School of Chemistry and Pharmaceutical Engineering, Shandong First Medical University & Shandong Academy of Medical Science, Taian, Shandong, 271016, PR China.
School of Chemistry and Pharmaceutical Engineering, Shandong First Medical University & Shandong Academy of Medical Science, Taian, Shandong, 271016, PR China.
Colloids Surf B Biointerfaces. 2020 Jan 1;185:110590. doi: 10.1016/j.colsurfb.2019.110590. Epub 2019 Oct 16.
Since low pH value is widely observed in most of solid tumors, pH-responsive drug delivery system (DDS) can provide a general strategy for tumor-targeting therapy. In this work, a traceable and pH-responsive DDS (MoS-PEG-DOX) based on MoS quantum dots (MoS QDs) is successfully developed by covalently grafting MoS QDs with diamine-terminated oligomeric polyethylene glycol (PEG) and then loading with a fluorescent antineoplastic anthracycline drug, doxorubicin (DOX). The functionalization of MoS QDs with PEG imparts the nanocomposite with strong blue photoluminescence, low cytotoxicity, and excellent physiological stability. The MoS-PEG-DOX nano-assembly can be effectively taken up by U251 cells, and an accelerated DOX release is then triggered by intracellular acid condition, which in turn diminishing unwanted side effects derived by the incorporation of DOX into healthy cells. Meanwhile, the cellular uptake of the MoS-PEG-DOX nano-assembly, consequent DOX release and the localization of nanocarrier can be real-time monitored due to the inherent stable fluorescence of MoS-PEG and DOX. These findings demonstrate that MoS-PEG-DOX will be promising for high treatment efficacy with minimal side effects in future therapy.
由于大多数实体瘤中普遍存在低 pH 值,因此 pH 响应型药物递送系统 (DDS) 可为肿瘤靶向治疗提供一种通用策略。在这项工作中,通过将 MoS 量子点 (MoS QDs) 与二胺封端的低聚聚乙二醇 (PEG) 共价接枝,然后负载荧光抗癌蒽环类药物阿霉素 (DOX),成功开发出一种基于 MoS QDs 的可追踪和 pH 响应型 DDS (MoS-PEG-DOX)。PEG 对 MoS QDs 的功能化赋予了纳米复合材料强的蓝色光致发光、低细胞毒性和优异的生理稳定性。MoS-PEG-DOX 纳米组装体可被 U251 细胞有效摄取,然后通过细胞内酸性条件触发 DOX 的加速释放,从而减少因将 DOX 掺入健康细胞而产生的不必要的副作用。同时,由于 MoS-PEG 和 DOX 的固有稳定荧光,可实时监测 MoS-PEG-DOX 纳米组装体的细胞摄取、随后的 DOX 释放和纳米载体的定位。这些发现表明,MoS-PEG-DOX 有望在未来的治疗中实现高治疗效果和最小的副作用。