磷酸钙纳米体系用于顺铂前药的运载

摘要

纳米载药体系能促进铂类广谱抗癌药物的运输和增强药效，并保护作为前药的四价铂在到达细胞前不被还原。以磷酸钙纳米颗粒为基础建立了一种生物兼容性高、制备方法简单的四价铂前药运载体系。通过动态光散射、扫描电镜和 X 射线衍射对颗粒粒径和形貌进行了表征，并研究其细胞摄取效率和细胞毒性。实验结果表明，该纳米载药体系的粒径分布较窄、分散性较好、细胞摄取效率较高，并具有还原响应性，可在胞内还原剂的作用下释放出顺铂，显著提高了四价铂前药对肿瘤细胞的抑制作用。%Drug delivery systems can facilitate the delivery of platinum‐based drugs ,enhance drug efficiency and protect Pt( Ⅳ ) from being reduced before cellular uptake .A highly biocompatible Pt ( Ⅳ ) prodrugs delivery system using calcium phosphate (CaP) nanoparticles with simple preparation procedures were reported .The diameter and morphology of Pt( Ⅳ )/CaP nanoparticles were characterized by dynamic light scattering , scanning electron microscope and X‐ray diffraction . Then cellular uptake efficiency and cytotoxicity were studied . The results indicate that nanoparticles are well‐dispersive with narrow size distribution ;they have high cellular uptake efficiency and redox response so as to release cisplatin after being reduced by cellular reductants .Moreover ,the delivery system demonstrates a significantly higher inhibitory effect than the free Pt( Ⅳ ) prodrug .