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甲川花青紫杉醇缀合物用于光热诱导化疗。

Merocyanine-paclitaxel conjugates for photothermal induced chemotherapy.

机构信息

State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry Chinese Academy of Sciences, Changchun 130022, P. R. China.

出版信息

J Mater Chem B. 2021 Mar 11;9(9):2334-2340. doi: 10.1039/d0tb02569k.

Abstract

Small molecular nanomedicines that integrate the flexibility of self-assembly strategies and the advantages of a precise molecular structure, a high drug content and controlled drug release are effective diagnostic and therapeutic modalities. Herein, merocyanine-paclitaxel conjugates (MC-PTX) were developed and fabricated by using the degradable ester bonds as the linker. The as-prepared MC-PTX could self-assemble into nanoparticles (MC-PTX NPs) using the non-covalent molecular interaction via the nanoprecipitation method. MC-PTX NPs possess a favorable biological stability and can efficiently release the paclitaxel (PTX) activated by the heat of the photoactive material merocyanine under light illumination, as monitored using dynamic light scattering. The obtained MC-PTX NPs could be endocytosed into cancer cells and release PTX under laser irradiation in the cytoplasm, thus eliciting a satisfactory anticancer effect. Photothermal triggered degradation upon light illumination could enhance the chemotherapeutic efficacy of paclitaxel. The fluorescent nature of the NPs could visualize the internalization process. We believe that this robust nanomedicine offers a novel strategy to facilitate clinical translation for use as a small molecular chemotherapy nanomedicine.

摘要

小分子纳米药物将自组装策略的灵活性和精确分子结构、高药物含量和控制药物释放的优势结合在一起,是一种有效的诊断和治疗方式。本文通过使用可降解酯键作为连接物,开发并制备了花青素-紫杉醇偶联物(MC-PTX)。所制备的 MC-PTX 可以通过纳米沉淀法通过非共价分子相互作用自组装成纳米颗粒(MC-PTX NPs)。MC-PTX NPs 具有良好的生物稳定性,并且可以在光照射下通过光活性材料花青素的热量有效地释放紫杉醇(PTX),如动态光散射所监测到的。所得的 MC-PTX NPs 可以被癌细胞内吞,并在细胞质中的激光照射下释放 PTX,从而产生令人满意的抗癌效果。光触发降解可以增强紫杉醇的化疗效果。纳米颗粒的荧光性质可以可视化内化过程。我们相信,这种强大的纳米药物为小分子化疗纳米药物的临床转化提供了一种新的策略。

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