Optimization of a novel chelerythrine-loaded magnetic Fe3O4/chitosan alpha-ketoglutaric acid system and evaluation of its anti-tumour activities

Objectives A novel magnetic targeting anti‐tumour drug delivery system (Fe3O4/KCTS‐CHE) was designed using magnetic Fe3O4/chitosan alpha‐ketoglutaric acid (Fe3O4/KCTS) as carrier and chelerythrine (CHE) as an anti‐tumour drug model. Moreover, the anti‐tumour activities and mechanisms of Fe3O4/KCTS‐C...

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Bibliographic Details
Published in:Journal of pharmacy and pharmacology 2016-08, Vol.68 (8), p.1030-1040
Main Authors: Yang, Fei, Xiao, Wen, Ma, Xiaohua, Huang, Ruixue, Yu, Ran, Li, Guiyin, Huang, Xiao, Chen, Cuimei, Ding, Ping
Format: Article
Language:English
Subjects:
anti-tumour drug
chelerythrine
chitosan alpha-ketoglutaric acid
magnetic nanoparticle
response surface methodology
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Summary:Objectives A novel magnetic targeting anti‐tumour drug delivery system (Fe3O4/KCTS‐CHE) was designed using magnetic Fe3O4/chitosan alpha‐ketoglutaric acid (Fe3O4/KCTS) as carrier and chelerythrine (CHE) as an anti‐tumour drug model. Moreover, the anti‐tumour activities and mechanisms of Fe3O4/KCTS‐CHE were investigated. Methods The preparation conditions of Fe3O4/KCTS‐CHE microspheres were optimized by response surface methodology (RSM). The CHE drug release kinetics was evaluated by fitting the experimental data to standard release equations. The inhibitive activities of Fe3O4/KCTS‐CHE microspheres against the HepG2 cells were estimated using MTT assay in vitro, and the mechanisms were studied using Hoechst 33258 staining. Key findings The optimum preparation conditions were 11.68 : 1 for Fe3O4/KCTS:CHE ratio, 4 : 1 for oil/water ratio and 50.03 min for the ultrasonic time. The drug loading content and entrapment efficiency under the optimal conditions were 23.3% and 50.9%. The best fit was Higuchi model for the microspheres. The inhibitive rate on HepG2 cells of Fe3O4/KCTS‐CHE nanoparticles varied from 30.19 ± 2.64% to 70.46 ± 6.42% at different concentrations from 50 to 400 mg/l in 72 h. Conclusion Fe3O4/KCTS‐CHE exhibited effective anti‐tumour activities against the HepG2 cells and induced cell apoptosis in HepG2 cells. Fe3O4/KCTS‐CHE possess a high drug loading efficiency and entrapment efficiency, which are a new matrix for controlling release of drugs and a promising candidate for targeted drug delivery.
ISSN:0022-3573
2042-7158
DOI:10.1111/jphp.12564