用于靶向递送阿霉素的ph敏感聚合物纳米颗粒

Yuzhe Yuan, Shuyao Geng, Chenxi Li, Jiayuan Yang
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引用次数: 0

摘要

为了提高阿霉素的靶向性,延长药物的作用时间,我们合成了一种ph响应的PEG-Schiff-DOX聚合物前药。采用聚乙二醇- cho的合成和聚乙二醇- cho与阿霉素的缩合反应制备纳米颗粒。对PEG-Schiff-DOX在不同pH下的释放行为进行了测试。酸处理(pH=5.0)后,PEG-Schiff-DOX纳米颗粒的形貌和粒径发生了明显变化,部分纳米颗粒已经完全崩解。粒径分布的变窄表明,非均质纳米颗粒在肿瘤细胞的酸性环境中分解,释放药物,最终在pH 5.0时达到最大药物释放。基于高分子前药的纳米药物制备简单、载药量高、储存稳定性好,在肿瘤微环境弱酸条件下可达到较高的局部药物浓度和较长的药物作用时间,既能保持疗效又能减少副作用。这一优势为新药的开发提供了选择,有望在癌症治疗中取得良好的应用,具有良好的发展前景。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
PH-Sensitive Polymeric Nanoparticles for Targeted Delivery of Doxorubicin
In order to improve the targeting of doxorubicin and prolong the action time of the drug, we synthesized a pH-responsive PEG-Schiff-DOX polymer prodrug loaded with nanoparticles. The nanoparticles were prepared by synthesis of PEG-CHO and condensation reaction of PEG-CHO and adriamycin. The release behavior of PEG-Schiff-DOX was tested at different pH. The morphology and particle size of these nanoparticles changed obviously after acid treatment(pH=5.0), and some of them had completely disintegrated. The narrowing of particle size distribution indicates that the heterogeneous nanoparticles disintegrate in the acidic environment of tumor cells, releasing the drug and finally achieving the maximum drug release at pH 5.0. The nanodrugs based on polymeric prodrug had advantages of simple preparation, high drug loading, good storage stability and achieve higher local drug concentration and longer drug action time under the condition of weak acid of tumor microenvironment to keep the curative effect and reduce the side effects. The advantages of offers choices for the development of new drugs and is expected to achieve good application in cancer therapy, has good prospects for development.
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