具有高载药量的两性离子树枝状纳米药物自组装体，增强抗肿瘤能力。
Zwitterionic dendrimer self-assembled nanodrugs with high drug loading for enhanced anti-tumor ability.
机构信息
State Key Laboratory of Metastable Materials Science and Technology, Hebei Key Laboratory of Nano-biotechnology, Hebei Key Laboratory of Applied Chemistry, Yanshan University, Qinhuangdao 066004, China.
State Key Laboratory of Metastable Materials Science and Technology, Hebei Key Laboratory of Nano-biotechnology, Hebei Key Laboratory of Applied Chemistry, Yanshan University, Qinhuangdao 066004, China.
出版信息
Colloids Surf B Biointerfaces. 2023 Nov;231:113574. doi: 10.1016/j.colsurfb.2023.113574. Epub 2023 Sep 29.
Zwitterionic dendrimers have been used to construct many nanomedicines due to their ability to achieve controlled drug release, but their low drug loading content limits their application in nanodrug delivery. To solve this problem, the surface of second generation polypropylimine (G2 PPI) was modified with mercapturized paclitaxel (PTX-SH) and zwitterionic groups to prepare zwitterionic prodrug molecule (PPIMPC), and then zwitterionic dendrimer self-assembled nanodrugs (PPIMPC-DOX micelles) were prepared by incorporating doxorubicin (DOX) into the micelles. The DOX loading and paclitaxel (PTX) loading in PPIMPC-DOX micelles was 6.7% and 26.2%, respectively, and the total drug loading of PPIMPC-DOX was high to 32.9%. In addition, PPIMPC-DOX micelles showed enhanced cytotoxicity due to improved cell uptake of DOX. More importantly, the inhibition rate of tumor was much higher than free DOX. The zwitterionic property and high drug loading of PPIMPC-DOX micelles enhanced anti-tumor ability of chemotherapeutic drugs. The method of preparation of zwitterionic and high drug loading of nanodrugs shows good application prospects in the future.
两性离子树枝状聚合物由于能够实现控制药物释放，因此已被用于构建许多纳米药物，但它们的载药率低限制了其在纳米药物递送中的应用。为了解决这个问题，第二代聚丙亚胺（G2 PPI）的表面用巯基化紫杉醇（PTX-SH）和两性离子基团进行了修饰，制备了两性离子前药分子（PPIMPC），然后将阿霉素（DOX）包入胶束中制备了两性离子树枝状聚合物自组装纳米药物（PPIMPC-DOX 胶束）。PPIMPC-DOX 胶束中的 DOX 载药量和紫杉醇（PTX）载药量分别为 6.7%和 26.2%，PPIMPC-DOX 的总载药量高达 32.9%。此外，由于 DOX 的细胞摄取增加，PPIMPC-DOX 胶束显示出增强的细胞毒性。更重要的是，肿瘤的抑制率远高于游离 DOX。PPIMPC-DOX 胶束的两性离子性质和高载药量增强了化疗药物的抗肿瘤能力。两性离子纳米药物的制备方法和高载药量显示出良好的应用前景。
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