Poly(lactic-co-glycolic acid) (PLGA) is the most commonly described biocompatible copolymer used in biomedical applications. In this work, a green synthetic approach based on the biocompatible zinc proline complex, as an initiator for PLGA synthesis, is reported for the first time for the synthesis of methoxy-poly(ethylene glycol)-block-poly(L-lactic-co-glycolic acid) (mPEG–PLGA). mPEG–PLGA with controlled molecular weight and narrow polydispersity was synthesised. Its potential for delivery of irinotecan (Ir), a poorly water-soluble chemotherapeutic drug used for the treatment of colon and pancreatic cancer, was studied. Nanoparticles of controlled size (140–160 nm), surface charge (∼−10 mV), release properties and cytotoxicity against CT-26 (colon) and BxPC-3 (pancreatic) cancer cells, were prepared. Tumor accumulation was confirmed by optical imaging of fluorescently labelled nanoparticles. Unlike Tween® 80 coated NP-Ir, the Pluronic® F-127 coated NP-Ir exhibits significant tumor growth delay compared to untreated and blank formulation treated groups in the CT-26 subcutaneous tumor model, after 4 treatments of 30 mg irinotecan per kg dose. Overall, this proof-of-concept study demonstrates that the newly synthesized copolymer, via a green route, is proven to be nontoxic, requires fewer purification steps and has potential applications in drug delivery.

中文翻译：

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使用脯氨酸锌作为生物相容性引发剂将伊立替康体内递送至结肠癌的绿色合成甲氧基-聚（乙二醇）-嵌段-聚（L-丙交酯-乙交酯）共聚物的绿色合成

聚（乳酸-共-glycolic乙酸）（PLGA）是在生物医学应用中使用的最通常描述生物相容性共聚物。在这项工作中，基于所述生物相容的锌脯氨酸络合物的绿色合成方法中，作为用于合成PLGA的引发剂，则报告首次对甲氧基-聚的合成（乙二醇） -嵌段-聚（大号-lactic-共-乙醇酸（mPEG–PLGA）。合成了分子量可控制且多分散性较窄的mPEG-PLGA。研究了其伊立替康（Ir）（一种水溶性差的化疗药物，用于治疗结肠癌和胰腺癌）的传递潜力。制备了尺寸可控的纳米颗粒（140-160 nm），表面电荷（〜-10 mV），针对CT-26（结肠）和BxPC-3（胰腺）癌细胞的释放特性和细胞毒性。通过荧光标记的纳米颗粒的光学成像确认了肿瘤的积累。与Tween®80包被的NP-Ir不同，与CT-26皮下肿瘤模型中未经治疗和空白制剂治疗的组相比，经Pluronic®F-127包被的NP-Ir表现出显着的肿瘤生长延迟，经过4次30 mg伊立替康/ kg治疗剂量。总体，通过绿色途径，被证明是无毒的，需要较少的纯化步骤，并且在药物输送中具有潜在的应用。