Repurposing Mesalamine via Peptide-Functionalized Zeolitic Imidazolate Framework-8 (ZIF-8) Nanoparticles for Selective Breast Cancer Targeting
Johari NAS, Borzehandani MY, Silvaraju G, Azhar MA, Saad N, Razali R, Kamal NAMA
Summary
Researchers developed an integrin-targeting nanosystem by encapsulating mesalamine (MES) within ZIF-8 nanoparticles functionalized with the Arg-Gly-Asp (RGD) peptide. The MES-RGD@nZIF-8 formulation achieved 99.69% encapsulation efficiency and induced 65% cytotoxicity against breast cancer cells at 48 hours, with a selectivity index of 4.53 — demonstrating significant preferential killing of cancer cells over normal cells.
Clinical Significance
This study demonstrates how small bioactive peptides like RGD can be leveraged to dramatically improve drug targeting in cancer therapy. The approach of drug repurposing (using mesalamine, an anti-inflammatory) combined with peptide-functionalized nanoparticles could reduce development timelines and costs for novel cancer therapies.
Key Findings:
- RGD-functionalized ZIF-8 nanoparticles with 99.69% drug encapsulation
- 65% cytotoxicity in breast cancer cells vs. free mesalamine
- Selectivity index of 4.53 (strong preference for cancer over normal cells)
- pH-responsive release: controlled at physiological pH, accelerated under acidic tumor conditions
- Molecular docking confirmed enhanced MES binding affinity with RGD
Clinical Takeaway: Peptide-functionalized nanoparticles represent a promising platform for repurposing existing drugs in oncology — offering improved tumor selectivity with potentially fewer systemic side effects.
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