Novel chondroitin sulfate A conjugated doxorubicin (CSA-DOX) was synthesized and characterized. The mean diameter of CSA-DOX was 152 nm analyzed by dynamic light scattering (DLS). Further, DOX was physically encapsulated into the CSA-DOX nanoparticles. Total amounts of DOX in three kinds of DOX-loaded CSA-DOX (CSA-DOX/DOX) nanoparticles were from 21.8 to 24.2%. The mean diameters of three CSA-DOX/DOX nanoparticles were in the range of 167–177 nm. The shape of CSA-DOX/DOX nanoparticles was almost spherical. DOX released from DOX-loaded nanoparticles exhibited a biphasic way in phosphate buffered saline (PBS, pH 7.4). Cellular uptake studies exhibited that CSA-DOX and CSA-DOX/DOX nanoparticles could enhance the uptake of DOX into CD44 receptor-positive A549 cells. Moreover, the cytotoxicity of CSA-DOX/DOX nanoparticles against A549 cells significantly improved in contrast with free DOX and CSA-DOX nanoparticles. These results suggested that CSA-DOX copolymer could be a potential carrier for antitumor drug delivery. Graphical abstract

中文翻译：

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基于硫酸软骨素 A 的两亲性纳米颗粒的制备和表征与疏水性药物增强阿霉素递送

合成并表征了新型硫酸软骨素 A 共轭多柔比星 (CSA-DOX)。通过动态光散射 (DLS) 分析 CSA-DOX 的平均直径为 152 nm。此外，DOX 被物理封装在 CSA-DOX 纳米颗粒中。三种载有 DOX 的 CSA-DOX (CSA-DOX/DOX) 纳米粒子中 DOX 的总量为 21.8% 至 24.2%。三个 CSA-DOX/DOX 纳米颗粒的平均直径在 167-177 nm 的范围内。CSA-DOX/DOX 纳米颗粒的形状几乎是球形的。从负载 DOX 的纳米粒子释放的 DOX 在磷酸盐缓冲盐水 (PBS, pH 7.4) 中表现出双相方式。细胞摄取研究表明，CSA-DOX 和 CSA-DOX/DOX 纳米颗粒可以增强 DOX 对 CD44 受体阳性 A549 细胞的摄取。而且，与游离 DOX 和 CSA-DOX 纳米颗粒相比，CSA-DOX/DOX 纳米颗粒对 A549 细胞的细胞毒性显着提高。这些结果表明 CSA-DOX 共聚物可能是抗肿瘤药物递送的潜在载体。图形概要