中国药科大学学报2017，Vol.48Issue(1)：46-52,7.DOI:10.11665/j.issn.1000-5048.20170107
N-（4-咪唑甲基）-羟乙基壳聚糖自组装胶束载槲皮素的研究
Research on self-assembly micelles of N-(4-methylimidazole)-hydroxyethyl-chitosan loading quercetin
摘要
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.关键词
槲皮素/N-(4-咪唑甲基)-羟乙基壳聚糖/自组装胶束/药代动力学Key words
quercetin/N-( 4-methylimidazole)-hydroxyethyl-chitosan/self-assembly micelles/pharmacokinetics分类
医药卫生引用本文复制引用
夏晓静,胡英,金江,徐蓓华,周建平..N-（4-咪唑甲基）-羟乙基壳聚糖自组装胶束载槲皮素的研究[J].中国药科大学学报,2017,48(1):46-52,7.基金项目
宁波市自然科学基金资助项目(No．2014A610203,No．2014A610212) （No．2014A610203,No．2014A610212）
浙江省教育厅课题资助项目(No． Y201226180) （No． Y201226180）
宁波市科技创新团队资助项目(No．2015C110027)This study was supported by Ningbo Municipal Natural Science Foundation ( No．2014A610203, No．2014A610212) （No．2015C110027）
the Foundation of Zhejiang Provincial Department of Education ( No． Y201226180) （ No． Y201226180）
and the Science and Technology Innovation Team Project of Ningbo Science and Technology Bureau ( No．2015C110027) （ No．2015C110027）
