Novel drug delivery system using thermo-reversible polymer for brain tumor

MG132是一种蛋白酶体抑制剂，在体外可诱导实验性恶性肿瘤细胞凋亡。然而，其全身毒性阻止了其在临床环境中的进一步使用。为了避免这种毒性，MG132可以直接递送到肿瘤。我们测试了掺入热可逆凝胶化聚合物（TGP）中的MG 132用于治疗实验性胶质瘤细胞系的功效，用MTT测定法测量。作为半胱天冬酶活性测定，在CytoFluor多孔板读数器中测量半胱天冬酶3、8和9的活性。在两种细胞系中均观察到胱天蛋白酶切割测定结果中检测到的胱天蛋白酶3、9和8的切割活性显著增加。MG132在体外对U87 MG和T98 G具有较强的细胞毒活性，可以通过TGP有效地掺入和递送。

MG132, a proteasome-inhibitor, has been shown to induce apoptosis of experimental malignant cells in vitro. However, its systemic toxicity prevents further use in clinical settings. To circumvent this toxicity, MG132 can be delivered directly to the tumor. We tested the efficacy of MG132 incorporated into thermoreversible gelation polymer (TGP) for treating experimental glioma cell lines were measured with MTT-assays. As a caspase activity assay, the activities for caspases 3, 8 and 9 were measured in a CytoFluor Multiwell Plate Reader. A significant increase in cleavage activities of caspases 3, 9, and 8 detected in caspase cleavage assay results was observed in both cell lines. MG132 exhibits potent cytotoxic-activity against U87MG and T98G in vitro, it can be efficiently incorporated and delivered using TGP.