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Development and Characterization of Quercetin-Loaded Delivery Systems for Increasing Its Bioavailability in Cervical

Miguel Ferreira1, Diana Gomes1,2,3, Miguel Neto1

  • 1CICS-UBI-Health Science Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, Portugal.

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|March 29, 2023
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Summary

This study developed a novel chitosan/sulfonyl-ether-β-cyclodextrin (SBE-β-CD) delivery system to enhance quercetin

Keywords:
chitosancyclodextrindelivery systemsinclusion complexquercetin

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Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Cancer Therapeutics

Background:

  • Quercetin, a natural flavonoid, shows potent anticancer activity, particularly against HPV-related cancers like cervical cancer.
  • Quercetin's therapeutic potential is limited by poor aqueous solubility, stability, and low bioavailability.
  • Effective drug delivery systems are needed to overcome these limitations and improve quercetin's efficacy.

Purpose of the Study:

  • To develop and characterize chitosan/SBE-β-CD-conjugated nanoparticles for enhanced quercetin delivery.
  • To evaluate the solubility, loading capacity, and bioavailability of quercetin using these novel delivery systems in cervical cancer cells.
  • To assess the anticancer efficacy of the quercetin-loaded nanoparticles against cervical cancer cells.

Main Methods:

  • Synthesis and characterization of SBE-β-CD/quercetin inclusion complexes and chitosan/SBE-β-CD/quercetin delivery systems using varying molecular weight chitosans.
  • Nanoparticle characterization included size, polydispersity index (PdI), zeta potential, and encapsulation efficiency.
  • In vitro quercetin release studies at different pH values and cytotoxicity assays (IC50) on HeLa cervical cancer cells were performed.

Main Results:

  • High molecular weight (HMW) chitosan/SBE-β-CD/quercetin formulations achieved optimal nanoparticle characteristics: size (272.07 ± 2.87 nm), PdI (0.287 ± 0.011), zeta potential (+38.0 ± 1.34 mV), and near-perfect encapsulation efficiency (~99.9%).
  • In vitro release studies showed pH-dependent quercetin release, with significantly higher release at acidic pH (57.53% at pH 5.8) compared to physiological pH (9.6% at pH 7.4).
  • HMW chitosan/SBE-β-CD/quercetin delivery systems demonstrated a significantly enhanced cytotoxic effect on HeLa cells, with an IC50 of 43.55 μM, indicating improved quercetin bioavailability.

Conclusions:

  • Chitosan/SBE-β-CD-conjugated nanoparticles represent a promising delivery system for improving quercetin's solubility, stability, and bioavailability.
  • The developed HMW chitosan-based system effectively enhanced quercetin's anticancer activity against cervical cancer cells.
  • This nanodelivery approach holds potential for more effective therapeutic strategies against HPV-related cancers.