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Theranostic liposomes containing conjugated polymer dots and doxorubicin for bio-imaging and targeted therapeutic delivery

机译：含有共轭聚合物点和多柔比星的治疗脂质体，用于生物成像和靶向治疗递送

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摘要

This work was devoted to the development of a lipid-based theranostic nanoparticle able to simultaneously host conjugated polymer dots, doxorubicin (Dox) and folate acid (FA). Poly(9,9-dioctylfluorene-2,7-diyl-co-benzothiadiazole) (PFBT) was chosen as the fluorescent probe because of its high brightness in in vitro cellular uptake studies and good biocompatibility in in vitro/in vivo toxicity experiments. The theranostic liposomes (PFBT-Dox-Lip-FA) exhibited a hydrodynamic size of 127.30 +/- 3.20 (nm) with a zeta potential of -25.00 + 2.00 (mV). Mostly importantly, the extent of Dox release at 24 h from PFBT-Dox-Lip-FA showed a satisfactory result under mild hyperthermia conditions compared with Dox-Lip-FA. Such rapid release led to a lower half maximal inhibitory concentration (IC50) in MCF-7 cells at 16.8 +/- 4.5 (mu g mL (1)), whereas the IC50 of Dox-Lip-FA (37 degrees C) was 28.3 +/- 3.7 (mu g mL(-1)). The cellular uptake study also revealed higher drug accumulation in tumor cells for theranostic liposomes. In vivo studies of PFBT-Dox-Lip-FA on tumor-bearing mouse models revealed that the distribution of liposomes in the tumors could be indicated accurately by PFBT. Besides, tumor-bearing mice could be significantly inhibited by PFBT-Dox-Lip-FA. Together with its negligible in vivo toxicity, PFBT-Dox-Lip-FA is a useful system for simultaneous cancer diagnosis and targeted drug delivery.
机译：该作品致力于开发一种能够同时宿主共轭聚合物点，多柔比蛋白（DOX）和叶酸（FA）的脂质的治疗纳米粒子。选择聚（9,9-二辛基氟醚-2,7-二苯基 - 苯并噻唑）（PFBT）作为荧光探针，因为其在体外细胞摄取研究中具有高亮度和体外/体内毒性实验中的良好生物相容性。 Heranostic脂质体（PFBT-DOX-LIP-FA）表现出127.30 +/- 3.20（NM）的流体动力学大小，Zeta电位为-25.00 + 2.00（MV）。主要是，与DOX-LIP-FA相比，来自PFBT-DOX-LIP-FA的24小时DOX释放的程度显示出令人满意的温和高温病症结果。这种快速释放在16.8 +/- 4.5（mu g ml（1））中，MCF-7细胞中的下半部分抑制浓度（IC50）较低，而Dox-Lip-Fa（37℃）的IC50是28.3 +/- 3.7（mu g ml（-1））。细胞摄取研究还揭示了治疗脂质体肿瘤细胞的较高药物积累。在携带肿瘤小鼠模型上的PFBT-Dox-Lip-Fa的体内研究表明，PFBT可以准确地用肿瘤中脂质体的分布。此外，通过PFBT-DOX-LIP-FA可以显着抑制肿瘤小鼠。 PFBT-Dox-Lip-Fa在体内毒性中可忽略不计，是一种用于同时癌症诊断和靶向药物递送的有用系统。

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  • 来源
    《RSC Advances》 |2016年第3期|共13页
  • 作者

    Ma Man; Lei Mingzhu; Tan Xiaoxiao; Tan Fengping; Li Nan;

  • 作者单位

    Tianjin Univ Sch Pharmaceut Sci &

    Technol Tianjin Key Lab Drug Delivery &

    High Efficiency Tianjin 300072 Peoples R China;

    Tianjin Univ Sch Pharmaceut Sci &

    Technol Tianjin Key Lab Drug Delivery &

    High Efficiency Tianjin 300072 Peoples R China;

    Tianjin Univ Sch Pharmaceut Sci &

    Technol Tianjin Key Lab Drug Delivery &

    High Efficiency Tianjin 300072 Peoples R China;

    Tianjin Univ Sch Pharmaceut Sci &

    Technol Tianjin Key Lab Drug Delivery &

    High Efficiency Tianjin 300072 Peoples R China;

    Tianjin Univ Sch Pharmaceut Sci &

    Technol Tianjin Key Lab Drug Delivery &

    High Efficiency Tianjin 300072 Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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