Abstract

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: CaCO₃ 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 CaCO₃-based DS during the DOC loading. Doping of CaCO₃ cores by co-precipitation reduces its sizes (up to 1 µm) and DOX encapsulation efficiency. Polyanion-coated CaCO₃ 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 tumor environment.

摘要

为了延长抗癌药物阿霉素（DOX）的释放并降低其毒性，已经开发了使用不同聚阴离子的递送系统（DS）。比较了三种类型DS的结构（尺寸，形态稳定性）和功能（包封效率，DOX释放）特性：通过共沉淀和涂覆技术掺杂了聚阴离子的CaCO ₃多孔钙钛矿和DOX-聚阴离子共轭物。使用扫描电子显微镜（SEM）和能量色散X射线光谱（EDS），结果表明，在DOC加载过程中，掺杂增强了基于CaCO ₃的DS的形态稳定性。通过共沉淀掺杂CaCO ₃核可减小其尺寸（最大1 µm）和DOX封装效率。聚阴离子涂层碳酸钙_3个核心和聚阴离子药物共轭物显示约98 w / w％的DOX包封。首次表明，与模型肿瘤环境相比，从发达的DS向人血浆释放的DOX更为强烈（对于不同的DS为1.3到3.0倍）。