Key Laboratory of Natural Medicine and Immune-Engineering of Henan Province, Henan Universitry, Kaifeng, Henan 475004, People's Republic of China.
Nanotechnology. 2020 Apr 3;31(25):255101. doi: 10.1088/1361-6528/ab7d71. Epub 2020 Mar 6.
Drug delivery carriers hold tremendous promise for improving cancer treatment, and polyrotaxane (PR) has shown excellent drug-carrying properties. However, there have been some reports that, when used as a drug carrier, water-soluble PR is not easily labeled with organic fluorescent dyes. Herein, we synthesized a drug-loaded fluorescent porphyrin-terminated PR (PR-COOH) which can be used as a tracer material in drug and gene delivery. The structure, morphology and zeta potential of PR-COOH were characterized by nuclear magnetic resonance, high-resolution transmission electron microscopy and zeta potentiometry. In this research, cisplatin (CDDP) is used as a model drug. The zeta potential, drug encapsulation efficiency and drug release of CDDP-loaded PR (PR-COOH-Pt) were studied. Confocal laser scanning microscopy showed that PR-COOH could be internalized by HeLa and CT26 cells. The antitumor efficacy of PR-COOH-Pt was investigated in vitro by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and in vivo by a xenograft tumor model. The results showed that PR-COOH-Pt could significantly inhibit tumor growth; thus PR-COOH-Pt has a promising role in cancer therapy.
药物传递载体在改善癌症治疗方面具有巨大的潜力，而聚轮烷（PR）已显示出优异的药物携带性能。然而，有一些报道称，水溶性 PR 作为药物载体时，不易被有机荧光染料标记。在此，我们合成了一种载药荧光卟啉封端的 PR（PR-COOH），可用作药物和基因传递中的示踪材料。通过核磁共振、高分辨率透射电子显微镜和zeta 电位仪对 PR-COOH 的结构、形态和zeta 电位进行了表征。在这项研究中，顺铂（CDDP）被用作模型药物。研究了载药 PR（PR-COOH-Pt）的zeta 电位、药物包封效率和药物释放。共聚焦激光扫描显微镜显示 PR-COOH 可以被 HeLa 和 CT26 细胞内化。通过 3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四氮唑溴盐（MTT）测定法和异种移植肿瘤模型在体外研究了 PR-COOH-Pt 的抗肿瘤功效。结果表明，PR-COOH-Pt 能显著抑制肿瘤生长；因此，PR-COOH-Pt 在癌症治疗中具有广阔的应用前景。
