| 阿霉素化学键接聚合物纳米颗粒的合成及pH敏感释放 |
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| 引用本文： | 赵鑫,曹明,冯晓双,陈鹏,张玉娇,宋长江.阿霉素化学键接聚合物纳米颗粒的合成及pH敏感释放[J].医学教育探索,2015,28(3):281-287. |
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| 作者姓名： | 赵鑫 曹明 冯晓双 陈鹏 张玉娇 宋长江 |
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| 作者单位： | 安徽大学化学化工学院, 安徽省绿色高分子材料重点实验室, 合肥 230601;安徽大学化学化工学院, 安徽省绿色高分子材料重点实验室, 合肥 230601;阿普杜拉国王科技大学, 物理科学与工程部, 图瓦 23955-6900, 沙特 阿拉伯;安徽大学化学化工学院, 安徽省绿色高分子材料重点实验室, 合肥 230601;安徽大学化学化工学院, 安徽省绿色高分子材料重点实验室, 合肥 230601;安徽中意胶带有限责任公司, 安徽 淮北 235000 |
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| 基金项目： | 国家自然科学基金(21174001) |
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| 摘 要： | 合成了前驱体三-(2-氨乙基)-N,N',N"-三硫辛酸氨,该前驱体经三丁基膦(TBUP)还原后得到末端带有6个巯基的小分子单体(C-6SH)并共价偶联腙键修饰的阿霉素-(6-马来酰亚胺基己酰)腙(MAL-DOX)。通过巯基与丙烯酸酯的点击化学反应,以二甲基丙烯酸乙二醇酯(EGDMA)为交联剂,连续投料制备了具有内核交联、表面聚乙二醇(PEG)化与pH敏感药物释放特性的聚合物纳米颗粒。采用动态光散射粒径分析(DLS)和透射电镜(TEM)对纳米颗粒的尺寸和形貌进行表征,结果表明该纳米颗粒呈球形,平均尺寸为42 nm。体外药物释放表明:通过腙键连接阿霉素(DOX)的聚合物纳米颗粒具有良好的pH响应性释放能力,即在酸性条件下(pH=5.5)的释放速率比生理pH环境下要明显加快。
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| 关 键 词： | pH敏感 核交联 药物可控释放 聚合物纳米颗粒 |
| 收稿时间： | 6/1/2015 12:00:00 AM |
Synthesis and pH-Sensitive Drug Release of DOX Conjugated Polymer Nanoparticles |
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| ZHAO Xin,CAO Ming,FENG Xiao-shuang,CHEN Peng,ZHANG Yu-jiao and SONG Chang-jiang.Synthesis and pH-Sensitive Drug Release of DOX Conjugated Polymer Nanoparticles[J].Researches in Medical Education,2015,28(3):281-287. |
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| Authors: | ZHAO Xin CAO Ming FENG Xiao-shuang CHEN Peng ZHANG Yu-jiao and SONG Chang-jiang |
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| Institution: | Key Laboratory of Environment-Friendly Polymeric Materials of Anhui Province, School of Chemistry and Chemical Engineering, Anhui University, Hefei 230601, China;Key Laboratory of Environment-Friendly Polymeric Materials of Anhui Province, School of Chemistry and Chemical Engineering, Anhui University, Hefei 230601, China;Division of Physical Sciences and Engineering, King Abdullah University of Science and Technology, Thuwal 23955-6900, Saudi Arabia;Key Laboratory of Environment-Friendly Polymeric Materials of Anhui Province, School of Chemistry and Chemical Engineering, Anhui University, Hefei 230601, China;Key Laboratory of Environment-Friendly Polymeric Materials of Anhui Province, School of Chemistry and Chemical Engineering, Anhui University, Hefei 230601, China;Anhui Zhongyi Rubber Belts Co., Ltd., Huaibei 235000, Anhui, China |
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| Abstract: | A monomer containing hexa-thiols (C-6SH) was obtained through the reduction of the precursor N, N', N"-tris-lipoic amides of tris(2-aminoethyl) amine and then modified with (6-maleimidocaproyl) hydrazone of doxorubicin(DOX)(MAL-DOX). By using ethylene diacrylate (EGDMA) as crosslinker, core-crosslinked nanoparticles were synthesized with polyethylene glycol (PEG) shells and pH-sensitive drug delivery via click reactions of thiol-acrylate. The size and morphology of nanoparticles were determined by Dynamic Light Scattering (DLS) and Transmission Electron Microscope (TEM). Results showed that the nanoparticles had a spherical morphology with average diameter of 42 nm. In vitro drug release studies indicated that DOX conjugated nanoparticles with hydrazone bond showed a pH sensitive release phenomenon, that was, the releasing was significantly faster at mildly acidic condition with pH of 5.5 than that at physiological condition. |
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| Keywords: | pH-sensitive core-crosslinked controlled drug releasing polymeric nanoparticles |
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