中国药房2013，Vol.24Issue(21)：1975-1979,5.DOI:10.6039/j.issn.1001-0408.2013.21.20
N-三甲基壳聚糖包覆的降钙素脂质体的制备及其体内外黏附性质研究
Study on Preparation of N-trimethyl Chitosan Coated Calcitonin Liposome and Adhesion Properties of It in vivo and in vitro
摘要
Abstract
OBJECTIVE:To prepare N-trimethyl chitosan (TMC) coated calcitonin liposome,and to investigate the physicochemical properties and adhesion properties of it in vitro and in vivo.METHODS:2-step reaction was adopted for the synthesis of TMC; calcitonin liposome was prepared by thin-film hydration method,and the liposomes were coated with TMC; the particle size,polydispersity index,Zeta potential,encapsulation efficiency and form were all investigated; the pig gastric mucosal protein particles combination method was used to evaluate in vitro adhesion properties of TMC liposome with pH of 4.5 and 6.8; 12 wistar rats were randomly divided into 4 groups,with 3 rats in each group; the adhesion behavior of TMC liposomes to duodenum,jejunum,ileum were investigated by C6 labeling.RESULTS:The degree of quatemization for synthesized TMC was 78.10％; the prepared uncoated calcitonin liposome showed strong negative charge,and charge reversal was achieved after coated with TMC; prepared liposomes was round in appearance and coated obviously with particle size of 262.9 nm,polydispersity index of 0.172,Zeta potential of (35.8 ± 1.2) mV and entrapment efficiency of (89.14 ± 3.1)％; TMC liposomes adhered to mucin nanoparticles under pH 4.5 and pH 6.8 conditions,and reduced the Zeta potential.In rats,at 2 h,most of TMC coated liposome adhered to upper part of small intestinal,especially the duodenum,while less of it adhered to ileum; at 4 h,TMC liposome still adhered to each intestinal segment,but the symptom relieved significantly compared to 2 h,and more adhesion was found in substrate side of the ileum.CONCLUSIONS:TMC coated liposomes show good biological adhesion performance,and can be used as carrier of oral delivery of peptide drugs to carry out further study.关键词
N-三甲基壳聚糖/降钙素/脂质体/合成/制备/黏膜黏附Key words
N-trimethyl chitosan/ Calcitonin/ Liposome/ Synthesis/ Preparation/ Mucosal adhesion分类
医药卫生引用本文复制引用
黄爱文,竹内洋文,宋洪涛..N-三甲基壳聚糖包覆的降钙素脂质体的制备及其体内外黏附性质研究[J].中国药房,2013,24(21):1975-1979,5.基金项目
福建省自然科学基金资助项目(No.2012J05159) （No.2012J05159）
