Zhang Ying, Zhuo Ren-xi
Key Laboratory of Biomedical Polymers of the Ministry of Education, Department of Chemistry, Wuhan University, Wuhan 430072, People's Republic of China.
J Biomed Mater Res A. 2006 Mar 15;76(4):674-80. doi: 10.1002/jbm.a.30395.
Novel ABA-type amphiphilic triblock copolymers composed of poly (ethylene glycol) (PEG) as hydrophilic segment and poly (2,2-dimethyltrimethylene carbonate) (PDTC) as hydrophobic segment were synthesized by ring-opening polymerization of 2,2-dimethyltrimethylene carbonate (DTC) initiated by dihydroxyl PEG. The influence of introducing PEG block on crystalline behavior of PDTC segment was investigated by DSC. Polymeric micelles in aqueous medium were characterized by fluorescence spectroscopy and dynamic light scattering. The critical micelle concentration of these copolymers was in the range of 5.1-50.5 mg/L. Particle size was 80-280 nm. Core-shell-type nanoparticles were prepared by the dialysis technique. Zeta potential was measured by laser Doppler anemometry, and all nanoparticles had negative zeta potential. Transmission electron microscopy images demonstrated that these nanoparticles were spherical in shape. Anticancer drug 5-fluorouracil (5-Fu) as a model drug was loaded in the polymeric nanoparticles. X-ray powder diffraction demonstrated that 5-Fu was encapsulated into polymeric nanoparticles as molecular dispersion. In vitro cytotoxicity of nanoparticles was evaluated by MTT assay. In vitro release behavior of 5-Fu was investigated, and sustained drug release was achieved.
以聚乙二醇(PEG)为亲水链段、聚(2,2-二甲基三亚甲基碳酸酯)(PDTC)为疏水链段合成了新型ABA型两亲性三嵌段共聚物,该共聚物由二羟基PEG引发2,2-二甲基三亚甲基碳酸酯(DTC)的开环聚合反应制备而成。通过差示扫描量热法(DSC)研究了引入PEG链段对PDTC链段结晶行为的影响。采用荧光光谱法和动态光散射法对水介质中的聚合物胶束进行了表征。这些共聚物的临界胶束浓度在5.1 - 50.5 mg/L范围内。粒径为80 - 280 nm。采用透析技术制备了核壳型纳米粒子。通过激光多普勒测速仪测量了zeta电位,所有纳米粒子的zeta电位均为负。透射电子显微镜图像表明这些纳米粒子呈球形。将抗癌药物5-氟尿嘧啶(5-Fu)作为模型药物负载于聚合物纳米粒子中。X射线粉末衍射表明5-Fu以分子分散的形式包封于聚合物纳米粒子中。通过MTT法评估了纳米粒子的体外细胞毒性。研究了5-Fu的体外释放行为,并实现了药物的持续释放。