Research on self-assembly micelles of N-(4-methylimidazole)-hydroxyethyl-chitosan loading quercetin
10.11665/j.issn.1000-5048.20170107
- VernacularTitle:N-（4-咪唑甲基）-羟乙基壳聚糖自组装胶束载槲皮素的研究
- Author:
Xiaojing XIA
;
Ying HU
;
Jiang JIN
;
Beihua XU
;
Jianping ZHOU
- Keywords:
quercetin;
N-( 4-methylimidazole)-hydroxyethyl-chitosan;
self-assembly micelles;
pharmacokinetics
- From:
Journal of China Pharmaceutical University
2017;48(1):46-52
- CountryChina
- Language:Chinese
-
Abstract:
To improve the solubility of quercetin ( QT) , one of flavonoids that can inhibit the proliferation of vari-ous types of cancer cells, the novel amphiphilic polymer N-( 4-methylimidazole)-hydroxyethyl-chitosan ( MHC) , synthetized by chemical derivatization from chitosan, was used as the self-assembly micelles of QT. The formed polymer was characterized by 1 H NMR, elemental analysis and pyrene fluorescence spectrometry. The formulation of MHC micelles loading quercetin was optimized through single factor experiment. Then the optimized formulation was obtained as follows:the concentration of MHC was 0. 67% and the ratio of drug and carrier was 1 ∶10. The micelles particle size was ( 99. 21 ± 1. 71) nm, Zeta potential was +( 20. 01 ± 0. 72) mV and drug loading was ( 5. 42 ± 0. 32 )%. The in vitro release curve was investigated and was found to conform to Higuchi equation of Q=0. 1101 t1/2 -0. 064. The results of in vivo experiment showed that the mean rentention time and bioavail-ability of the MHC-QT micelles were 21. 42 h and 57. 49 μg h/mL, respectively, compared to 0. 30 h and 2. 50 μg h/mL of the free QT solution. These indicated that the MHC micelles could significantly improve the solubility of QT, the drug sustained-release effect and bioavailability, which would used as carrier for the anti-tumor drugs.
