Construction of Dimeric Drug-Loaded Polymeric Micelles with High Loading Efficiency for Cancer Therapy
Construction of Dimeric Drug-Loaded Polymeric Micelles with High Loading Efficiency for Cancer Therapy
复制标题
用于癌症治疗的高负载效率二聚体载药聚合物胶束的构建
DOI：
10.3390/ijms20081961
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发表时间：
2019
影响因子：
5.6
通讯作者：
Hailin Cong
中科院分区：
文献类型：
--
作者：
Bing Yu;Qingye Meng;Hao Hu;Tao Xu;Youqing Shen;Hailin Cong
聚合物胶束（PMs）已被广泛应用于将疏水性药物转运到肿瘤部位以用于癌症治疗。然而，药物在PM中的低负载效率显著降低了治疗效率。本文报道了二硫键连接的喜树碱（CPT）作为一种二聚体药物可以有效地嵌入聚己内酯-聚乙二醇-聚己内酯（PCL-PEG-PCL）微球的核中，以提高载药效率，而PEG可以作为亲水性壳层。此外，二聚体CPT负载的PCL-PEG-PCL PM在磷酸盐缓冲盐水（PBS）介质中表现出优异的溶解性和对癌细胞的显著细胞毒性。
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.