Chen Siming, Wang Jin, Cheng Hao, Guo Wenjun, Yu Min, Zhao Qiang, Wu Zhenzhou, Zhao Liqing, Yin Zhinan, Hong Zhangyong
State Key Laboratory of Medicinal Chemical Biology, College of Life Sciences, Nankai University, Tianjin, 300071, P. R. China.
J Pharm Sci. 2015 Jul;104(7):2276-84. doi: 10.1002/jps.24473. Epub 2015 May 11.
Macrophages are important therapeutic targets for various disorders, including infectious diseases, inflammatory diseases, metabolic diseases, and cancer. In this study, we report a novel oral delivery system for the targeted delivery of anti-inflammatory therapeutics to macrophages. Using this formulation, the model drug tylophorine malate (NK007) was tightly incorporated inside beta-glucan particle shells by the formation of colloidal particles with chitosan, tripolyphosphate, and alginate via electrostatic interactions. This formulation specifically delivered NK007 to macrophages in vivo after oral gavage and effectively cured colitis in the dextran sulfate sodium-induced murine colitis model, highlighting the utility of beta-glucan particles as an oral anti-inflammation drug delivery system by targeting macrophages. In this work, NK007 was selected as the model drug. However, this novel oral carrier system has the potential to be applied as a platform for the treatment of many other diseases for which macrophages are the therapeutic targets.
巨噬细胞是包括传染病、炎症性疾病、代谢性疾病和癌症在内的各种疾病的重要治疗靶点。在本研究中，我们报告了一种新型口服给药系统，用于将抗炎治疗药物靶向递送至巨噬细胞。使用该制剂，通过壳聚糖、三聚磷酸钠和海藻酸盐经静电相互作用形成胶体颗粒，模型药物马来酸娃儿藤碱（NK007）被紧密包裹在β-葡聚糖颗粒壳内。该制剂在口服灌胃后能在体内将NK007特异性递送至巨噬细胞，并有效治愈葡聚糖硫酸钠诱导的小鼠结肠炎模型中的结肠炎，突出了β-葡聚糖颗粒作为通过靶向巨噬细胞的口服抗炎药物递送系统的实用性。在这项工作中，选择NK007作为模型药物。然而，这种新型口服载体系统有潜力作为一个平台，用于治疗许多其他以巨噬细胞为治疗靶点的疾病。
