Xu Xiuling, Chen Xuesi, Xu Xiaoyi, Lu Tiancheng, Wang Xin, Yang Lixin, Jing Xiabin
State key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China.
J Control Release. 2006 Sep 12;114(3):307-16. doi: 10.1016/j.jconrel.2006.05.031. Epub 2006 Jun 23.
The purpose of the present study was to develop implantable BCNU-loaded poly(ethylene glycol)-poly(L-lactic acid) (PEG-PLLA) diblock copolymer fibers for the controlled release of 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU). BCNU was well incorporated and dispersed uniformly in biodegradable PEG-PLLA fibers by using electrospinning method. Environmental Scanning Electron Microscope (ESEM) images indicated that the BCNU-loaded PEG-PLLA fibers looked uniform and their surfaces were reasonably smooth. Their average diameters were below 1500 nm. The release rate of BCNU from the fiber mats increased with the increase of BCNU loading amount. In vitro cytotoxicity assay showed that the PEG-PLLA fibers themselves did not affect the growth of rat Glioma C6 cells. Antitumor activity of the BCNU-loaded fibers against the cells was kept over the whole experiment process, while that of pristine BCNU disappeared within 48 h. These results strongly suggest that the BCNU/PEG-PLLA fibers have an effect of controlled release of BCNU and are suitable for postoperative chemotherapy of cancers.
本研究的目的是开发用于1,3-双（2-氯乙基）-1-亚硝基脲（BCNU）控释的可植入载有BCNU的聚（乙二醇）-聚（L-乳酸）（PEG-PLLA）双嵌段共聚物纤维。通过静电纺丝法，BCNU被很好地掺入并均匀分散在可生物降解的PEG-PLLA纤维中。环境扫描电子显微镜（ESEM）图像表明，载有BCNU的PEG-PLLA纤维看起来均匀，其表面相当光滑。它们的平均直径低于1500 nm。BCNU从纤维垫中的释放速率随着BCNU负载量的增加而增加。体外细胞毒性试验表明，PEG-PLLA纤维本身不影响大鼠胶质瘤C6细胞的生长。载有BCNU的纤维对细胞的抗肿瘤活性在整个实验过程中保持，而原始BCNU的抗肿瘤活性在48小时内消失。这些结果强烈表明，BCNU/PEG-PLLA纤维具有BCNU控释作用，适用于癌症术后化疗。
