Quercetin, Rutin And Quercetin-Rutin Incorporated Hydroxypropyl β-Cyclodextrin Inclusion Complexes

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Biochemistry

Background:

• Flavonoids like quercetin (Q) and rutin (R) possess significant anti-inflammatory, antioxidant, and anti-cancer properties.
• Limited oral bioavailability due to poor aqueous solubility hinders the therapeutic application of Q and R.
• Hydroxypropyl-β-cyclodextrin (HP-β-CD) is a promising excipient for enhancing drug solubility and delivery.

Purpose of the Study:

• To formulate inclusion complexes of quercetin and rutin with HP-β-CD.
• To enhance the aqueous solubility, antiproliferative efficacy, and antioxidant activity of quercetin and rutin.
• To evaluate the in vitro release characteristics and synergistic effects of combined flavonoid complexes.

Main Methods:

• Formation of inclusion complexes using quercetin, rutin, and HP-β-CD.
• Characterization of complexes using ZP values and 1H-NMR spectroscopy.
• In vitro dissolution studies, MTT assays for antiproliferative activity, and DPPH assays for antioxidant activity.

Main Results:

• Aqueous solubility of Q and R increased by up to ~630-fold and ~55-fold, respectively.
• Complex formation was confirmed by 1H-NMR. In vitro release profiles varied, with Q release decreasing and R release increasing in specific formulations.
• Significant antiproliferative effects were observed, particularly for combined Q/R complexes on MDA-MB-231 and A549 cell lines. Highest antioxidant activity was noted for T9 (Q), T14 (R), and T24 (Q/R) complexes.

Conclusions:

• HP-β-CD based inclusion complexes significantly enhance the solubility and antioxidant activity of quercetin and rutin.
• The developed complexes exhibit potent in vitro antiproliferative effects against various cancer cell lines, with synergistic activity observed for combined flavonoids.
• These findings highlight the potential of Q, R, and Q/R-HP-β-CD complexes for developing effective treatments for severe disorders.