DSAPM Lab and PCFM Lab, Department of Polymer and Materials Science, School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China.
DSAPM Lab and PCFM Lab, Department of Polymer and Materials Science, School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China; Guangdong Provincial Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Science, Sun Yat-sen University, Guangzhou 510006, China.
Mater Sci Eng C Mater Biol Appl. 2014 Aug 1;41:36-41. doi: 10.1016/j.msec.2014.04.015. Epub 2014 Apr 13.
For the development of biomimetic carriers for stimuli-sensitive delivery of anticancer drugs, a novel amphiphilic glycopolypeptide conjugate containing the disulfide bond was prepared for the first time by the ring-opening polymerization of benzyl glutamate N-carboxy anhydride in the presence of (propargyl carbamate)ethyl dithio ethylamine and then click conjugation with α-azido dextran. Its structure was characterized by Fourier-transform infrared spectroscopy and nuclear magnetic resonance analyses. Owing to its amphiphilic nature, such a conjugate could self assemble into nanosize micelles in aqueous medium, as confirmed by fluorometry, transmission electron microscopy and dynamic light scattering. For the resultant micelles, it was found to encapsulate poorly water-soluble anticancer drug (methotrexate, MTX) with the loading efficiency of 45.2%. By the in vitro drug release tests, the release rate of encapsulated MTX was observed to be accelerated significantly in the presence of 10 mM 1,4-dithio-DL-threitol (DTT), analogous to the intracellular redox potential.
为了开发用于刺激响应性递抗癌药物的仿生载体，首次通过在（炔丙基氨基甲酸酯）乙基二硫代乙基胺存在下开环聚合苯谷氨酸 N-羧酸酐，然后与α-叠氮葡聚糖点击偶联，制备了一种含有二硫键的新型两亲性糖多肽偶联物。其结构通过傅里叶变换红外光谱和核磁共振分析进行了表征。由于其两亲性，这种偶联物可以在水介质中自组装成纳米尺寸的胶束，这通过荧光法、透射电子显微镜和动态光散射得到了证实。对于所得的胶束，发现其可以包封疏水性差的抗癌药物（甲氨蝶呤，MTX），载药量为 45.2%。通过体外药物释放试验，发现含有 10 mM 1,4-二硫-DL-苏糖醇（DTT）时，包封的 MTX 的释放速率明显加快，类似于细胞内氧化还原电势。
