Genistein in 1:1 inclusion complexes with ramified cyclodextrins: theoretical, physicochemical and biological

Corina Danciu1, Codruta Soica2, Mircea Oltean3

  • 1Faculty of Pharmacy, University of Medicine and Pharmacy "Victor Babeş", Eftimie Murgu Square, No. 2, 300041 Timişoara, Romania. cadehelean@umft.ro.

Insights

Genistein (Gen) complexation with cyclodextrins (CDs) improves its anticancer and antimicrobial properties. This study shows three CDs can enhance Gen

Area of Science:

  • Phytochemistry
  • Drug Delivery
  • Computational Chemistry

Background:

  • Genistein (Gen), an isoflavone, exhibits anticancer properties but suffers from low water solubility.
  • Cyclodextrins (CDs) are hydrophilic polymers used to improve the solubility of poorly soluble drugs.
  • Complexation with CDs may enhance Gen's therapeutic efficacy.

Purpose of the Study:

  • To theoretically analyze the complex formation between Gen and three different ramified CDs.
  • To evaluate the in vitro and in vivo activities of Gen-CD complexes.
  • To identify the most suitable CD for Gen incorporation in pharmaceutical formulations.

Main Methods:

  • Theoretical analysis of interaction energy for Gen:CD complex formation at a 1:1 molar ratio.
  • Screening of in vitro antiproliferative activity against human cancer cell lines.
  • Assessment of antimicrobial activity against Bacillus subtilis and antiangiogenic activity via CAM assay.

Main Results:

  • Gen-CD complexes demonstrated antiproliferative activity with varying IC50 values across tested cell lines.
  • Significant antimicrobial activity was observed for Gen-CD complexes against Bacillus subtilis.
  • Antiangiogenic effects were confirmed by the CAM assay, with differences noted between pure Gen and its complexes.

Conclusions:

  • The three studied cyclodextrins show potential for complexing genistein.
  • Gen-CD complexes exhibit enhanced antiproliferative, antimicrobial, and antiangiogenic activities.
  • These findings support the use of cyclodextrins for developing improved genistein-based pharmaceutical formulations.

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