Glucose-conjugated chitosan nanoparticles for targeted drug delivery and their specific interaction with tumor cells

• Published in: Frontiers of materials science Vol. 8; no. 4; pp. 363 - 372
• Main Authors: LI, Jing, MA, Fang-Kui, DANG, Qi-Feng, LIANG, Xing-Guo, CHEN, Xi-Guang
• Format: Journal Article
• Language: English
• Published: Heidelberg Higher Education Press 01.12.2014
• Subjects: Chemistry and Materials Science; chitosan (CS); drug delivery; glucose transporter (Glut); Materials Science; nanoparticle; Research Article; target; 共轭; 壳聚糖; 异性; 相互作用; 纳米颗粒; 肿瘤细胞; 葡萄糖转运; 靶向药物; nanoparticle; drug delivery; glucose transporter (Glut); chitosan (CS); target
• ISSN: 2095-025X; 2095-0268
• DOI: 10.1007/s11706-014-0262-8

A novel targeted drug delivery system, glucose-conjugated chitosan nanoparticles （GCNPs）, was developed for specific recognition and interaction with glucose transporters （Gluts） over-expressed by tumor cells. GC was synthesized by using succinic acid as a linker between glucosamine and chitosan （CS）, and successful synthesis was confirmed by NMR and elemental analysis. GCNPs were prepared by ionic crosslinking method, and characterized in terms of morphology, size, and zeta potential. The optimally prepared nanoparticles showed spherical shapes with an average particle size of （187.9 ± 3.8） nm and a zeta potential of （-15.43 ± 0.31） mV. The GCNPs showed negligible cytotoxicity to mouse embryo fibroblast and 4T1 cells. Doxorubicin （DOX） could be efficiently entrapped into GCNPs, with a loading capacity and encapsulation efficiency of 20.11% and 64.81%, respectively. DOX-Ioaded nanoparticles exhibited sustained-release behavior in phosphate buffered saline （pH 7.4）. In vitro cellular uptake studies showed that the GCNPs had better endocytosis ability than CSNPs, and the antitumor activity of DOX/GCNPs was 4-5 times effectiveness in 4T1 cell killing than that of DOX/CSNPs. All the results demonstrate that nanoparticles decorated with glucose have specific interactions with cancer cells via the recognition between glucose and Gluts. Therefore, Gluts-targeted GCNPs may be promising delivery agents in cancer therapies.