Department of Polymer Science and Engineering, Sunchon National University, 255 Jungang-ro, Suncheon, Jeonnam 57922, Republic of Korea.
Biomedical Research Institute, Pusan National University Hospital, Pusan 49241, Republic of Korea.
Carbohydr Polym. 2019 Apr 1;209:161-171. doi: 10.1016/j.carbpol.2019.01.018. Epub 2019 Jan 9.
To develop a carrier for targeted drug delivery and triggered drug release in a reducing-tumor environment, reduction-sensitive hyaluronic acid-g-stearic acid (HCS) micelles were synthesized using a coupling agent. The HCS 40% was shown to have a more compact particle size than HCS 20% and the particle size of doxorubicin (DOX)-loaded HCS (HCSD) was increased relative to that of HCS micelles. The behavior of DOX release from HCSD showed that DOX was rapidly released in GSH (10 mM) solution. The site-specific targeting effect of HCSD nanoparticles was investigated by cellular uptake and competition assay at HCT116 and CT26 cell lines. An in vivo study of HCSD revealed that tumor suppression and site-specific targeted delivery of HCSD nanoparticles in HCT116-xenografted tumors were more superb than in the CT26-xenografted tumor. These results suggest that HCSD nanoparticles can be expected to have high therapeutic efficacy because they enable targeted drug delivery and rapid drug release.
为了在肿瘤微环境中开发一种用于靶向药物输送和触发药物释放的载体，使用偶联剂合成了还原敏感的透明质酸-g-硬脂酸（HCS）胶束。结果表明，HCS40%的粒径比 HCS20%更紧凑，载多柔比星（DOX）的 HCS（HCSD）的粒径相对于 HCS 胶束增加。HCSD 中 DOX 释放的行为表明 DOX 在 GSH（10mM）溶液中迅速释放。通过 HCT116 和 CT26 细胞系的细胞摄取和竞争测定研究了 HCSD 纳米颗粒的位点特异性靶向作用。HCSD 的体内研究表明，HCSD 纳米颗粒在 HCT116 异种移植瘤中的肿瘤抑制和位点特异性靶向递送效果优于 CT26 异种移植瘤。这些结果表明，HCSD 纳米颗粒有望具有高治疗效果，因为它们能够实现靶向药物输送和快速药物释放。
