Self-assembled nanoparticles of methotrexate conjugated O-carboxymethyl chitosan: Preparation, characterization and drug release behavior in vitro
Self-assembled nanoparticles of methotrexate conjugated O-carboxymethyl chitosan: Preparation, characterization and drug release behavior in vitro
复制标题
甲氨蝶呤缀合O-羧甲基壳聚糖自组装纳米颗粒的制备、表征及体外药物释放行为
DOI：
10.1016/j.carbpol.2011.06.080
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发表时间：
2011-10-15
影响因子：
11.2
通讯作者：
Zhang, Ning
中科院分区：
文献类型：
--
作者：
Wang, Yinsong;Yang, Xiaoying;Zhang, Ning
采用碳化二亚胺偶联法制备了O-羧甲基壳聚糖(OCM-壳聚糖)与甲氨蝶呤(MTX)的偶联物，并用傅立叶变换红外光谱(FTIR)、核磁共振氢谱(H-1NMR)和紫外光谱(UV)对其进行了表征。OCM-壳聚糖-MTX偶联物具有两亲性，荧光光谱测定其在水介质中的临界聚集浓度分别为4.24×10~(-2)、1.81×10~(-2)和0.84×10~(-2)mg/mL，相应的MTX含量分别为10.8%、16.2%和19.3%。透析法制备的壳聚糖-甲氨蝶呤纳米粒形状接近球形，粒径在187.2~363.5 nm之间。Zeta电位变化范围为-8.19 mV~-3.08 mV。用动态透析法研究了OCM-壳聚糖-甲氨蝶呤纳米粒的释药行为，发现甲氨蝶呤在PBS缓冲溶液(pH 4.0、7.2和9.0)中具有显著的缓释行为，表明该纳米粒具有良好的体外稳定性，有望成为一种新型的药物载体系统。(C)2011爱思唯尔有限公司。保留所有权利。
The conjugates of O-carboxymethyl chitosan (OCM-chitosan) with methotrexate (MTX) were synthesized by carbodiimide coupling and characterized by Fourier transform infrared (FTIR), proton nuclear magnetic resonance (H-1 NMR) and ultraviolet spectroscopy (UV). OCM-chitosan-MTX conjugates had amphiphilic properties and their critical aggregation concentrations in aqueous media determined by fluorescence spectroscopy were 4.24 x 10(-2), 1.81 x 10(-2) and 0.84 x 10(-2) mg/mL, respectively, responding to MTX contents of 10.8%, 16.2% and 19.3%. OCM-chitosan-MTX nanoparticles prepared by the dialysis method had nearly spherical shape and their sizes were in the range of 187.2-363.5 nm. Meanwhile, their zeta potentials ranged from -8.19 mV to -3.08 mV. Drug releases of OCM-chitosan-MTX nanoparticles were studied by the dynamic dialysis method and MTX exhibited significant sustained-release behaviors in PBS buffer solutions (pH 4.0, 7.2 and 9.0), indicating that these nanoparticles had good in vitro stability and the potential to be used as a novel drug carrier system. (C) 2011 Elsevier Ltd. All rights reserved.