Institute of Biomedical Materials and Engineering, College of Chemistry and Chemical Engineering, College of Materials Science and Engineering, Qingdao University, Qingdao 266071, China.
Laboratory for New Fiber Materials and Modern Textile, Growing Base for State Key Laboratory, Qingdao University, Qingdao 266071, China.
Int J Mol Sci. 2019 Apr 22;20(8):1961. doi: 10.3390/ijms20081961.
Polymeric micelles (PMs) have been applied widely to transport hydrophobic drugs to tumor sites for cancer treatment. However, the low load efficiency of the drug in the PMs significantly reduces the therapeutic efficiency. We report here that disulfide-linked camptothecin (CPT) as a kind of dimeric drug can be effectively embedded in the core of poly(ε-caprolactone)-poly(ethylene glycol)-poly(ε-caprolactone) (PCL-PEG-PCL) PMs for improving drug-loading efficiency, and PEG can be used as a hydrophilic shell. Moreover, the dimeric CPT-loaded PCL-PEG-PCL PMs exhibited excellent solubility in phosphate-buffered saline (PBS) media and significant cytotoxicity to cancer cells.
聚合物胶束（PMs）已广泛应用于将疏水性药物输送到肿瘤部位以治疗癌症。然而，药物在 PMs 中的低载药效率显著降低了治疗效率。我们在这里报告，二聚体喜树碱（CPT）作为一种药物可以有效地嵌入聚（ε-己内酯）-聚乙二醇-聚（ε-己内酯）（PCL-PEG-PCL）PM 的核心中，以提高载药效率，并且PEG 可以用作亲水性外壳。此外，负载二聚体 CPT 的 PCL-PEG-PCL PMs 在磷酸盐缓冲盐水（PBS）介质中具有优异的溶解度，并对癌细胞表现出显著的细胞毒性。
