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Porphyrin-terminated nanoscale fluorescent polyrotaxane as a biodegradable drug carrier for anticancer research

机译：卟啉封端的纳米尺度荧光聚发光烷作为抗癌研究的可生物降解的药物载体

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摘要

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.
机译：药物递送载体对改善癌症治疗具有巨大的承诺，并表明热传星（PR）显示出优异的携带药物。然而，存在一些报道中，当用作药物载体时，水溶性PR不容易用有机荧光染料标记。在此，我们合成了一种药物负载的荧光卟啉终端的PR（PR-COOH），其可用作药物和基因递送的示踪材料。 PR-COOH的结构，形态和Zeta电位的特征在于核磁共振，高分辨率透射电子显微镜和Zeta电位测量。在该研究中，顺铂（CDDP）用作模型药物。研究了Zeta潜力，药物包封效率和CDDP-COOH-PR（PR-COOH-PT）的药物释放。共聚焦激光扫描显微镜显示PR-COOH可以通过HELA和CT26细胞内化。通过卵黄移植肿瘤模型，通过3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四烷基溴（MTT）测定和体内体外进行PR-CoOH-PT的抗肿瘤效果。结果表明，PR-CoOH-PT可以显着抑制肿瘤生长;因此，PR-CoOH-PT在癌症治疗中具有有希望的作用。

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