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Cationic Poly(amide-imide)-Conjugated Camptothecin Prodrug with Variable Nanomorphology for Efficient Reductive-Responsive Drug Delivery
European Polymer Journal ( IF 6 ) Pub Date : 2020-01-01 , DOI: 10.1016/j.eurpolymj.2019.109462
Mengzhen Wang , Junjie Yan , Cong Li , Xinyu Wang , Jianjun Xiong , Donghui Pan , Lizhen Wang , Yuping Xu , Xiaotian Li , Min Yang

Abstract Poly(amide-imide)s (PAIs) present limited use in bioapplications due to their poor aqueous solubility and difficulty in functional accessibility. Herein, we prepared PAI-based prodrugs by leveraging aliphatic PAIs as the polymer scaffolds and conjugating camptothecin (CPT) via thiol-disulfide exchange reaction. The degree of CPT attachment can be smoothly controlled by initial feed ratios of PEG and a pyridinedisulfide-modified CPT precursor. Due to the abundant secondary amine groups in PAI backbones, amphiphilic PAI-CPT prodrugs self-assembled into cationic nanoparticles and showed an efficient cellular internalization (

中文翻译:

具有可变纳米形态的阳离子聚(酰胺-酰亚胺)-共轭喜树碱前药,用于有效的还原反应药物递送

摘要 聚(酰胺-酰亚胺)(PAI)由于水溶性差和功能可及性困难,在生物应用中的应用有限。在此,我们通过利用脂肪族 PAI 作为聚合物支架并通过硫醇-二硫化物交换反应结合喜树碱 (CPT) 来制备基于 PAI 的前药。CPT 的附着程度可以通过 PEG 和吡啶二硫化物修饰的 CPT 前体的初始进料比来平稳控制。由于 PAI 主链中丰富的仲胺基团,两亲性 PAI-CPT 前药自组装成阳离子纳米颗粒并显示出有效的细胞内化。
更新日期:2020-01-01
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