Drug intelligence / Profile preview

FA-ZA + IR780 @ HPNs

Development stage
Preclinical
Lead developer
National Chung Hsing University
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Intravenous
01

Overview

FA-ZA + IR780 @ HPNs (FA-ZA/IR780@HPNs) is a research-stage nanomedicine formulation consisting of folate (FA)-modified hybrid polymeric nanoassemblies (HPNs) designed for tumor-targeted co-delivery of two active agents: IR780 (a lipophilic heptamethine near-infrared photothermal/photosensitizing dye) and zoledronic acid (ZA, a nitrogen-containing bisphosphonate chemotherapy drug). The nanoassemblies feature a PLGA-rich core co-encapsulating IR780 and ZA/PEI complexes, stabilized by FA-modified TPGS and acidity-sensitive PEG-benzoic imine-octadecane conjugates that enable PEG detachment in the acidic tumor microenvironment. This exposes folate moieties that promote internalization via folate receptor-mediated endocytosis in folate receptor-overexpressing cancer cells (e.g., 4T1 breast cancer cells). Upon NIR laser irradiation, IR780 mediates photothermal therapy (hyperthermia), while ZA provides chemotherapeutic activity, together suppressing tumor growth and metastasis. The formulation is intended to treat aggressive breast cancer and was developed by researchers at National Chung Hsing University.

Other names
FA-ZA/IR780@HPNsIR780/zoledronic acid-containing hybrid polymeric nanoassemblies with folate modification
02

Targets

FOLR1 (FRα)FDPS (Farnesyl pyrophosphate synthase)

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