Wang Cheng, Liang Jian, Deng Xin, Long Chaofeng, Xie Chengshi, Chen Xiaoxin, Zhang Lan, Guo Qingfa, Wang Yingjing, Wang Yujun, Luo Feng, Qian Zhiyong
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
J Nanosci Nanotechnol. 2013 Jan;13(1):68-76. doi: 10.1166/jnn.2013.6695.
In this paper, we successfully synthesized amino-terminated poly(ethylene glycol)-block-poly (epsilon-caprolactone) (NH2-PEG-PCL) block copolymer from polyethylene glycol 2000, epsilon-caprolactone (epsilon-CL) and hydrazine hydrate. The obtained copolymer was characterized by nuclear magnetic resonance (1H-NMR), the molecular weight and distribution of NH2-PEG-PCL were characterized by Gel permeation chromatography (GPC). The NH2-PEG-PCL copolymer could self-assemble into micelles in water. Paclitaxel (PTX) loaded NH2-PEG-PCL (PNPP) micelles were prepared by solid dispersion technique without organic solvent. The micelles were characterized by XRD, TEM and Malvern laser particle size. The results of this work indicated that PNPP micelles were uniform and spherical shapes in solution. The average size and zeta potential of PNPP (DL = 8%) in water was about 97.1 +/- 1.2 nm, +13.9 +/- 0.6 mV, respectively. The in vitrodrug release profile of PNPP micelles showed a clear slow-release effect. The results suggested that NH2-PEG-PCL copolymer might be an excellent carrier for hydrophobic drugs such as PTX. In particular, the NH2-PEG-PCL polymer has potential value for modifying with ligands to work as active targeting drug delivery carriers, which has great significance for cancer therapeutics.
在本文中，我们成功地由聚乙二醇2000、ε-己内酯（ε-CL）和水合肼合成了氨基封端的聚（乙二醇）-嵌段-聚（ε-己内酯）（NH2-PEG-PCL）嵌段共聚物。通过核磁共振（1H-NMR）对所得共聚物进行了表征，通过凝胶渗透色谱法（GPC）对NH2-PEG-PCL的分子量及分布进行了表征。NH2-PEG-PCL共聚物在水中可自组装成胶束。采用无有机溶剂的固体分散技术制备了载紫杉醇（PTX）的NH2-PEG-PCL（PNPP）胶束。通过X射线衍射（XRD）、透射电子显微镜（TEM）和马尔文激光粒度仪对胶束进行了表征。这项工作的结果表明，PNPP胶束在溶液中呈均匀的球形。PNPP（载药量 = 8%）在水中的平均粒径和zeta电位分别约为97.1±1.2 nm、+13.9±0.6 mV。PNPP胶束的体外药物释放曲线显示出明显的缓释效果。结果表明，NH2-PEG-PCL共聚物可能是一种用于疏水性药物如PTX的优良载体。特别是，NH2-PEG-PCL聚合物具有用配体进行修饰以作为主动靶向药物递送载体的潜在价值，这对癌症治疗具有重要意义。
