College of Chemistry and Chemical Engineering, Nanjing University, Nanjing 210093, PR China.
Carbohydr Polym. 2013 Apr 2;93(2):430-7. doi: 10.1016/j.carbpol.2012.12.051. Epub 2013 Jan 7.
Amphiphilic dextran-b-poly(ɛ-caprolactone) diblock copolymers were synthesized with the purpose of preparing nanocarriers for doxorubicin (DOX), an anticancer drug. The Dex-b-PCL diblock copolymers were synthesized by end-to-end coupling of amino-terminated dextran and aldehyde-terminated poly(ɛ-caprolactone) and characterized by (1)H NMR spectra and gel permeation chromatography. The DOX-loaded Dex-b-PCL nanoparticles were prepared by a modified nanoprecipitation method and characterized by transmission electron microscopy and dynamic light scattering. In vitro release of DOX from DOX-Dex-b-PCL nanoparticles showed a sustained release manner with certain amount of burst release in the first 9h. In vitro cytotoxicity test of DOX-Dex-b-PCL nanoparticles against SH-SY5Y cells showed that DOX is still pharmacologically active after drug loading. The fluorescence imaging results showed that DOX-Dex-b-PCL nanoparticles could be easily uptaken by SH-SY5Y cells. These results indicate that DOX-Dex-b-PCL nanoparticles may be a promising nanocarrier for DOX.
两亲性葡聚糖-b-聚（己内酯）嵌段共聚物的合成目的是制备阿霉素（DOX）的纳米载体，阿霉素是一种抗癌药物。通过氨基封端的葡聚糖和醛基封端的聚（己内酯）的端到端偶联合成了 Dex-b-PCL 嵌段共聚物，并通过（1）H NMR 谱和凝胶渗透色谱进行了表征。通过改良的沉淀法制备了载 DOX 的 Dex-b-PCL 纳米颗粒，并通过透射电子显微镜和动态光散射进行了表征。DOX-Dex-b-PCL 纳米颗粒中 DOX 的体外释放表现出持续释放方式，在前 9 小时内具有一定的突释。载药前后 DOX-Dex-b-PCL 纳米颗粒对 SH-SY5Y 细胞的体外细胞毒性试验表明，载药后 DOX 仍具有药理活性。荧光成像结果表明，DOX-Dex-b-PCL 纳米颗粒可以很容易地被 SH-SY5Y 细胞摄取。这些结果表明，DOX-Dex-b-PCL 纳米颗粒可能是 DOX 的一种有前途的纳米载体。
