化疗是临床治疗恶性肿瘤的主要方法。然而，通常使用的化疗药物具有生物毒性高、水溶性差、靶向能力低和副作用大的缺点。由带有离子性基团和靶向配体修饰的两亲性树状分子组装而成的离子性胶束应该能够在很大程度上克服这些缺点。本文利用带有离子性基团和靶向肽c(RGDfC)修饰的第二代聚丙烯酰胺树状分子（G2 PPI）表面进行修饰，并与疏水性N-(2-巯基乙基)油酰胺结合形成两亲性树状分子（PPIMYRC）。PPIMYRC自组装成胶束，内部装载阿霉素（DOX）制备DOX负载胶束（PPIMYRC-DOX胶束）。PPIMYRC-DOX胶束在纤维蛋白原中具有很高的稳定性和pH响应性药物释放。此外，PPIMYRC-DOX胶束的细胞摄取率比自由DOX高，导致PPIMYRC-DOX胶束的细胞毒性比自由DOX高。更重要的是，PPIMYRC-DOX胶束比自由DOX更好地抑制肿瘤。PPIMYRC-DOX胶束抑制肿瘤的率高达93％。综上，PPIMYRC-DOX胶束是由带有离子性和靶向基团的两亲性树状分子组装而成，增强了DOX的治疗效果并降低了其副作用。制备的靶向纳米药物在抗肿瘤治疗中具有极大的潜力。

Chemotherapy is the main method of treating malignant tumors in clinical treatment. However, the commonly used chemotherapeutic drugs have the disadvantages of high biological toxicity, poor water solubility, low targeting ability, and high side effects. Zwitterionic micelles assembled by amphiphilic dendrimers modified with zwitterionic groups and targeting ligand should largely overcome these shortcomings. Herein, the zwitterionic group and targeting peptide c(RGDfC) were modified on the surface of generation 2 poly(propylene imine) dendrimers (G2 PPI), which was conjugated with hydrophobic N-(2-mercaptoethyl) oleamide to form amphiphilic dendrimers (PPIMYRC). PPIMYRC self-assembled into micelles with doxorubicin (DOX) loaded in the interior of micelles to prepare DOX-loaded micelles (PPIMYRC-DOX micelles). The PPIMYRC-DOX micelles had great stability in fibrinogen and pH-responsive drug release. Furthermore, PPIMYRC-DOX micelles had higher cellular uptake rates than free DOX, resulting in higher cytotoxicity of PPIMYRC-DOX micelles than that of free DOX. More importantly, PPIMYRC-DOX micelles inhibited tumors much better than free DOX. The tumor inhibition rate of PPIMYRC-DOX micelles was as high as 93%. Taken together, PPIMYRC-DOX micelles were assembled by amphiphilic dendrimers with the zwitterionic and targeting groups, which enhanced the therapeutic effect of DOX and reduced its side effects. The prepared targeting nanodrug has great potential for further application in antitumor therapy.