Effects of Fluorinated Functionalization of Linker on Quercetin Encapsulation, Release and Hela Cell Cytotoxicity of Cu-Based MOFs as Smart pH-Stimuli Nanocarriers

Chemistry. 2024 Jan 2;30(1):e202301630. doi: 10.1002/chem.202301630. Epub 2023 Nov 10.

Abstract

Controlled delivery of target molecules is required in many medical and chemical applications. For such purposes, metal-organic frameworks (MOFs), which possess desirable features such as high porosity, large surface area, and adjustable functionalities, hold great potential as drug carriers. Herein, Quercetin (QU), as an anticancer drug, was loaded on Cu2 (BDC)2 (DABCO) and Cu2 (F4 BDC)2 )DABCO) MOFs (BDC=1,4-benzenedicarboxylate and DABCO=1,4-diazabicyclo[2.2.2]octane). As these Cu-MOFs have a high surface area, an appropriate pore size, and biocompatible ingredients, they can be utilized to deliver QU. The loading efficiency of QU in these MOFs was 49.5 % and 41.3 %, respectively. The drug-loaded compounds displayed sustained drug release over 15 days, remarkably high drug loading capacities and pH-controlled release behavior. The prepared nanostructures were characterized by different characterization technics including FT-IR, PXRD, ZP, TEM, FE-SEM, UV-vis, and BET. In addition, MTT assays were carried out on the HEK-293 and HeLa cell lines to investigate cytotoxicity. Cellular apoptosis analysis was performed to investigate the cell death mechanisms. Grand Canonical Monte Carlo simulations were conducted to analyze the interactions between MOFs and QU. Moreover, the stability of MOFs was also investigated during and after the drug release process. Ultimately, kinetic models of drug release were evaluated.

Keywords: Drug delivery; Nanoparticle; Nanoporous; Quercetin; Sustained release.

MeSH terms

  • Drug Carriers / chemistry
  • Drug Carriers / toxicity
  • HEK293 Cells
  • HeLa Cells
  • Humans
  • Hydrogen-Ion Concentration
  • Metal-Organic Frameworks* / chemistry
  • Quercetin
  • Spectroscopy, Fourier Transform Infrared

Substances

  • Metal-Organic Frameworks
  • Quercetin
  • Drug Carriers