本文设计合成了一种用于光动力治疗的聚合物光敏剂PDPA-AMA-BOD.研究表明,在pH中性时,聚合物自组装形成胶束,疏水端的光敏剂被包裹在疏水内腔中,处于局部高浓度聚集态,引发homo-FRET效应,单重态氧效率大幅降低;而在弱酸性条件下,由于疏水端的氨基功能团质子化,胶束形态被破坏,聚合物分子均匀分散水中,降低了光敏剂的自粹灭,PDPA-AMA-BOD具有较高的单重态氧效率.PDPA-AMA-BOD的pH响应特性赋予其在肿瘤细胞弱酸性环境中光动力靶向治疗肿瘤的能力.
We designed and synthesized anamphiphilic polymer-based PDT photosensitizer PDPA-AMA-BOD.Experimental results demonstrated that PDPA-AMA-BOD could self-assemble into micelles in neutral aqueous environment and thus enabled the BODIPY photosensitizer trapped within the hydrophobic interior,which induced a high local concentration of BODIPY.As such,the efficiency of 1O2 generation was reduced by homoFRET effect.In contrast,the protonation of amino sites attached to the hydrophobic end of PDPA-AMA-BOD resulted in the polymer well-dispersing in acidic aqueous solutions.As a consequence,concentration induced inhibition of 1O2 production was abolished.In this way,PDPA-AMA-BOD showed the acidity-controlled production of 1O2,suggesting the potential application as a selective PDT photosensitizer towards acidic tumor microenvironment.
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