Enhanced cytotoxicity of core modified chitosan based polymeric micelles for doxorubicin delivery.
In this study, the cytotoxicity of doxorubicin (DOX) loaded stearic acid grafted chitosan oligosaccharide (CSO-SA) micelles and its core modified drug delivery systems were investigated in vitro. The in vitro drug release experiments using cellular culture medium, Roswell Park Memorial Institute 1640 (RPMI-1640) medium as a dissolution medium confirmed that the DOX release from CSO-SA micelles was successfully delayed by the core modification of CSO-SA micelles with stearic acid (SA). The cell viability assay against A549 cells indicated the 50% inhibition concentration (IC(50)) of blank CSO-SA micelles and the core modified CSO-SA micelles was 369 +/- 27 microg/mL and 234 +/- 9 microg/mL, respectively. The entrapment of DOX by CSO-SA micelles could decrease the IC(50) of DOX from 3.5 to 1.9 microg/mL, and a further reduction to 0.7 microg/mL could result by the core modification of CSO-SA micelles. The fluorescence image observations of DOX and DOX concentration measurements inside A549 cells demonstrated that the DOX concentration inside cells was increased by the entrapment of CSO-SA micelles, and further enhanced by the core modification of CSO-SA micelles. The results indicated that the CSO-SA micelles with modified cores could be useful as a drug delivery vehicle for cancer chemotherapy.
Ye
Yi-Qing
YQ
Women Hospital, School of Medicine, Zhejiang University, Hangzhou, PR China.
Chen
Feng-Ying
FY
Wu
Qiao-Ai
QA
Hu
Fu-Qiang
FQ
Du
Yong-Zhong
YZ
Yuan
Hong
H
Yu
He-Yong
HY
D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D048271:Chitosan / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D004337:Drug Carriers; D004339:Drug Compounding; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008175:Lung Neoplasms / Q000378:metabolism / Q000473:pathology; D008823:Micelles; D010316:Particle Size; D012995:Solubility; D013229:Stearic Acids / Q000737:chemistry
D000903:Antibiotics, Antineoplastic; D004337:Drug Carriers; D008823:Micelles; D013229:Stearic Acids; C031183:stearic acid; D004317:Doxorubicin; D048271:Chitosan