1. Academic Validation
  2. 6-Aminocaproic acid as a linker to improve near-infrared fluorescence imaging and photothermal cancer therapy of PEGylated indocyanine green

6-Aminocaproic acid as a linker to improve near-infrared fluorescence imaging and photothermal cancer therapy of PEGylated indocyanine green

  • Colloids Surf B Biointerfaces. 2021 Jan;197:111372. doi: 10.1016/j.colsurfb.2020.111372.
Qiang Hu 1 Kesi Wang 2 Liyan Qiu 3
Affiliations

Affiliations

  • 1 College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
  • 2 Ministry of Educational (MOE) Key Laboratory of Macromolecular Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang University, Hangzhou 310027, China.
  • 3 Ministry of Educational (MOE) Key Laboratory of Macromolecular Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang University, Hangzhou 310027, China. Electronic address: lyqiu@zju.edu.cn.
Abstract

Clinical extensive application of indocyanine green (ICG) is limited by several drawbacks such as poor bioenvironmental stability, aggregate propensity, and rapid elimination from the body, etc. In this study, we construct a novel amphiphilic mPEG-ACA-ICG conjugate by modifying synthetic heptamethine cyanine derivative ICG-COOH with a hydrophobic linker 6-aminocaproic acid (ACA) and amino-terminal poly(ethylene glycol) (mPEG-NH2). The as-prepared mPEG-ACA-ICG conjugate has the ability to self-assemble into micellar aggregates in an aqueous solution with a lower CMC value than mPEG-ICG conjugate without ACA linker. More importantly, compared with free ICG and mPEG-ICG conjugate, mPEG-ACA-ICG nanomicelles exhibited better stability and higher photothermal conversion efficiency upon near-infrared LIGHT irradiation due to the intramolecular introduction of a hydrophobic ACA segment. In our in vivo experiment, mPEG-ACA-ICG nanomicelles ensured the formidable effect on tumor photothermal therapy (PTT) and the maximum tumor inhibition rate reached 72.6 %. In addition, real-time determination ability for fluorescence image-guided surgery (FIGS) of mPEG-ACA-ICG nanomicelles was also confirmed on tumor xenograft mice model. Taken together, mPEG-ACA-ICG conjugate may hold great promise for non-invasive Cancer theranostics.

Keywords

Cancer photothermal therapy; Fluorescence image-guided surgery; Indocyanine green; Nanomicelle; PEGylated conjugation.

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