ROS-Activatable "off-on" Fluorescent Prodrug Loaded Micelles for Targeted Therapy and in Situ Imaging of Breast Cancer Cells.

Authors

Jindong Li, Xinyu Zhang, Ting Guo, Ziliang Liu, Huiling Zhou, Fang Zhang, Yan Zhang, Shengnan Yin

Published in

International journal of pharmaceutics: X. Volume 12. Pages 100592. Epub Jun 29, 2026.

Abstract

This study developed an intelligent drug-loaded micelle system based on folic acid-conjugated polyglycidol (FAPG), which incorporates a reactive oxygen species (ROS) responsive fluorophore-drug conjugate (BTBP-PTX, BP). The system integrates folate receptor-α (FR-α) targeting, esterase/ROS dual-responsive drug release, and aggregation-induced emission (AIE)-based fluorescence activation for tumor-targeted delivery and imaging. Under simulated tumor microenvironment conditions (esterase-rich, high ROS levels), the system displayed dual-responsive release behavior, achieving over 80% paclitaxel (PTX) release within 24 h through esterase-catalyzed ester bond cleavage and ROS-triggered oxalate bond hydrolysis. Cellular assays demonstrated that BP@FAPG enhanced cellular uptake by approximately 2.5-fold in MDA-MB-231 cells compared to non-targeted controls BP@GAPG, along with significant cytotoxicity (IC₅₀ = 60 nM) and deep penetration into three-dimensional tumor spheroids-effects primarily attributed to FR-α-mediated endocytosis. Furthermore, the AIE fluorophore was activated during drug release, allowing real-time fluorescence tracking of micelle localization and release dynamics.

PMID:
42436868
Bibliographic data and abstract were imported from PubMed on 12 Jul 2026.

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