文献：

iRGD Peptide-Mediated Liposomal Nanoparticles with Photoacoustic/Ultrasound Dual-Modality Imaging for Precision Theranostics Against Hepatocellular Carcinoma

文献链接：

作者：

Huipu Li,Shasha Shi,Meng Wu,Wei Shen,Jianli Ren,Zhechuan Mei , Haitao Ran,Zhigang Wang ,Yi Tian,Jian Gao,Hongyun Zhao

相关产品：

DSPE-PEG2000-MAL（磷脂-聚乙二醇2000-马来酰亚胺）

原文摘要：

Purpose: Prepare a multifunctional ultrasound molecular probe, cell-penetrating peptidemodified 10-hydroxycamptothecin-loaded phase-transformation lipid nanoparticles (iRGDICG-10-HCPT-PFP-NPs), and to combine iRGD-ICG-10-HCPT-PFP -NPs with low-intensity focused ultrasound (LIFU) for precision theranostics against hepatocellular carcinoma (HCC).Materials and Methods: The morphology of nanoparticles (NPs) and iRGD-ICG-10- HCPT-PFP-NPs was detected. In vitro, we examined targeting ability by flow cytometry and confocal laser scanning microscopy (CLSM), assessed penetration ability into hepatoma cells, and assessed killing ability. In vivo, we examined the targeting ability of the NPs with a photoacoustic (PA) imager and fluorometer (FL), while LIFU irradiation was used to trigger the release of chemotherapeutic drugs, which had a therapeutic effect on tumors.Results: The particle size of iRGD-ICG-10-HCPT-PFP-NPs was 298.4 ± 10.42 nm. In vitro, iRGD-ICG-10-HCPT-PFP-NPs bound more to SK-Hep1 cells than ICG-10-HCPT-PFP-NPs. iRGD-ICG-10-HCPT-PFP-NPs could achieve PA/ultrasound imaging. The percentage of antiproliferative and apoptotic cells in the iRGD-ICG-10-HCPT-PFP-NPs+LIFU group was significantly higher. In vivo, iRGD-ICG-10-HCPT-PFP-NPs can target tumor sites and achieve PA/ ultrasound imaging. The tumor volume in the iRGD-ICG-10-HCPT-PFP-NPs+LIFU group was significantly smaller, and the antiproliferative and proapoptotic effects were higher.Conclusion: We successfully prepared a novel molecular probe that has good targeting, can perform ultrasound/PA dual-modality imaging, and can penetrate deep into tumors to achieve better therapeutic tumor effects, providing a new idea and method for theranostics of HCC.

DSPE - PEG2000 - MAL 主要由三部分组成。DSPE（1,2 - 二硬脂酰 - sn - 甘油 - 3 - 磷酸乙醇胺）是一种磷脂，它含有亲水性的磷酸乙醇胺头部和两条疏水性的硬脂酸长链。PEG2000 代表分子量约为 2000 的聚乙二醇（Polyethylene glycol）部分，其作用是增加分子的亲水性和空间位阻，减少与生物体内成分的非特异性相互作用。MAL（Maleimide）即马来酰亚胺基团，这是一个具有高度反应活性的官能团，能够与含有巯基（-SH）的化合物发生特异性的化学反应。基于DSPE-PEG2000-MAL的性质，该文献产品合成了荧光标记的纳米颗粒——iRGD-ICG-10-HCPT-PFP-NPs，流程如下：

图：合成流程

iRGD-ICG-10-HCPT-PFP-NPs的制备：

DPPC，DSPE-peg2000-iRGD，胆固醇，和10-HCPT 制药粉添加到圆底瓶和溶解在三氯甲烷中。将圆底烧瓶连接到一个旋转蒸发器上蒸发。将 ICG溶解于水中，加入 PFP，首先用超声超声器乳化，然后在相同功率下乳化。最后，制备iRGD-ICG-10-HCPT-PFP-NPs，在离心机中离心，弃上清，用PBS溶液重悬。ICG-10-HCPT-PFPNPs通过上述相同的程序获得，只是使用DSPE代替DSPE-iRGD。

图：浓度变化

结论：

该文献成功制备了一种靶向性良好、能进行超声/PA双模态成像、能穿透tumour的新型分子探针iRGDICG-10-HCPT-PFP-NPs。文献中对该产品进行了相关实验，结果表明该产品具有良好的靶向能力、成像能力，数据均取得理想结果。