Research on self-assembly micelles of<i> N</i>-(4-methylimidazole)-hydroxyethyl-chitosan loading quercetin

XIA Xiaojing; HU Ying; JIN Jiang; XU Beihua; ZHOU Jianping

doi:10.11665/j.issn.1000-5048.20170107

Journal of China Pharmaceutical University > 2017 > 48(1): 46-52. > DOI: 10.11665/j.issn.1000-5048.20170107

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. 1101t^1/2-0. 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.
- quercetin,
- N-(4-methylimidazole)-hydroxyethyl-chitosan,
- self-assembly micelles,
- pharmacokinetics

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[1]	Yuan Z,Long C,Junming T,et al.Quercetin-induced apoptosis of HL-60 cells by reducing PI3K/Akt[J].Mol Biol Rep,2012,39(7):7785-7793.
[2]	Yang F,Jiang X,Song L,et al.Quercetin inhibits angiogenesis through thrombospondin-1 upregulation to antagonize human prostate cancer PC-3 cell growth in vitro and in vivo[J].Oncol Rep,2016,35(3):1602-1610.
[3]	Zhang Y,Huo MR,Zhou JP,et al.Potential of amphiphilically modified low molecular weight chitosan as a novel carrier for hydrophobic anticancer drug:synthesis,characterization,micellization and cytotoxicity evaluation[J].Carbohydr Polym,2009,77:231-238.
[4]	Liu WW,Zhang SY,Yang Y,et al.Preparation of tumor-targeting chitosan micelle with transmembrane effect[J].J China Pharm Univ(中国药科大学学报),2015,46(5):561-567.
[5]	Zheng YX,Zhang WN,He LP,et al.Trimethyl chitosan nanoparticles coated with Pluronic F-127 for oral insulin delivery system[J].J China Pharm Univ(中国药科大学学报),2016,47(4):442-447.
[6]	Varkouhi AK,Scholte M,Storm G,et al.Endosomal escape pathways for delivery of biologicals[J].J Control Release,2011,151(3):220-228.
[7]	Zhang MB,Li L,Sun YT,et al.Study on antitumor mechanism of quercetin based on molecular reverse docking method[J].Chin J Exper Tradit Med Formu(中国实验方剂学杂志),2012,18(23):145-148.
[8]	Hans M,Shimoni K,Danino D,et al.Synthesis and characterization of mPEG-PLA prodrug micelles[J].Biomacromolecules,2005,6(5):2708-2717.
[9]	Xia XJ,Xu BH,Zhang TQ,et al.Preparation,characteration and pharmacokinetics in rats of thiolated-chitosan microspheres loading quercetin[J].J China Pharm Univ(中国药科大学学报),2014,45(2):185-191.
[10]	Ghosn B,Singh A,Li M,et al.Efficient gene silencing in lungs and liver using imidazole-modified chitosan as a nanocarrier for small interfering RNA[J].Oligonucleotides,2010,20(3):163-172.
[11]	Zhong CH,Luo BH,Zhou CR,et al.Synthesis of hydroxyethyl chitosan and its compatibility with poly(D,L-lactide)[J].Chem Res App(化学研究与应用),2010,22(9):1102-1107.

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