Liu Hui, Guo Chunlei, Shang Yuhong, Zeng Lin, Jia Haixue, Wang Zhongyan
Henan Key Laboratory of Immunology and Targeted Drug, Henan Collaborative Innovation Center of Molecular Diagnosis and Laboratory Medicine, School of Laboratory Medicine, Xinxiang Medical University, Xinxiang, China.
ChosenMed Technology Co., Ltd., Beijing, China.
Front Bioeng Biotechnol. 2021 Dec 21;9:804747. doi: 10.3389/fbioe.2021.804747. eCollection 2021.
In recent years, supramolecular nanoparticles consisting of peptides and drugs have been regarded as useful drug delivery systems for tumor therapy. Pemetrexed (PEM) is a multitarget drug that is effective for many cancers, such as non-small cell lung cancer. Here, RGD-conjugated molecular nanoparticles mainly composed of an anticancer drug of PEM (PEM-FFRGD) were prepared to deliver PEM to tumors. The peptide could self-assemble into a nanoparticle structure with diameter of about 20 nm. Moreover, the nanoparticle showed favorable solubility and biocompatibility compared with those of PEM, and the MTT test on A549 and LLC cells showed that the PEM-FFRGD nanoparticles had stronger cytotoxic activity than PEM alone. Most importantly, the nanoparticle could promote tumor apoptosis and decrease mitochondrial energy metabolism in tumors. studies indicated that PEM-FFRGD nanoparticles had enhanced antitumor efficacy in LLC tumor-bearing mice compared to that of PEM. Our observations suggested that PEM-FFRGD nanoparticles have great practical potential for application in lung cancer therapy.
近年来，由肽和药物组成的超分子纳米颗粒被视为用于肿瘤治疗的有用药物递送系统。培美曲塞（PEM）是一种对多种癌症有效的多靶点药物，如非小细胞肺癌。在此，制备了主要由抗癌药物PEM组成的RGD共轭分子纳米颗粒（PEM-FFRGD），以将PEM递送至肿瘤。该肽可自组装成直径约20nm的纳米颗粒结构。此外，与PEM相比，该纳米颗粒表现出良好的溶解性和生物相容性，对A549和LLC细胞的MTT试验表明，PEM-FFRGD纳米颗粒比单独的PEM具有更强的细胞毒性活性。最重要的是，该纳米颗粒可促进肿瘤细胞凋亡并降低肿瘤中的线粒体能量代谢。研究表明，与PEM相比，PEM-FFRGD纳米颗粒在荷LLC肿瘤小鼠中具有增强的抗肿瘤功效。我们的观察结果表明，PEM-FFRGD纳米颗粒在肺癌治疗中具有巨大的实际应用潜力。
