荧光标记pH敏感胶束的合成及其药物控释
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- 英文论文题名：Preparation and characterization of fluoresence and pH-Sensitive Polymeric Micelles for drug delivery
- 论文作者：郝伟举 ; 尚亚卓 ; 刘洪来 ; 徐首红
- 英文论文作者：Hao Weiju ; Shang Yazhuo ; Liu Honglai ; Xu Shouhong ; Key Laboratory for Advanced Materials and Department of Chemistry ; East China University of Science and Technology
- 年：2016
- 作者机构：华东理工大学结构可控先进功能材料及其国家重点实验室;
- 论文关键词：pH敏感聚合物 ; 自组装胶束 ; 靶向运输 ; 可控释药
- 英文论文关键词：pH-sensitive copolymer ; self-assembly micelle ; targeting delivery ; controlled release
- 会议召开时间：2016-07-01
- 会议录名称：中国化学会第30届学术年会摘要集-第三十一分会：胶体与界面化学
- 语种：中文
- 分类号：O631;TQ460.1
- 学会代码：ZGHY
- 会议名称：中国化学会第30届学术年会-第三十一分会 ; 胶体与界面化学
- 会议地点：中国辽宁大连
- 主办单位：中国化学会
- 学会名称：中国化学会
- 页数：1
- 文件大小：156k
- 原文格式：D
- 会议级别：全国
摘要
以溴代异丁酰溴与聚乙二醇单甲醚(mPEG)及具有绿色荧光的异硫氰酸荧光素(FITC)的聚乙二醇酯化,合成含溴的大分子引发剂PEG_(45)-Br及FITC-PEG_(45)-Br。以甲基丙烯酸二异丙胺基乙酯(DPA)为单体,利用原子转移自由基聚合方法(ATRP)合成不同亲疏水段比例的pH敏感的嵌段共聚物mPEG-b-PDPA_n(n=100-200)及具有荧光及pH敏感的嵌段聚合物FITC-PEG_(45)-PDPA_(100)。以此为载体,采用溶剂挥发的方法制备了胶束,此胶束呈现均一的球形分布,平均粒径200nm,电位为负。以阿霉素(DOX)为模拟药物,其胶束载药量约11%(w/w),包封率为70%左右,外环境pH对载药胶束的粒径和体外释放行为有显著影响。在弱酸环境下,载药胶束迅速解离,在1-2h内药物可释放80%。体外毒性试验表明,空白胶束与细胞有良好的生物相容性。同时,与细胞共同孵育5h的荧光聚合物胶束,体现了较好的转染效果。
In this paper,novel pH-sensitive micelles with and without fluorescence terminal group(FITC)were developed as drug carrier.The pH-sensitive amphiphilic diblock copolymer could act as smart pH-trigger because the micelles were stable at pH7.4 and became looser at pH6.0.DOX was used as the model drug,which had high load efficiency.The release behavior of DOX was a burst one as soon as the micelles entered in a weak acid environment.Cell toxicity assays for blank micelles were carried out using the human cancer cells(Huh7),which showed good cyto-compatibility.Besides,the micelles composed of the fluorescence copolymers were found to have better transfection efficiency.As a result,the micelles with fluorescent copolymers may open up new perspectives to real-time track of drug delivery and/or distribution during chemotherapy.
In this paper,novel pH-sensitive micelles with and without fluorescence terminal group(FITC)were developed as drug carrier.The pH-sensitive amphiphilic diblock copolymer could act as smart pH-trigger because the micelles were stable at pH7.4 and became looser at pH6.0.DOX was used as the model drug,which had high load efficiency.The release behavior of DOX was a burst one as soon as the micelles entered in a weak acid environment.Cell toxicity assays for blank micelles were carried out using the human cancer cells(Huh7),which showed good cyto-compatibility.Besides,the micelles composed of the fluorescence copolymers were found to have better transfection efficiency.As a result,the micelles with fluorescent copolymers may open up new perspectives to real-time track of drug delivery and/or distribution during chemotherapy.
引文
[1]Evans,C.M.;Henderson,K.J.;Macromolecules 2013,46(10),4131-4140.
[2]Qian,J.;Sullivan,B.P.;Berkland,C.Biomacromolecules 2015,16(8),2340-6.
[2]Qian,J.;Sullivan,B.P.;Berkland,C.Biomacromolecules 2015,16(8),2340-6.