Therapeutic
drug monitoring is central to optimize therapeutic efficacy and minimize adverse events; however, the pharmacokinetics and pharmacodynamics of most drugs differ greatly among individuals. Evaluation of the therapeutic response is in urgent need to help clinician predict the clinical dose of
drug. Herein, we described an analytical assay using
gold nanocluster (AuNC)-decorated
metal-organic frameworks (MOFs) for targeted
drug delivery and monitoring pharmacodynamics, giving attractive options for studying individualized
therapy. The
camptothecin (Cam) anticancer
drug was caged in the NH2-MIL-101(Fe) MOFs. Modification with pegylated
folate (FA) for specifically recognizing a FA receptor on the
cancer cell membrane significantly improved the delivery efficiency. Intercellular delivery of Cam initiated programmed death of cells and upregulated the apoptosis
indicator (caspase-3), which cleaved the
peptide linker between AuNCs and MOFs. The quenched fluorescence of AuNCs was then recovered once the
peptide was enzymatically cleaved by
caspase-3. Real-time monitoring of targeted
drug delivery was achieved by imaging of the light-up fluorescence in HepG2 cells, while the amount of
caspase-3 could be quantified by detecting Au in the released AuNCs in inductively coupled plasma mass spectrometry (ICP-MS) with a limit of detection (LOD) of 0.12 ng mL-1. Our assay emphasizes the application of multifunctional nanomaterial for therapeutic self-monitoring and quantitative evaluation of therapeutic response, allowing the acceleration of
drug evaluation.