A multi-functional polymeric carrier for simultaneous positron emission tomography imaging and combination therapy

作者：Sun, Jingjing; Sun, Lingyi; Li, Jianchun; Xu, Jieni; Wan, Zhuoya; Ouyang, Zubin; Liang, Lei; Li, Song^*; Zeng, Dexing^*

来源：Acta Biomaterialia, 2018, 75: 312-322.

DOI：10.1016/j.actbio.2018.06.010

• PET imaging
• Farnesyl thiosalicylic acid (FTS)
• Paclitaxel
• Prodrug micelles
• Drug delivery

Multifunctional nanoplatforms offering simultaneous imaging and therapeutic functions have been recognized as a highly promising strategy for personalized nanomedicine. In this work, we synthesized a farnesylthiosalicylate (FTS, a nontoxic Ras antagonist) based triblock copolymer POEG-b-PVBA-b-PFTS (POVF) composed of a poly(oligo(ethylene glycol) methacrylate) (POEG) hydrophilic block, a poly(FTS) hydrophobic block, and a poly(4-vinylbenzyl azide) (PVBA) middle block. The POVF polymer itself was active in inhibiting the tumor growth in vitro and in vivo. Besides, it could serve as a carrier to effectively encapsulate paclitaxel (PTX) to form stable PTX/POVF mixed micelles with a diameter around 100 nm. Meanwhile, POVF polymer provides the active azide group for incorporating a positron emission tomography (PET) imaging modality via a facile strategy based on metal-free click chemistry. This nanocarrier system could not only be used for co-delivery of PTX and FTS, but also for PET imaging guided drug delivery. In the 4T1.2 tumor bearing mice, PET imaging showed rapid uptake and slow clearance of radiolabeled PTX/POVF nanomicelles in the tumor tissues. In addition, the FTS-based multi-functional nanocarrier was able to inhibit tumor growth effectively, and the co-delivery of PTX by the carrier further improved the therapeutic effect.

• 出版日期2018-7-15
• 单位重庆医科大学