Abstract Polymer bioconjugate theranostics with inherent fluorescence and tumor targeting properties offers the advantage of diagnosis via fluorescence imaging and tumor targeted cancer therapy in a single platform without any requirement of external probes. Herein, fluorescent tumor targeted polymer biomolecule conjugate (comprising of cancer cell specific biotin moieties) was synthesized as potential theranostic platform for cancer therapy. The polymer biomolecule conjugate (PFBT-B) was used as a non-toxic, tumor-targeted, and fluorescent (greenish-yellow fluorescence) coating on magnetite nanoparticles (MNPs, a probable hyperthermia agent) and subsequently loaded with chemotherapeutic drug 5-Fluorouracil (5FU). The MNPs showed a saturation magnetization of 56.28 emu/g and coercivity of 75.5 Oe. The coating of MNPs with PFBT-B was confirmed from TEM studies which showed an average shell thickness of 1.88 nm. Drug (5FU) loading studies revealed a loading capacity of ~6.64 μg/μg of PFBT-B, while release studies showed pH-sensitive release profiles with accelerated release of drug in acidic milieu. MTT assay showed enhanced cytotoxicity of 5FU in the nanoformulated form as compared to pure 5FU. Additionally, PFBT-B coated MNPs showed preferential localization into the HeLa cancer cells as compared to HEK 293T normal cells. The inherent fluorescence and tumor targeting properties, thus, indicate that PFBT-B could serve as potential theranostic platform for cancer therapy.

中文翻译：

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荧光肿瘤靶向聚合物-生物偶联物：用于癌症治疗的有效治疗诊断平台

摘要 具有固有荧光和肿瘤靶向特性的聚合物生物共轭治疗诊断在单一平台上通过荧光成像和肿瘤靶向治疗提供诊断优势，无需任何外部探针。在此，合成了荧光肿瘤靶向聚合物生物分子缀合物（包含癌细胞特异性生物素部分）作为癌症治疗的潜在治疗诊断平台。聚合物生物分子偶联物 (PFBT-B) 被用作磁铁矿纳米颗粒（MNP，一种可能的热疗剂）上的无毒、靶向肿瘤和荧光（黄绿色荧光）涂层，随后加载化疗药物 5-氟尿嘧啶(5FU)。MNP 显示出 56.28 emu/g 的饱和磁化强度和 75.5 Oe 的矫顽力。从 TEM 研究证实了具有 PFBT-B 的 MNP 涂层，显示平均壳厚度为 1.88 nm。药物 (5FU) 负载研究显示 PFBT-B 的负载能力约为 6.64 μg/μg，而释放研究显示 pH 敏感的释放曲线，在酸性环境中加速释放药物。MTT 测定表明，与纯 5FU 相比，纳米制剂形式的 5FU 的细胞毒性增强。此外，与 HEK 293T 正常细胞相比，PFBT-B 包被的 MNP 显示出优先定位到 HeLa 癌细胞中。因此，固有的荧光和肿瘤靶向特性表明 PFBT-B 可以作为癌症治疗的潜在治疗诊断平台。而释放研究表明 pH 敏感的释放曲线与药物在酸性环境中加速释放。MTT 测定表明，与纯 5FU 相比，纳米制剂形式的 5FU 的细胞毒性增强。此外，与 HEK 293T 正常细胞相比，PFBT-B 包被的 MNP 显示出优先定位到 HeLa 癌细胞中。因此，固有的荧光和肿瘤靶向特性表明 PFBT-B 可以作为癌症治疗的潜在治疗诊断平台。而释放研究表明 pH 敏感的释放曲线与药物在酸性环境中加速释放。MTT 测定表明，与纯 5FU 相比，纳米制剂形式的 5FU 的细胞毒性增强。此外，与 HEK 293T 正常细胞相比，PFBT-B 包被的 MNP 显示出优先定位到 HeLa 癌细胞中。因此，固有的荧光和肿瘤靶向特性表明 PFBT-B 可以作为癌症治疗的潜在治疗诊断平台。