Doxorubicin shows good anticancer activity, but poor pharmacokinetic property and high organ toxicity restrict its clinical application. The synthesized phenylboronic acid‐modified F127‐chitosan conjugate was used to prepare doxorubicin‐loaded micelles through dialysis method. The physicochemical properties of the doxorubicin‐loaded micelles were characterized. These micelles were further evaluated for in vitro release/cytotoxicity, in vivo activity/biosafety, and pharmacokinetic studies. in vitro release experiment demonstrated that the release of doxorubicin from drug‐loaded micelles was pH‐dependent. in vitro cytotoxic study showed that the introduction of phenylboronic acid resulted in lower IC₅₀ against B16 cells than that in non‐modified F127‐chitosan micelles group, and the doxorubicin‐loaded micelles displayed lower in vitro activity against B16, A549, and HT‐29 cells than free doxorubicin did. However, in vivo experiments confirmed that the doxorubicin‐loaded micelles were safe for mouse main organs, obviously improved pharmacokinetic parameters of doxorubicin in rat and achieved comparable inhibition of tumor growth with no animal death in B16‐bearing mice models throughout the experiment when compared with free doxorubicin. The phenylboronic acid‐sialic acid interaction and pH‐sensitive drug release might play important roles in increased tumor targeting and therapeutic effect of the doxorubicin‐loaded micelles.

中文翻译：

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苯硼酸功能化 F127-低聚壳聚糖共轭胶束用于阿霉素包封。

多柔比星显示出良好的抗癌活性，但药代动力学差和器官毒性高限制了其临床应用。合成的苯基硼酸修饰的 F127-壳聚糖偶联物用于通过透析法制备载有阿霉素的胶束。表征了载有阿霉素的胶束的理化性质。进一步评估了这些胶束的体外释放/细胞毒性、体内活性/生物安全性和药代动力学研究。体外释放实验表明，阿霉素从载药胶束中的释放是 pH 依赖性的。体外细胞毒性研究表明，苯硼酸的引入导致较低的 IC ₅₀与未修饰的 F127-壳聚糖胶束组相比，对 B16 细胞的抑制作用，并且载有阿霉素的胶束对 B16、A549 和 HT-29 细胞的体外活性低于游离阿霉素。然而，体内实验证实，载有阿霉素的胶束对小鼠主要器官是安全的，在整个实验过程中，载有 B16 的小鼠模型中阿霉素的药代动力学参数明显改善，并且在无动物死亡的情况下实现了可比的肿瘤生长抑制。游离阿霉素。苯基硼酸-唾液酸相互作用和 pH 敏感的药物释放可能在增加载有阿霉素的胶束的肿瘤靶向和治疗效果方面发挥重要作用。