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聚天冬氨酸-甲硝唑纳米前药制备、表征及抗虫活性的初步研究
引用本文:戚晓红,陈汐敏,冯振卿,管晓虹,吴 军,陈 强,阚延静,童 华.聚天冬氨酸-甲硝唑纳米前药制备、表征及抗虫活性的初步研究[J].生物化学与生物物理进展,2009,36(8):1056-1063.
作者姓名:戚晓红  陈汐敏  冯振卿  管晓虹  吴 军  陈 强  阚延静  童 华
作者单位:1. 南京医科大学卫生部抗体技术重点实验室,南京,210029;南京医科大学病理与病理生理学系,南京,210029
2. 南京医科大学卫生部抗体技术重点实验室,南京,210029
3. 南京大学表面和界面化学工程技术研究中心,南京,210093
4. 南京市妇幼保健院,南京,210004
基金项目:南京市卫生局科技发展专项基金资助 (D:ZKX 0103)
摘    要:实验以聚天冬氨酸(PASP)为载体,以甲硝唑为模型药物,用较温和简便的方法制备了新型聚天冬氨酸-甲硝唑(PASP-MTI)纳米前药.采用红外光谱及核磁氢谱分析、透射电镜观察、激光粒度、透析和紫外分光光度测定、MTT比色、荧光显微镜和流式细胞术等方法,观察到甲硝唑以酯键方式键合于聚天冬氨酸高分子链上.PASP-MTI纳米前药呈球型,平均粒径404.8 nm,载药量30%,体外释药明显延缓;MTT结果显示,PASP-MTI显著提高甲硝唑对滴虫的抑杀作用,经纳米甲硝唑作用后,部分滴虫胞核出现染色质浓集、核固缩、核碎裂等一系列凋亡改变.流式细胞术检测可见凋亡峰,凋亡率由对照组的11.5%上升到纳米前药组的35.69%.上述实验结果表明:PASP是一种非常有潜力的前药载体,制得的新型PASP-MTI纳米前药具有载药量高、缓释和杀虫作用强等特点,可能的杀虫机制除与高聚物纳米前药促吞噬作用有关外,还与诱导滴虫凋亡有关.

关 键 词:聚天冬氨酸,甲硝唑,纳米粒,前药,缓释,阴道毛滴虫,凋亡
收稿时间:2008/12/18 0:00:00
修稿时间:2009/3/15 0:00:00

Preparation, characterization and preliminary trichomonacidal effect of poly aspartic acid-metronidazole nanoprodrug
QI Xiao-Hong,CHEN Xi-Min,FENG Zhen-Qing,GUAN Xiao-Hong,WU Jun,CHEN Qiang,KAN Yan-Jing and TONG Hua.Preparation, characterization and preliminary trichomonacidal effect of poly aspartic acid-metronidazole nanoprodrug[J].Progress In Biochemistry and Biophysics,2009,36(8):1056-1063.
Authors:QI Xiao-Hong  CHEN Xi-Min  FENG Zhen-Qing  GUAN Xiao-Hong  WU Jun  CHEN Qiang  KAN Yan-Jing and TONG Hua
Institution:The Key Laboratory Antibody Technology of State Ministry of Health, Nanjing Medical University, Nanjing 210029, China; Department of Pathology and Pathophysiology, Nanjing Medical University, Nanjing 210029, China;The Key Laboratory Antibody Technology of State Ministry of Health, Nanjing Medical University, Nanjing 210029, China;The Key Laboratory Antibody Technology of State Ministry of Health, Nanjing Medical University, Nanjing 210029, China; Department of Pathology and Pathophysiology, Nanjing Medical University, Nanjing 210029, China;The Key Laboratory Antibody Technology of State Ministry of Health, Nanjing Medical University, Nanjing 210029, China;Center of Research on Surface and Interface Chemical Engineering and Technology, Nanjing University, Nanjing 210093, China;Center of Research on Surface and Interface Chemical Engineering and Technology, Nanjing University, Nanjing 210093, China;Nanjing Maternal and Child Health Hospital, Nanjing 210004, China;Nanjing Maternal and Child Health Hospital, Nanjing 210004, China
Abstract:
Keywords:poly aspartic acid  metronidazole  nanoparticle  prodrug  prolonged release  T  vaginalis  apoptosis
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