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XIA Xiaojing, HU Ying, JIN Jiang, XU Beihua, ZHOU Jianping. Research on self-assembly micelles of N-(4-methylimidazole)-hydroxyethyl-chitosan loading quercetin[J]. Journal of China Pharmaceutical University, 2017, 48(1): 46-52. DOI: 10.11665/j.issn.1000-5048.20170107
Citation: XIA Xiaojing, HU Ying, JIN Jiang, XU Beihua, ZHOU Jianping. Research on self-assembly micelles of N-(4-methylimidazole)-hydroxyethyl-chitosan loading quercetin[J]. Journal of China Pharmaceutical University, 2017, 48(1): 46-52. DOI: 10.11665/j.issn.1000-5048.20170107
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Research on self-assembly micelles of N-(4-methylimidazole)-hydroxyethyl-chitosan loading quercetin

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  • To improve the solubility of quercetin(QT), one of flavonoids that can inhibit the proliferation of various 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 1H 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. 1101t1/2-0. 064. The results of in vivo experiment showed that the mean rentention time and bioavailability 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.
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    • References (11)
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