Multifunctional Liposome: A Bright AIEgen-Lipid Conjugate with Strong Photosensitization

Angew Chem Int Ed Engl. 2018 Dec 10;57(50):16396-16400. doi: 10.1002/anie.201809641. Epub 2018 Nov 14.

Abstract

Liposomes have been used as popular drug delivery systems for cancer therapy. However, it is difficult to track traditional liposome delivery systems in an efficient and stable fashion to assess their delivery efficacy and biodistribution after administration. Meanwhile, conventional fluorescent liposomes containing optical tracers face the challenge of aggregation-caused quenching. Herein, we report a strategy for the integration of an aggregation-induced emission fluorogen with a liposome to yield an AIEgen-lipid conjugate, termed "AIEsome". The AIEsome exhibits bright red fluorescence along with great photostability and biocompatibility, and can be used for in vitro cancer cell labeling and in vivo tumor targeting. Meanwhile, benefiting from the excellent photosensitizing ability of the AIEgen and its good oxygen exposure in aqueous media, the AIEsome also performs well in efficient photodynamic therapy (PDT) for both in vitro cancer cell ablation and in vivo antitumor therapy after white light illumination.

Keywords: aggregation-induced emission; antitumor therapy; fluorescence imaging; liposomes; photodynamic therapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Drug Delivery Systems
  • Female
  • Fluorescent Dyes / administration & dosage*
  • Fluorescent Dyes / pharmacokinetics
  • Fluorescent Dyes / therapeutic use
  • Lipids / chemistry*
  • Liposomes / chemistry*
  • Mammary Neoplasms, Animal / diagnostic imaging*
  • Mammary Neoplasms, Animal / drug therapy*
  • Mice
  • Optical Imaging
  • Photochemotherapy
  • Photosensitizing Agents / administration & dosage*
  • Photosensitizing Agents / pharmacokinetics
  • Photosensitizing Agents / therapeutic use
  • Tissue Distribution

Substances

  • Fluorescent Dyes
  • Lipids
  • Liposomes
  • Photosensitizing Agents