Yang Chung-Lin, Chen Jyh-Ping, Wei Kuo-Chen, Chen Ju-Yu, Huang Chia-Wen, Liao Zi-Xian
Department of Neurosurgery, Chang Gung Memorial Hospital, Taoyuan 33305, Taiwan.
Department of Chemical and Materials Engineering, Chang Gung University, Taoyuan 33305, Taiwan.
Nanomaterials (Basel). 2017 Apr 13;7(4):85. doi: 10.3390/nano7040085.
In clinical tumor therapy, chemotherapeutic routes have caused severe side effects; current delivery methods are unsatisfactory. Successful design of a remotely folate (FA)-grafted chitosan (CS)-coated magnetic nanoparticle (MNP) with low toxicity, has been achieved. A chemotherapeutic drug such as doxorubicin (DOX), is loaded in the MNP-based matrix (FA-grafted CS-DOX--MNP), which is coated by an activated target tumor molecule of FA-grafted CS biopolymer with the inclusion of tripolyphosphate (TPP) as a linker. The resultant nano-complexes exhibited random aggregates (~240 nm) and zeta potential (-24.9 mV). In vivo experiments using athymic BALB/c nude mice with human glioblastoma U87 cells in a subcutaneous tumor model revealed that magnetic guidance of FA-grafted CS-DOX--MNP, injected via the tail vein, significantly decreased tumor growth. This manuscript demonstrates the feasibility of magnetizing control of FA-grafted CS-DOX--MNP to enhance the localization of drug release.
在临床肿瘤治疗中,化疗途径会引发严重的副作用;目前的给药方法并不理想。现已成功设计出一种毒性低的远程叶酸(FA)接枝壳聚糖(CS)包被的磁性纳米颗粒(MNP)。一种化疗药物如阿霉素(DOX)被负载于基于MNP的基质(FA接枝CS-DOX-MNP)中,该基质由FA接枝CS生物聚合物的活化靶肿瘤分子包被,并包含三聚磷酸钠(TPP)作为连接剂。所得的纳米复合物呈现出随机聚集体(约240纳米)和ζ电位(-24.9毫伏)。在使用人胶质母细胞瘤U87细胞皮下肿瘤模型的无胸腺BALB/c裸鼠体内实验表明,经尾静脉注射的FA接枝CS-DOX-MNP的磁导向显著降低了肿瘤生长。本论文证明了对FA接枝CS-DOX-MNP进行磁化控制以增强药物释放定位的可行性。