磷酸钙纳米体系用于顺铂前药的运载

Calcium phosphate nanoparticles for the delivery of the prodrug of cisplatin

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.