Biocompatible, pH-sensitive and charge-conversion micelles derived from hyaluronic acid (HA), poly(lactide) (PLA) and half-generation of sectorial poly(amidoamine) dendrimers (sPA G4.5) were designed and fabricated to target delivery of docetaxel (DTX) to cancer cells. The novel micelles (HA-PALA-DTX) possessed stability against rat plasma and were capable of reversing surface zeta potential under acidic conditions in the presence of HAase. Moreover, the blank micelles demonstrated satisfactory biocompatibility and viability for biomedical applications. A cellular internalization experiment indicated that HA played an important role in increasing intracellular accumulation of DTX delivered by the micelles. Compared to Taxotere^® and PALA-DTX, HA-PALA-DTX showed an enhanced anticancer activity in vivo, with a tumor growth inhibition rate of 72.32 ± 5.22%. Overall, the functionalized micelles could be utilized as an alternative carrier for effective targeted delivery of anticancer agents to improve therapeutic efficacy and minimize adverse effects.

设计并制造了透明质酸（HA），聚丙交酯（PLA）和半代扇形聚（酰胺基胺）树枝状大分子（sPA G4.5）衍生的生物相容性，pH敏感和电荷转换胶束。多西紫杉醇（DTX）对癌细胞的作用。新型胶束（HA-PALA-DTX）具有对抗大鼠血浆的稳定性，并能够在酸性条件下在HAase存在的情况下逆转表面Zeta电位。此外，空白胶束表现出令人满意的生物相容性和生物医学应用的生存能力。细胞内化实验表明，HA在增加微团传递的DTX的细胞内积累中起着重要作用。相较于泰索帝^®与PALA-DTX相比，HA-PALA-DTX在体内显示出增强的抗癌活性，肿瘤生长抑制率为72.32±5.22％。总体而言，功能化的胶束可被用作有效靶向递送抗癌药的替代载体，从而改善治疗效果并使副作用最小化。