School of Chemistry and Chemical Engineering, Tianjin Key Laboratory of Organic Solar Cells and Photochemical Conversion, Tianjin University of Technology , 300384 Tianjin, China.
Department of Chemistry, Massachusetts Institute of Technology , Cambridge, Massachusetts 02139, United States.
ACS Appl Mater Interfaces. 2015 Dec 30;7(51):28494-501. doi: 10.1021/acsami.5b09639. Epub 2015 Dec 16.
Characteristic aggregation-induced quenching of π-fluorophores imposed substantial hindrance to their utilization in nanomedicine for insight into microscopic intracellular trafficking of therapeutic payload. To address this obstacle, we attempted to introduce a novel aggregation-induced emission (AIE) fluorophore into the cationic polymer, which was further used for formulation of a gene delivery carrier. Note that the selective restriction of the intramolecular rotation of the AIE fluorophore through its covalent bond to the polymer conduced to immense AIE. Furthermore, DNA payload labeled with the appropriate fluorophore as the Förster resonance energy transfer (FRET) acceptor verified a facile strategy to trace intracellular DNA releasing activity relying on the distance limitation requested by FRET (AIE fluorophore as FRET donor). Moreover, the hydrophobic nature of the AIE fluorophore appeared to promote colloidal stability of the constructed formulation. Together with other chemistry functionalization strategies (including endosome escape), the ultimate formulation exerted dramatic gene transfection efficiency. Hence, this report manifested a first nanomedicine platform combining AIE and FRET for microscopic insight into DNA intracellular trafficking activity.
特征聚集诱导猝灭的π-荧光团对其在纳米医学中用于洞察治疗有效载荷的微观细胞内转运造成了实质性的阻碍。为了解决这个障碍，我们试图将一种新型的聚集诱导发射（AIE）荧光团引入阳离子聚合物中，进一步用于基因传递载体的配方。值得注意的是，通过将 AIE 荧光团的分子内旋转与其共价键限制在聚合物上，可以实现巨大的 AIE。此外，用适当的荧光团标记 DNA 有效负载作为Förster 共振能量转移（FRET）受体，验证了一种基于 FRET 要求的距离限制来追踪细胞内 DNA 释放活性的简便策略（AIE 荧光团作为 FRET 供体）。此外，AIE 荧光团的疏水性似乎促进了构建制剂的胶体稳定性。结合其他化学功能化策略（包括内涵体逃逸），最终制剂表现出显著的基因转染效率。因此，本报告展示了第一个将 AIE 和 FRET 结合用于微观洞察 DNA 细胞内转运活性的纳米医学平台。
