Polysaccharides derivatives are typical drug nanocarriers which are nontoxic and biodegradable. However, as is the case for all drug delivery systems, polysaccharides derivatives have to face the issue of protein fouling. In this paper, we present the design and synthesis of carboxybetaine-modified dextran-polycaprolactone (CB-Dex-PCL) copolymers as doxorubicin (DOX) nanocarriers. Results showed that DOX/CB-Dex-PCL micelles exhibited better cumulative release at the pH value of 5.2 than at the physiological pH of 7.4, which indicated potential applications in killing tumor cells while minimizing the toxicity to normal tissues. Additionally, antifouling properties of carboxybetaine functionalized dextran micelles were much better than that of unmodified dextran for fibrinogen and lysozyme as tested by ITC. Finally, cytotoxicity tests using Hela cells showed that CB-Dex-PCL and DOX-loaded micelles exhibited great biocompatibility. All the above observations indicated that CB-Dex-PCL micelles are potentially excellent drug carriers for the treatment of human cancerous tumors.

多糖衍生物是无毒且可生物降解的典型药物纳米载体。但是，就像所有药物输送系统一样，多糖衍生物必须面对蛋白质污染的问题。在本文中，我们介绍了设计和合成羧基甜菜碱改性的葡聚糖-聚己内酯（CB-Dex-PCL）共聚物作为阿霉素（DOX）纳米载体。结果表明，DOX / CB-Dex-PCL胶束在pH值为5.2时比在生理pH值为7.4时表现出更好的累积释放，这表明在杀死肿瘤细胞的同时潜在地将对正常组织的毒性降至最低的潜在应用。另外，通过ITC测试，羧基甜菜碱官能化的葡聚糖胶束的防污性能比未修饰的葡聚糖对纤维蛋白原和溶菌酶的防污性能要好得多。最后，使用Hela细胞进行的细胞毒性测试表明，CB-Dex-PCL和DOX加载的胶束具有很好的生物相容性。所有上述观察结果表明，CB-Dex-PCL胶束是治疗人类癌性肿瘤的潜在极好药物载体。