Organic NIR-II dyes with ultralong circulation persistence for image-guided delivery and therapy

J Control Release. 2022 Feb:342:157-169. doi: 10.1016/j.jconrel.2022.01.005. Epub 2022 Jan 5.

Abstract

Nanocarriers hold great promise for the controlled release of therapeutic payloads to target organs/tissues and extended duration of anticancer agents in the bloodstream. However, limited data on their in vivo pharmacokinetics and delivery process hamper clinical applications. Here we report a series of micellar nanocarriers self-assembled from new-generation thiophenthiadiazole (TTD)-based NIR-II fluorophores HLAnP (n = 1-4) for simultaneous bioimaging and drug delivery. The NIR-II HLA4P nanocarrier displays exceptional non-fouling performance, minimal immunogenicity, ultralong blood half-life, and high tumor accumulation even with different administration routes. When used as a drug carrier, HLA4P with encapsulated doxorubicin (DOX) realized accurate tumor targeting and continuous real-time in vivo NIR-II tracking of drug delivery and therapy, showing a sustained release rate, improved therapeutic effect, and diminished cardiotoxicity as compared to free DOX. This study provides a new perspective on the design of dual-functional NIR-II fluorophores for diagnostic and therapeutic applications.

Keywords: Drug delivery; Fluorescence imaging; Image-guided therapy; Second near-infrared window (NIR-II); Self-assembly.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Doxorubicin
  • Drug Carriers
  • Drug Delivery Systems
  • Fluorescent Dyes
  • Nanoparticles*
  • Theranostic Nanomedicine* / methods

Substances

  • Drug Carriers
  • Fluorescent Dyes
  • Doxorubicin