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评价含偶氮苯或香豆素部分的聚乙二醇-聚碳酸酯自组装体作为纳米载体,以紫杉醇为模型疏水性药物。

Evaluation of PEG--polycarbonates self-assemblies containing azobenzene or coumarin moieties as nanocarriers using paclitaxel as a model hydrophobic drug.

机构信息

Instituto de Nanociencia y Materiales de Aragón (INMA), CSIC-Universidad de Zaragoza, Zaragoza, Spain.

Departamento de Química Orgánica, Facultad de Ciencias, Universidad de Zaragoza, Zaragoza, Spain.

出版信息

J Microencapsul. 2022 May;39(3):276-287. doi: 10.1080/02652048.2022.2061621. Epub 2022 Apr 9.

Abstract

The work assesses the performance of nanocarriers from amphiphilic block copolymers with functional azobenzene or coumarin moieties for delivery of paclitaxel. Placlitaxel was encapsulated by the nanoprecipitation method. Characterisations were performed by DLS, TEM, Zeta potential and HPLC. Cell viability was investigated in HeLa and Huh-5-2-cell lines. Coumarin-containing polymeric micelles ( = 26±2nm, PDI=0.28, ζ = ‒22.9±3.6mV) with 11.2±0.5%w/w drug loading showed enhanced cytotoxicity in HeLa cells (IC50<0.02nM) compared to free paclitaxel (IC50=0.17±0.02nM). Azobenzene-containing polymeric vesicles ( = 390±20nm, PDI=0.24, ζ = ‒33.2±5.0mV) with a 6.8±0.4%w/w drug loading showed increased cytotoxicity under 530nm light (IC50=0.0114±0.00033nM) in HeLa cells due to a stimulated delivery of paclitaxel. Effectivity of these block copolymers as paclitaxel nanovectors and light stimulated release has been demonstrated.

摘要

该工作评估了具有功能化偶氮苯或香豆素部分的两亲嵌段共聚物的纳米载体在紫杉醇传递中的性能。采用纳米沉淀法包载紫杉醇。通过 DLS、TEM、Zeta 电位和 HPLC 进行了表征。在 HeLa 和 Huh-5-2 细胞系中研究了细胞活力。载有香豆素的聚合物胶束( = 26±2nm,PDI=0.28,ζ = -22.9±3.6mV),药物载量为 11.2±0.5%w/w,与游离紫杉醇(IC50=0.17±0.02nM)相比,在 HeLa 细胞中显示出增强的细胞毒性(IC50<0.02nM)。载有偶氮苯的聚合物囊泡( = 390±20nm,PDI=0.24,ζ = -33.2±5.0mV),药物载量为 6.8±0.4%w/w,在 HeLa 细胞中在 530nm 光下显示出增强的细胞毒性(IC50=0.0114±0.00033nM),这是由于紫杉醇的刺激释放。已经证明了这些嵌段共聚物作为紫杉醇纳米载体和光刺激释放的有效性。

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