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Anti Cancer · Journal article
International Journal of Pharmaceutics: X · June 29, 2026
Early or partial results. Treat as a signal, not a conclusion.
This preclinical study describes a novel folate receptor-targeted micelle system (BP@FAPG) for dual-responsive paclitaxel delivery with integrated fluorescence imaging in breast cancer cells. The system demonstrated enhanced cellular uptake, nanomolar-range cytotoxicity, and tumor spheroid penetration in vitro, providing proof-of-concept for ROS-activatable theranostic drug delivery.
In vitro cellular assay and tumor spheroid model. MDA-MB-231 breast cancer cells and three-dimensional tumor spheroids. Intervention: BP@FAPG (folic acid-conjugated polyglycidol micelles loaded with ROS-responsive fluorophore-drug conjugate BTBP-PTX). Compared with: BP@GAPG (non-targeted control micelles).
Over 80% paclitaxel release within 24 h under simulated tumor microenvironment conditions Approximately 2.5-fold enhanced cellular uptake in MDA-MB-231 cells compared to non-targeted controls IC50 of 60 nM demonstrated in cytotoxicity assays
No in vivo efficacy, toxicity, or pharmacokinetic data provided Confidence intervals and p-values for uptake and cytotoxicity not provided
This folate-targeted, dual-responsive micelle system offers a preclinical foundation for combining targeted paclitaxel delivery with real-time fluorescence imaging in FR-α-positive breast cancers. Translation to in vivo models and clinical settings requires validation of efficacy, safety, pharmacokinetics, and imaging performance.
Preclinical cellular assay data demonstrating targeted drug delivery and imaging in breast cancer cells with promising uptake and cytotoxicity results.
As stated by the source record.
Quoted from the source exactly as published.
This folate-targeted, dual-responsive micelle system offers a preclinical foundation for combining targeted paclitaxel delivery with real-time fluorescence imaging in FR-α-positive breast cancers. Translation to in vivo models and clinical settings requires validation of efficacy, safety, pharmacokinetics, and imaging performance.
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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.
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