Tauro Jovita R, Gemeinhart Richard A
Departments of Biopharmaceutical Sciences and Bioengineering, The University of Illinois, Chicago, Illinois 60612-7231, USA.
Mol Pharm. 2005 Sep-Oct;2(5):435-8. doi: 10.1021/mp050028n.
A novel paradigm for local cancer chemotherapy, based upon local activation of chemotherapeutic molecules by soluble proteases, is presented. In the presence of matrix metalloproteases, a family of cancer-associated proteases, cisplatin is released from a hydrogel matrix in an active form. In the absence of matrix metalloproteases, cisplatin is released at a much lower rate. The mesh size of the polymer controls metalloprotease-based cisplatin release from the hydrogel matrix with approximate doubling of cisplatin release in the presence of matrix metalloprotease. Overall, this novel paradigm shows much potential for local chemotherapy where local chemotherapeutic release is in response to the invasive properties of the tumor.
本文提出了一种基于可溶性蛋白酶对化疗分子进行局部激活的局部癌症化疗新范式。在基质金属蛋白酶（一类与癌症相关的蛋白酶）存在的情况下，顺铂以活性形式从水凝胶基质中释放出来。在没有基质金属蛋白酶的情况下，顺铂的释放速率要低得多。聚合物的网孔大小控制着基于基质金属蛋白酶的顺铂从水凝胶基质中的释放，在基质金属蛋白酶存在时顺铂释放量大约会增加一倍。总体而言，这种新范式在局部化疗方面显示出很大潜力，即局部化疗药物的释放是对肿瘤侵袭特性的响应。
