Department of Polymer Science and Engineering, College of Chemistry and Chemical Engineering, and Jiangsu Provincial Laboratory for Nanotechnology, Nanjing University, Nanjing 210093, People's Republic of China.
Biomacromolecules. 2015 Jul 13;16(7):2059-71. doi: 10.1021/acs.biomac.5b00479. Epub 2015 Jun 10.
Cisplatin-incorporating pseudoblock copolymer nanoparticles with high drug loading efficiency (ca. 50%) were prepared built on host-guest inclusion complexation between β-cyclodextrin end-capped poly(N-vinylpyrrolidone) block and admantyl end-capped poly(aspartic acid) block, followed by the coordination between cisplatin and carboxyl groups in poly(aspartic acid). The host-guest interaction between the two polymer blocks was examined by two-dimensional nuclear overhauser effect spectroscopy. The size and morphology of nanoparticles formed were characterized by dynamic light scattering, zeta potential, transmission electron microscopy, and atomic force microscopy. The size control of nanoparticles was carried out by varying the ratio of poly(N-vinylpyrrolidone) to poly(aspartic acid). The nanoparticles were stable in the aqueous medium with different pH values but disintegrated in the medium containing Cl(-) ions. The in vitro and in vivo antitumor effects of cisplatin-loaded nanoparticles were evaluated. The biodistribution of the nanoparticles in vivo was studied by noninvasive near-infrared fluorescence imaging and ion-coupled plasma mass spectrometry. It was found that cisplatin-loaded nanoparticles could effectively accumulate in the tumor site and exhibited significant superior in vivo antitumor activity to the commercially available free cisplatin by combining the tumor volume, body weight, and survival rate measurements.
基于β-环糊精封端的聚（N-乙烯基吡咯烷酮）嵌段与金刚烷基封端的聚（天冬氨酸）嵌段之间的主客体包合络合作用，以及顺铂与聚（天冬氨酸）中羧基之间的配位作用，制备了载药效率高（约 50%）的顺铂结合假嵌段共聚物纳米粒子。通过二维核磁共振波谱研究了两种聚合物嵌段之间的主客体相互作用。通过动态光散射、zeta 电位、透射电子显微镜和原子力显微镜对形成的纳米粒子的尺寸和形态进行了表征。通过改变聚（N-乙烯基吡咯烷酮）与聚（天冬氨酸）的比例来控制纳米粒子的尺寸。纳米粒子在不同 pH 值的水介质中稳定，但在含有 Cl-离子的介质中会分解。评价了载顺铂纳米粒子的体内外抗肿瘤作用。通过无创近红外荧光成像和离子偶联等离子体质谱研究了纳米粒子在体内的分布。结果发现，载顺铂纳米粒子能够有效地聚集在肿瘤部位，通过结合肿瘤体积、体重和存活率的测量，与市售的游离顺铂相比，显示出显著优越的体内抗肿瘤活性。
