發明
美國
12/799,887
US 8,992,990 B2
用於抑制/治療腫瘤之磁性奈米複合物及其製備方法Magnetic nanocomposite for inhibiting/treating cancer and method for fabricating the same
長庚大學
2015/03/31
本發明提供一種可抗惡性神經膠質瘤之磁性奈米藥物(簡稱為SPAnH/MNPs/BCNU),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,殼外以共價鍵接上抗腦腫瘤藥物 BCNU (1,3- bis(2-chloroethyl)-1-nitrosourea,卡莫司汀) 而成。本發明提出的磁性奈米藥物,不僅可明顯改善BCNU藥物之熱穩定性,在37 ℃ 下其藥物半衰期可從 12 hr 延長至 30 hr;在4 ℃儲存經過30天,純BCNU其活性只剩 22 %,而本發明之磁性奈米藥物的活性仍高達 54 %,儲存安定性明顯優於BCNU。由於此新藥可以均勻的分散於水中,大大改善此類藥物不溶於水的缺點;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,在有效藥量100 M條件下,無論對老鼠的惡性神經膠質瘤細胞或人類的惡性神經膠質瘤細胞的毒殺率,在磁場 (800 Gauss) 作用下,本發明之磁性奈米藥物都較純的BCNU好,分別增加約 35% 和 22%,具經濟競爭性。 關鍵字:磁性奈米粒子、神經膠質瘤、卡莫司汀。 This investion provides a novel magnetic nano-drug (SPAnH/MNPs/BCNU) which is used for the malignant glioma therapy. This nanodrug comprise a magnetic nanoparticle of Fe3O4/ carboxy-functionalized polyaniline (PAn-RCOOH) core/shell and an anti-brain tumor drug of 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) which is covalent bonded with the shell of PAn-RCOOH. This nano-drug is water solvable and can be dispersed uniformly in water. In comparison with crude BCNU, the in vitro cytotoxicity tests of this magnetic nanodrug with the concentrations of 100 uM and the applied magnetic field of 800 G show that the killing rates of malignant glioma cell of adult male rat and human are increased 35% and 22%, respectively. This result implicates that the magnetic nanodrug has a great economic advantage. 關鍵字:magnetic nano-drug、superparamagnetic、BCNU、glioma cell
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