Gao Peng Fei, Zheng Lin Ling, Liang Li Jiao, Yang Xiao Xi, Li Yuan Fang, Huang Cheng Zhi
Education Ministry Key Laboratory on Luminescence and Real-Time Analysis, College of Pharmaceutical Sciences, Southwest University, Chongqing, 400715, China.
J Mater Chem B. 2013 Jul 7;1(25):3202-3208. doi: 10.1039/c3tb00026e. Epub 2013 May 24.
A new type of coordination polymer sphere prepared by combining 1,1'-(1,4-butanediyl)bis(imidazole) (bbi) and ferrous ions has been demonstrated as a targeted delivery system for in situ encapsulating anticancer drugs. These stable coordination polymer spheres can be fabricated simply by a deposition method. Drugs, doxorubicin hydrochloride (DOX·HCl) for example, can be easily in situ encapsulated by simply mixing the drug with bbi ligand through the deposition method and results in a high drug loading efficiency up to 98% and a drug loading content of nearly 40%, which is remarkably high for not only metal-organic but also other materials. A noticeable feature of the drug loaded coordination polymer spheres is that they show sustainable drug release for several days due to their superior stability, and are sensitive to external pH owing to the coordination bonds. The drug can be released faster in mild acidic conditions in comparison to physiological acidity. By conjugating folic acid to the surface of the coordination polymer spheres, the vehicles can be taken up selectively by cancer cells through cell surface receptor-mediated mechanisms. Cell viability experiments with HeLla cells demonstrated the low toxicity of the delivery vehicles and the good anticancer efficacy of the drug-loaded coordination polymer spheres.
一种通过将1,1'-(1,4-丁二醇)双(咪唑)(bbi)与亚铁离子结合制备的新型配位聚合物球已被证明是一种用于原位包封抗癌药物的靶向递送系统。这些稳定的配位聚合物球可以通过沉积法简单制备。例如,药物盐酸阿霉素(DOX·HCl),通过沉积法将药物与bbi配体简单混合,即可轻松实现原位包封,药物负载效率高达98%,负载量接近40%,这不仅对于金属有机材料,而且对于其他材料来说都是非常高的。负载药物的配位聚合物球的一个显著特点是,由于其卓越的稳定性,它们能持续释放药物数天,并且由于配位键的存在,对外部pH敏感。与生理酸度相比,药物在轻度酸性条件下释放得更快。通过将叶酸缀合到配位聚合物球的表面,载体可以通过细胞表面受体介导的机制被癌细胞选择性摄取。对HeLla细胞进行的细胞活力实验证明了递送载体的低毒性以及负载药物的配位聚合物球良好抗癌效果。