Conjugated Polymer Amplified Far‐Red/Near‐Infrared Fluorescence from Nanoparticles with Aggregation‐Induced Emission Characteristics for Targeted In Vivo Imaging

Fluorescence-amplified far-red/near-infrared (FR/NIR) nanoparticles (NPs) are synthesized by co-encapsulation of conjugated polymer donor (poly[9,9-bis(2-(2-(2-methoxyethoxy)ethoxy)ethyl)fluorenyldivinylene]; PFV) and a fluorogen acceptor (2-(2,6-bis((E)-4-(phenyl(4'-(1,2,2-triphenylvinyl)-[1,1'-biphenyl]-4-yl)amino)styryl)-4H-pyran-4-ylidene)malononitrile; TPE-TPA-DCM) with aggregation-induced emission (AIE) characteristics using biocompatible bovine serum albumin (BSA) as the encapsulation matrix. The good spectral overlap and close proximity between PFV and TPE-TPA-DCM in BSA NPs result in a 5.3-fold amplified TPE-TPA-DCM emission signal via fluorescence resonance energy transfer (FRET). The obtained PFV/TPE-TPA-DCM co-loaded BSA NPs are spherical in shape with a large Stokes shift of ∼223 nm and low cytotoxicity. The BSA matrix allows further functionalization with arginine-glycine-aspartic acid (RGD) peptide to yield fluorescent probes for specific recognition of integrin receptor-overexpressed cancer cells. The advantage of PFV amplified FR/NIR signal from TPE-TPA-DCM is further demonstrated in cellular and in vivo imaging using HT-29 colon cancer cells and a murine hepatoma H22 tumor-bearing mouse model, respectively. The high FR/NIR fluorescence and specific cancer targeting ability by RGD surface functionalization make the PFV/TPE-TPA-DCM co-loaded BSA-RGD NPs a unique FR/NIR fluorescent probe for cellular imaging and in vivo tumor diagnosis in a high contrast and selective manner.