified with cyclic arginine-glycine-aspartate (cRGD). Liposomes were exposed to sonication at 20-kHz using three different power densities (6.2, 9, and 10 mW/cm). Our results showed that increasing the power density increased calcein release from the sonicated liposomes. Moreover, cRGD conjugation to the surface of the liposomes rendered cRGD-liposomes more susceptible to ultrasound compared to the non-targeted liposomes. cRGD conjugation was also found to increase cellular uptake of calcein by human colorectal carcinoma (HCT116) cells which were further enhanced following sonicating the cells with low-frequency ultrasound (LFUS).

摘要

靶向脂质体通过靶向癌细胞表面过度表达的特定受体将包裹的化疗药物递送到肿瘤中;这有助于减少与细胞毒性药物相关的全身副作用。到达靶向部位后,这些脂质体可以使用内部或外部触发物触发释放其有效载荷。在这项研究中,我们研究了低频超声作为外部手段来触发用环精氨酸-甘氨酸-天冬氨酸(cRGD)修饰的非靶向和靶向聚乙二醇化脂质体释放模型药物(钙黄绿素)。使用三种不同的功率密度(6.2、9 和 10 mW/cm),将脂质体在 20 kHz 下进行超声处理。我们的结果表明,增加功率密度会增加超声处理后的脂质体中钙黄绿素的释放。此外,与非靶向脂质体相比,脂质体表面的 cRGD 缀合使 cRGD 脂质体更容易受到超声的影响。还发现 cRGD 缀合增加了人结肠直肠癌细胞(HCT116)对钙黄绿素的细胞摄取,并且在用低频超声(LFUS)对细胞进行超声处理后进一步增强。

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