Polymeric micelles with simultaneous bioimaging, drug delivery monitoring, and effective delivery of therapeutic agents to target sites have attracted increasing attention in cancer therapy. In this study, a new biodegradable, pH-responsive, aggregation-induced emission (AIE)-active polycarbonate brush-like polymer was developed by combining ring-opening polymerization with click reaction. The anticancer drug, doxorubicin (DOX), was covalently conjugated to the polymer backbone via acid-sensitive Schiff base linkage, resulting in the pH-sensitive controlled release of DOX. The prodrug polymer self-assembled into nanomicelles in an aqueous solution, as confirmed using dynamic light scattering and transmission electron microscopy. Fluorescence imaging results demonstrated that prodrug micelles could be traced owing to the AIE features of micelles. In vitro drug release studies showed that DOX release was faster in acidic conditions (pH 5.0), whereas only a minimal amount of DOX was released in a physiological environment (pH 7.4). In summary, these smart prodrug micelles could be promising candidates for simultaneous intracellular imaging and cancer therapy.

具有同步生物成像、药物递送监测和治疗剂有效递送至靶位点的聚合物胶束在癌症治疗中引起了越来越多的关注。在这项研究中，通过将开环聚合与点击反应相结合，开发了一种新的可生物降解、pH 响应、聚集诱导发射 (AIE) 活性聚碳酸酯刷状聚合物。抗癌药物阿霉素 (DOX) 通过对酸敏感的席夫碱键共价结合到聚合物骨架上，导致 DOX 的 pH 敏感控制释放。使用动态光散射和透射电子显微镜证实，前药聚合物在水溶液中自组装成纳米胶束。荧光成像结果表明，由于胶束的 AIE 特征，可以追踪前药胶束。体外药物释放研究表明，在酸性条件下（pH 5.0）DOX 释放更快，而在生理环境（pH 7.4）中仅释放极少量 DOX。总之，这些智能前药胶束可能是同时进行细胞内成像和癌症治疗的有希望的候选者。