Department of Neurosurgery, First Affiliated Hospital of PLA General Hospital, 51 Fucheng Road, Haidian District, Beijing, 100048 PR China.
Anticancer Res. 2010 Jun;30(6):2217-23.
Paclitaxel has fared poorly in clinical trials against brain glioma. We hypothesized that superparamagnetic nanocarriers may enhance its bioactivities by delivering it into the brain.
The magnetic paclitaxel nanoparticles (MPNPs) were fabricated and their cytotoxicity against glioma was tested both in vitro and in glioma-bearing rats.
MPNPs exhibited superparamagnetism and produced an extended release of paclitaxel over 15 days in vitro. They were easily internalized into glioma cells and exerted remarkable toxicity, as free paclitaxel did. Furthermore, after intravenous injection of MPNPs to glioma-bearing rats and magnetic targeting with a 0.5 T magnet, drug content increased for 6- to 14-fold in implanted glioma and 4.6- to 12.1-fold in the normal brain compared to free paclitaxel. The survival of glioma-bearing rats was significantly prolonged after magnetic targeting therapy with MPNPs.
MPNPs efficiently delivered paclitaxel into brain glioma by magnetic targeting and enhance its antitumor activity. They are promising for local chemotherapy for malignant glioma.
紫杉醇在脑胶质瘤的临床试验中表现不佳。我们假设超顺磁纳米载体通过将其递送至大脑中可能增强其生物活性。
制备了磁性紫杉醇纳米颗粒（MPNPs），并在体外和荷胶质瘤大鼠中测试了它们对胶质瘤的细胞毒性。
MPNPs 表现出超顺磁性，并在体外延长了紫杉醇的释放时间，超过 15 天。它们很容易被内吞到胶质瘤细胞中，并产生了与游离紫杉醇相当的显著毒性。此外，将 MPNPs 静脉注射到荷胶质瘤大鼠中，并使用 0.5 T 磁铁进行磁靶向后，与游离紫杉醇相比，植入的胶质瘤中的药物含量增加了 6 至 14 倍，正常脑组织中的药物含量增加了 4.6 至 12.1 倍。磁靶向治疗 MPNPs 后，荷胶质瘤大鼠的存活时间显著延长。
MPNPs 通过磁靶向有效地将紫杉醇递送至脑胶质瘤中，并增强了其抗肿瘤活性。它们有望成为恶性胶质瘤的局部化疗药物。
