FSBIS Institute of Macromolecular Compounds of the Russian Academy of Sciences, Saint-Petersburg, Russia.
Pavlov Saint-Petersburg Medical University, Saint-Petersburg, Russia.
J Microencapsul. 2021 May;38(3):164-176. doi: 10.1080/02652048.2021.1872724. Epub 2021 Feb 21.
In order to prolong the release and reduce the toxicity of anticancer drug - doxorubicin (DOX), delivery systems (DS) using different polyanions have been developed. Structural (size, morphological stability) and functional (encapsulation efficiency, DOX release) characteristics of three types of DS are compared: CaCO porous vaterites doped with polyanions by co-precipitation and coating techniques, and DOX-polyanion conjugates. Using scanning electron microscopy (SEM) and energy dispersive X-ray spectroscopy (EDS), it was shown that the doping enhances the morphological stability of CaCO-based DS during the DOC loading. Doping of CaCO cores by co-precipitation reduces its sizes (up to 1 µm) and DOX encapsulation efficiency. Polyanion-coated CaCO cores and polyanion drug conjugates show about 98 w/w% DOX encapsulation. For the first time, it was shown that the release of DOX from developed DS into human blood plasma is more intense (from 1.3 to 3.0 times for different DS) than into model tumour environment.
为了延长抗癌药物阿霉素（DOX）的释放时间并降低其毒性，已经开发出了使用不同聚阴离子的给药系统（DS）。比较了三种 DS 的结构（尺寸、形态稳定性）和功能（包封效率、DOX 释放）特性：通过共沉淀和涂层技术掺杂聚阴离子的 CaCO 多孔 Vaterites，以及 DOX-聚阴离子缀合物。使用扫描电子显微镜（SEM）和能谱（EDS）表明，掺杂在 DOX 加载过程中增强了基于 CaCO 的 DS 的形态稳定性。通过共沉淀掺杂 CaCO 核可减小其尺寸（最大可达 1μm）并降低 DOX 的包封效率。聚阴离子包覆的 CaCO 核和聚阴离子药物缀合物的 DOX 包封率约为 98 w/w%。首次表明，开发的 DS 向人血浆中的 DOX 释放比向模型肿瘤环境中的释放更为剧烈（对于不同的 DS，释放强度增加 1.3 到 3.0 倍）。
