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Improving the drug delivery performance of ZIF-8 with amine functionalization as a 5-fluorouracil nanocarrier

Sahba Mirzanejad, Mojtaba Bagherzadeh, Arshad Bayrami, Hossein Daneshgar, Aida Bahrami, Majid Mahdavi

2025Scientific Reports23 citationsDOIOpen Access PDF

Abstract

This study investigates the effect of amine functional groups in ZIF-8 metal–organic frameworks on the loading and release of 5-fluorouracil (5-FU). The facile and cost-effective solvent-assisted linker exchange (SALE) method was used to exchange 2-methylimidazole (2-MIM) linkers with 3-amino-1,2,4-triazole (Atz) in the ZIF-8 structure, which resulted in a synthesis of ZIF-8A with 22, 53, and 74% Atz exchange, respectively. The prepared nanoparticles were characterized by 1 H-NMR, XRD, FT-IR, FE-SEM, UV–Vis spectroscopy, and zeta potential analysis. Drug encapsulation efficiency results showed 12% for 5-FU@ZIF-8 which increased to 48% for 5-FU@ZIF-8A(53%). Also, the results of in-vitro experiments exhibited the pH-responsive behavior of nanocarriers and slower release for 5-FU@ZIF-8A(53%) compared to 5-FU@ZIF-8. The increase in drug encapsulation efficiency and slower release is due to the presence of the amine functional group in the structure, which improves the host-guest interactions between drug molecules and linkers. Moreover, the MTT assay was performed on MCF-7 and HFF-2 cell lines which revealed that 5-FU@ZIF-8A(53%) exhibited more significant cytotoxicity toward cancer cells while less toxicity toward normal cells compared to 5-FU@ZIF-8. These findings highlight the capability of amine-functionalized ZIF-8 as an effective drug delivery system for 5-FU and demonstrate the potential of the facial and low-cost SALE approach as a promising technique in nanocarrier development.

Topics & Concepts

NanocarriersSurface modificationDrug deliveryDrugAmine gas treatingFluorouracilNanotechnologyChemistryPharmacologyCombinatorial chemistryMedicineMaterials scienceOrganic chemistryInternal medicineChemotherapyPhysical chemistryMetal-Organic Frameworks: Synthesis and ApplicationsNanoplatforms for cancer theranosticsSilicone and Siloxane Chemistry
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