Preparation and characterization of N-succinyl-N'-octyl chitosan micelles as doxorubicin carriers for effective anti-tumor activity.
N-Succinyl-N'-octyl chitosan (SOC) was prepared and characterized by elemental analysis, FTIR, (1)H 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 100-200 nm. 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.
Xiangyang
Xu
X
China Pharmaceutical University, Department of Pharmacy, No. 24 Tongjiaxiang, 210009 Nanjing, China.
Ling
Li
L
Jianping
Zhou
Z
Shiyue
Lu
L
Jie
Yang
Y
Xiaojin
Yin
Y
Jinsheng
Ren
R
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D048271:Chitosan / Q000138:chemical synthesis / Q000737:chemistry*; D004317:Doxorubicin / Q000737:chemistry* / Q000494:pharmacology*; D004337:Drug Carriers / Q000138:chemical synthesis / Q000737:chemistry; D005434:Flow Cytometry; D006801:Humans; D020128:Inhibitory Concentration 50; D020014:K562 Cells; D008823:Micelles; D015394:Molecular Structure
D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; D004317:Doxorubicin; D048271:Chitosan