Preparation and characterization of N-succinyl-N′-octyl chitosan micelles as doxorubicin carriers for effective anti-tumor activity

• Published in: Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2007-04, Vol.55 (2), p.222-228
• Main Authors: Xiangyang, Xu, Ling, Li, Jianping, Zhou, Shiyue, Lu, Jie, Yang, Xiaojin, Yin, Jinsheng, Ren
• Format: Article
• Language: English
• Subjects: Anti-tumor activity; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Cell Line, Tumor; Cell Survival - drug effects; Chitosan; Chitosan - chemical synthesis; Chitosan - chemistry; Doxorubicin; Doxorubicin - chemistry; Doxorubicin - pharmacology; Drug Carriers - chemical synthesis; Drug Carriers - chemistry; Flow Cytometry; Humans; In vitro release; Inhibitory Concentration 50; K562 Cells; Micelles; Molecular Structure; Polymeric micelles
• ISSN: 0927-7765; 1873-4367
• DOI: 10.1016/j.colsurfb.2006.12.006

N-Succinyl-N′-octyl chitosan (SOC) was prepared and characterized by elemental analysis, FTIR, 1H NMR, WAXD and TG. An anticancer drug, doxorubicin (DOX), was incorporated into polymeric micelles forming by SOC in aqueous solutions. Critical micelle concentrations (CMC) of SOC were determined by fluorescence spectroscopy. The DOX-loaded SOC micelles were characterized by measurement of size and drug loading. The loading content of DOX increased with increasing drug-to-carrier ratio, and the more amount of the octyl chain, the higher the drug loading content. The average size, which was affected by the amount of octyl chain and drug loading content, was in the range of 100–200nm. The polymeric micelles containing doxorubicin in the core region exhibited a sustained release and more cytotoxic activity against HepG2, A549, BGC and K562 than doxorubicin alone, this can be attributed to an endocytosis mechanism rather than passive diffusion.