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自组装温敏性聚(乳酸-共-乙醇酸)接枝普鲁兰纳米粒用于肿瘤协同热化疗。

Self-organized thermo-responsive poly (lactic-co-glycolic acid)-graft-pullulan nanoparticles for synergistic thermo-chemotherapy of tumor.

机构信息

Department of Pharmaceutics, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.

Department of Traditional Chinese Medicine, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.

出版信息

Carbohydr Polym. 2020 Jun 1;237:116104. doi: 10.1016/j.carbpol.2020.116104. Epub 2020 Mar 2.

Abstract

Poly (lactic-co-glycolic acid)-graft-pullulan (PPLGA) based self-organized nanoparticles hold immense potential for synergistic thermo-chemotherapy of tumor. Herein, the biocompatible and biodegradable PPLGA were synthesized by a novel microwave-assisted solution polymerization. The polymers showed thermo-responsive properties, which was attributed to the change of polymer-water hydrogen bonding in controlling the macromolecular contraction, chain collapse as a result of changes in micro-rigidity of core. The curcumin loaded PPLGA nanoparticles (CUR-PPLGA-N), with impressively high drug loading (10.85 ± 0.27 %), exhibited temperature dependence in drug release kinetics. The results of both MTT and antitumor efficiency elucidated that the CUR-PPLGA-N under high temperature facilitated on-demand drug release from the nano-assembly and had a synergistic therapeutic effect for cancer. Thus the developed thermo-responsive PPLGA addressed concerns related to the low drug loading and inefficient drug release at target sites, and might be considered as a powerful nanoplatform for synergistic thermo-chemotherapy of tumor.

摘要

基于聚(乳酸-共-乙醇酸)接枝普鲁兰(PPLGA)的自组装纳米颗粒在肿瘤协同热化疗方面具有巨大的潜力。本文通过一种新的微波辅助溶液聚合方法合成了具有生物相容性和可生物降解性的 PPLGA。聚合物表现出热响应特性,这归因于聚合物-水氢键的变化,控制了大分子的收缩,由于核的微刚性变化导致链的坍塌。载姜黄素的 PPLGA 纳米颗粒(CUR-PPLGA-N)具有令人印象深刻的高药物载量(10.85±0.27%),在药物释放动力学中表现出温度依赖性。MTT 和抗肿瘤效率的结果表明,高温下的 CUR-PPLGA-N 有利于纳米组装体中按需释放药物,并对癌症具有协同治疗效果。因此,开发的温敏性 PPLGA 解决了与目标部位药物载量低和药物释放效率低相关的问题,它可能被认为是肿瘤协同热化疗的一种强大的纳米平台。

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