【作者】 郝伟举； 尚亚卓； 刘洪来； 徐首红；

【Author】 Hao Weiju;Shang Yazhuo;Liu Honglai;Xu Shouhong;Key Laboratory for Advanced Materials and Department of Chemistry, East China University of Science and Technology;

【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；

【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PEG₄₅-Br及FITC-PEG₄₅-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-PEG₄₅-PDPA₁₀₀。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。更多还原

【Abstract】 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.更多还原