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One-Step and Facile Synthesis of Poly(phenylalanine) as a Robust Drug Carrier for Enhanced Cancer Therapy
ACS Applied Materials & Interfaces ( IF 9.5 ) Pub Date : 2021-10-14 , DOI: 10.1021/acsami.1c13013
Yabin Meng 1 , Jun Wu 1
Affiliation  

In recent decades, many poly(amino acid)s have been successfully prepared for various biomedical applications. To date, the synthesis and purification procedures used to generate these poly(amino acid)s have generally been complicated and costly. Here, a one-step synthesis strategy was developed and optimized via direct polymerization using thionyl chloride to easily and economically obtain poly(amino acid)s. Phenylalanine (Phe) was selected as a model amino acid to construct a family of biodegradable and biocompatible poly(phenylalanine) (PPhe) molecules with a tunable molecular weight. The prepared PPhe can self-assemble into nanoparticles (PP-NPs) through nanoprecipitation with a particle size of approximately 100 nm. PP-NPs exhibit a high drug-loading capacity (>12 wt %) of paclitaxel (PTX, a commercial antitumor drug) and good therapeutic effects in CT26 cells. The in vivo evaluation of PTX@PP-NPs indicates that it has a prolonged blood circulation time and high tumor aggregation after intravenous injection, resulting in significant antitumor effects in CT26 tumor-bearing mice with minimal toxicity to normal organs. Overall, this study provides a facile and simple strategy for synthesizing poly(amino acids) and a PPhe-based nanoparticle platform for effectively delivering various small-molecule drugs.

中文翻译:

聚苯丙氨酸的一步简便合成作为增强癌症治疗的强大药物载体

近几十年来,许多聚(氨基酸)已成功制备用于各种生物医学应用。迄今为止,用于产生这些聚(氨基酸)的合成和纯化程序通常是复杂且昂贵的。在这里,通过使用亚硫酰氯直接聚合开发和优化一步合成策略,以轻松经济地获得聚(氨基酸)。苯丙氨酸 (Phe) 被选为模型氨基酸,以构建具有可调分子量的可生物降解和生物相容性聚苯丙氨酸 (PPhe) 分子家族。制备的PPhe可以通过纳米沉淀自组装成纳米颗粒(PP-NPs),粒径约为100 nm。PP-NPs 表现出高载药能力 (>12 wt%) 的紫杉醇 (PTX, 一种商业抗肿瘤药物)和对 CT26 细胞的良好治疗效果。PTX@PP-NPs的体内评价表明,它在静脉注射后具有延长的血液循环时间和高肿瘤聚集性,从而在CT26荷瘤小鼠中产生显着的抗肿瘤作用,对正常器官的毒性最小。总体而言,这项研究为合成聚(氨基酸)和基于 PPhe 的纳米粒子平台提供了一种简便易行的策略,以有效地传递各种小分子药物。
更新日期:2021-10-27
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