應用於治療血栓性疾病的磁性奈米藥物

專利類型

發明

專利國別 (專利申請國家)

中華民國

專利申請案號

101110199

專利證號

I 510256

專利獲證名稱

應用於治療血栓性疾病的磁性奈米藥物

專利所屬機關 (申請機關)

長庚大學

獲證日期

2015/12/01

技術說明

本發明提供一種可治療局部中風或腦中風之磁性奈米藥物 (簡稱為rt-PA/SPAnH/MNPs)，此藥物以磁性奈米四氧化三鐵為核，以羧基化聚苯胺高分子為殼，殼外以共價鍵接上可溶解血栓之胞漿素原活化劑(recombinant tissue-type plasminogen activator, rt-PA) 而成。本發明提出的rt-PA/SPAnH/MNPs具有很好的藥物穩定性，在25 ℃ 下儲存 35 天後，rt-PA/SPAnH/MNPs 依然仍保有約 73% 的藥物活性；而純 rt-PA在25 ℃儲存 21 天後，已完全失去其原本之藥物活性，結果顯示本發明提供之rt-PA/SPAnH/MNPs其儲存安定性明顯優於純 rt-PA。由於此新藥可以均勻的分散於水中，再加上此磁性奈米藥物具有超順磁性，可藉由外加磁場將藥物導引集中於特定部位，增加局部治療濃度。由體外毒性測試可知，SPAnH/MNPs 對血管內皮細胞並不具生物毒性；由體外人血血栓溶解測試可知，純 rt-PA約需 39 分鐘才會溶解5mm´2mm´2mm的血塊，而 rt-PA/SPAnH/MNPs 在磁場的導引下只需約 9 分鐘即能使相同大小的血塊溶解，是ㄧ無毒、可被磁導、可集中治療且兼俱發展潛力之血栓溶解新藥，具經濟競爭性。 This invention provides a novel magnetic nanodrug (rt-PA/SPAnH/MNPs) which is used for the malignant glioma therapy. This nanodrug comprises magnetic nanoparticles of Fe3O4 coating with a shell of carboxy-functionalized polyaniline (SPAnH) and an anti-thrombosis drug of recombinant tissue-type plasminogen activator (rt-PA), which is covalently bonded with the shell of SPAnH. The thermal stability of rt-PA/SPAnH/MNPs is much better than that of crude rt-PA. It has the superparamagnetic property and can be concentrated and guided by an externally applied magnetic field to specific target area to enhance the local drug concentration effect. It is also evidenced that SPAnH/MNPs has no toxicity to the endothelial cells. This result implicates that the rt-PA/SPAnH/MNPs is a non-toxicity and magnetic nanodrug with the potential to be used for targeted thrombosis.

備註

本部(收文號1090058260)同意該校109年9月15日長庚大字第1090090253號函申請終止維護專利(長庚大學)

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