Wang Chongzhi, Tang YiKai, Li Cheng, Wu Wei, Jiang Xiqun
Department of Polymer Science & Engineering, College of Chemistry & Chemical Engineering, and Jiangsu Key Laboratory for Nanotechnology, Nanjing University, Nanjing, 210093, P.R. China.
Biomater Sci. 2025 Jan 28;13(3):617-626. doi: 10.1039/d4bm01121j.
Nanomedicines whose size can be varied on demand may synchronously achieve excellent tumor accumulation and penetration. In this study, by taking advantage of the pH sensitivity of a boronate ester, we synthesized acid-triggered size-reducing polymer nanoparticles (named PCD) by cross-linking β-cyclodextrin-cored multiarm polymers through the boronate ester. In PCD, the antitumor agent doxorubicin was loaded the pH-sensitive hydrazone linkage. The and properties of PCD were investigated using a non-responsive nanoparticle (named UCD) as a reference. In the neutral condition of the bloodstream, PCD was stable and exhibited a suitable size for long circulation time. Upon entering tumors, PCD decomposed into stable and smaller multiarm polymers, which could deeply penetrate tumors. The high tumor accumulation and penetration of PCD offered significantly better anti-tumor efficacy than UCD.
尺寸可按需变化的纳米药物可能会同时实现出色的肿瘤蓄积和渗透。在本研究中，利用硼酸酯的pH敏感性，我们通过硼酸酯将β-环糊精为核心的多臂聚合物交联，合成了酸触发的尺寸减小的聚合物纳米颗粒（命名为PCD）。在PCD中，抗肿瘤剂阿霉素通过pH敏感的腙键负载。以无反应性纳米颗粒（命名为UCD）作为对照，对PCD的[此处原文缺失相关内容]和[此处原文缺失相关内容]性质进行了研究。在血液的中性条件下，PCD是稳定的，并且呈现出适合长循环时间的尺寸。进入肿瘤后，PCD分解为稳定且更小的多臂聚合物，这些聚合物能够深入渗透肿瘤。PCD的高肿瘤蓄积和渗透能力提供了比UCD显著更好的抗肿瘤疗效。
