由于现有治疗方法的有效性有限且复发的可能性很高，乳腺癌面临着巨大的挑战。 iRGD同时具有RGD序列和C端序列，具有靶向和透膜双重功能。 iRGD修饰的纳米载体可以增强药物对肿瘤血管内皮细胞的靶向和新生微血管的渗透，增加肿瘤组织中的药物浓度。SiO2/AuNCs与iRGD/PTX之间进行酰胺化反应，产生缀合的药物递送系统（SiO2/ AuNCs-iRGD/PTX、SAIP@NPs）。评估包括 SAIP@NP 的形态、粒径分布、理化性质、体外释放曲线、细胞毒性和细胞摄取的表征。分别使用小动物体内成像系统和荷瘤裸鼠模型评估SAIP@NPs的肿瘤靶向和抗肿瘤功效。分别利用小动物体内成像系统和原位裸鼠乳腺癌异种移植模型评估SAIP@NPs的肿瘤靶向和抗肿瘤功效。所制备的SAIP@NPs表现出良好的稳定性和一定的缓释作用磷酸盐缓冲液（PBS，pH 7.4）中。体外研究表明，由于iRGD肽的跨膜和靶向双重功能，SAIP@NPs与MDA-MB-231细胞膜上高表达的整合素αvβ3表现出较强的结合能力，提高了对细胞膜的摄取能力。抑制肿瘤细胞的快速生长，促进肿瘤细胞凋亡。动物实验结果进一步证明SAIP@NPs在肿瘤部位的滞留时间更长、抗肿瘤作用更强，且对实验动物主要器官无明显毒性。工程化SAIP@NPs表现出高效的膜通透性、精确的膜通透性、精准的抗肿瘤活性等优异的功能。肿瘤靶向和成像，从而显着增强乳腺癌的治疗效果，并具有良好的安全性。© 2024 Hou 等人。

Breast cancer presents significant challenges due to the limited effectiveness of available treatments and the high likelihood of recurrence. iRGD possesses both RGD sequence and C-terminal sequence and has dual functions of targeting and membrane penetration. iRGD-modified nanocarriers can enhance drug targeting of tumor vascular endothelial cells and penetration of new microvessels, increasing drug concentration in tumor tissues.The amidation reaction was carried out between SiO2/AuNCs and iRGD/PTX, yielding a conjugated drug delivery system (SiO2/AuNCs-iRGD/PTX, SAIP@NPs). The assessment encompassed the characterization of the morphology, particle size distribution, physicochemical properties, in vitro release profile, cytotoxicity, and cellular uptake of SAIP@NPs. The tumor targeting and anti-tumor efficacy of SAIP@NPs were assessed using a small animal in vivo imaging system and a tumor-bearing nude mice model, respectively. The tumor targeting and anti-tumor efficacy of SAIP@NPs were assessed utilizing a small animal in vivo imaging system and an in situ nude mice breast cancer xenograft model, respectively.The prepared SAIP@NPs exhibited decent stability and a certain slow-release effect in phosphate buffer (PBS, pH 7.4). In vitro studies had shown that, due to the dual functions of transmembrane and targeting of iRGD peptide, SAIP@NPs exhibited strong binding to integrin αvβ3, which was highly expressed on the membrane of MDA-MB-231 cells, improving the uptake capacity of tumor cells, inhibiting the rapid growth of tumor cells, and promoting tumor cell apoptosis. The results of animal experiments further proved that SAIP@NPs had longer residence time in tumor sites, stronger anti-tumor effect, and no obvious toxicity to major organs of experimental animals.The engineered SAIP@NPs exhibited superior functionalities including efficient membrane permeability, precise tumor targeting, and imaging, thereby significantly augmenting the therapeutic efficacy against breast cancer with a favorable safety profile.© 2024 Hou et al.