Antifouling zwitterionic dextran micelles for efficient loading DOX

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.