State Key Laboratory of Agricultural Microbiology, College of Science, Huazhong Agricultural University, Wuhan, 430070, China.
Adv Healthc Mater. 2017 Oct;6(19). doi: 10.1002/adhm.201700470. Epub 2017 Jul 17.
Both excess dosages of drug and unwanted drug carrier can lead to severe side effects as well as the failure of tumor therapy. Here, an Fe -gallic acid based drug delivery system is designed for efficient monitoring of drug release in tumor. Fe and polyphenol gallic acid can form polygonal nanoscale coordination polymer in aqueous solution, which exhibits certain antitumor effect. Importantly, this coordination polymer possesses extremely high doxorubicin (DOX) loading efficacy (up to 48.3%). In vitro studies demonstrate that the fluorescence of DOX can be quenched efficiently when DOX is loaded on the coordination polymer. The acidity in lysosome also triggers the release of DOX and fluorescence recovery simultaneously, which realizes real-time monitoring of drug release in tumor cells. In vivo studies further indicate that this polyphenol-rich drug delivery system can significantly inhibit tumor growth with negligible heart toxicity of DOX. This system with minimal side effects should be a promising nanoplatform for tumor treatment.
过量的药物和不需要的药物载体都可能导致严重的副作用，以及肿瘤治疗的失败。在这里，设计了一种基于 Fe-没食子酸的药物输送系统，用于有效地监测肿瘤中的药物释放。Fe 和没食子酸在水溶液中可以形成多边形纳米级配位聚合物，具有一定的抗肿瘤作用。重要的是，这种配位聚合物具有极高的阿霉素（DOX）负载效率（高达 48.3%）。体外研究表明，当 DOX 负载在配位聚合物上时，DOX 的荧光可以被有效地猝灭。溶酶体中的酸性也同时触发 DOX 的释放和荧光恢复，实现了肿瘤细胞中药物释放的实时监测。体内研究进一步表明，这种富含多酚的药物输送系统可以显著抑制肿瘤生长，而 DOX 的心脏毒性可以忽略不计。这种副作用最小的系统应该是一种很有前途的肿瘤治疗纳米平台。
