Polymer-drug conjugates have several advantages in controlled drug delivery to inflammation as they can accumulate and release the drug in inflamed tissues or cells, which could circumvent the shortcomings of current therapy. To improve the therapeutic potential of polymer-drug conjugates in joint inflammation, we synthesized polymer conjugates based on N-(2-hydroxypropyl) methacrylamide) copolymers labeled with a near-infrared fluorescent dye and covalently linked to the anti-inflammatory drug dexamethasone (DEX). The drug was bound to the polymer via a spacer enabling pH-sensitive drug release in conditions mimicking the environment inside inflammation-related cells. An in vivo murine model of adjuvant-induced arthritis was used to confirm the accumulation of polymer conjugates in arthritic joints, which occurred rapidly after conjugate application and remained until the end of the experiment. Several tested dosage schemes of polymer DEX-OPB conjugate showed superior anti-inflammatory efficacy. The highest therapeutic effect was obtained by repeated i.p. application of polymer conjugate (3 × 1 mg/kg of DEX eq.), which led to a reduction in the severity of inflammation in the ankle by more than 90%, compared to 40% in mice treated with free DEX.

中文翻译：

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Ph敏感释放地塞米松的聚合物纳米药物用于炎症的局部治疗。

聚合物-药物缀合物在控制药物向炎症的传递方面具有多个优势，因为它们可以在发炎的组织或细胞中积聚并释放药物，这可以避免当前疗法的缺点。为了提高聚合物-药物缀合物在关节炎症中的治疗潜力，我们合成了基于N的聚合物缀合物-（2-羟丙基）甲基丙烯酰胺）共聚物标记有近红外荧光染料，并与抗炎药地塞米松（DEX）共价连接。该药物通过间隔物与聚合物结合，从而在与炎症相关的细胞内部环境相似的条件下释放出对pH敏感的药物。使用佐剂诱导的关节炎的体内鼠模型来证实聚合物缀合物在关节炎关节中的积累，其在施用缀合物后迅速发生并且一直保持到实验结束。聚合物DEX-​​OPB偶联物的几种测试剂量方案均显示出优异的抗炎功效。重复腹膜内施用聚合物结合物（3×1 mg / kg DEX当量）可获得最高的治疗效果，