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Rutin/Sulfobutylether-β-Cyclodextrin as a Promising Therapeutic Formulation for Ocular Infection
Federica De Gaetano1, Martina Pastorello1, Venerando Pistarà2
1Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Ferdinando Stagno d'Alcontres 31, 98166 Messina, Italy.
Pharmaceutics
|February 24, 2024
Summary
This study developed a novel liquid formulation using rutin/sulfobutylether-β-cyclodextrin (RTN/SBE-β-CD) inclusion complexes to enhance rutin
Area of Science:
- Ophthalmic drug delivery
- Natural product chemistry
- Nanotechnology in medicine
Background:
- Ocular pathologies pose significant therapeutic challenges due to anatomical and physiological barriers.
- Flavonoids, like rutin, offer therapeutic benefits (anticancer, anti-inflammatory, antibacterial) but suffer from poor water solubility, limiting clinical use.
- Developing effective ocular delivery systems for natural products is crucial for improved treatment outcomes.
Purpose of the Study:
- To design and characterize a liquid formulation of rutin/sulfobutylether-β-cyclodextrin (RTN/SBE-β-CD) inclusion complex for ocular applications.
- To enhance the water solubility and bioavailability of rutin for treating ocular infections.
- To evaluate the in vitro antibacterial and antibiofilm efficacy of the developed formulation.
Main Methods:
- Formation and characterization of RTN/SBE-β-CD inclusion complex using UV-vis titration and SupraFit software.
- Determination of stoichiometry (1:1 molar ratio) and binding constant (Kc, 9660 M-1).
- Assessment of water solubility enhancement (20-fold increase) and dissolution time (30 min).
- Structural elucidation using NMR spectroscopy and molecular modeling.
- In vitro evaluation of antibacterial and antibiofilm activity against *Staphylococcus aureus* and *Pseudomonas aeruginosa*.
Main Results:
- A stable RTN/SBE-β-CD inclusion complex was successfully formed with a 1:1 molar ratio.
- The formulation exhibited a 20-fold increase in water solubility (2.5 mg/mL) compared to free rutin (0.125 mg/mL), dissolving within 30 minutes.
- NMR and molecular modeling confirmed the complexation involving the flavonoid moiety.
- The formulation demonstrated significantly enhanced in vitro antibacterial and antibiofilm activity against tested bacterial strains compared to free rutin.
Conclusions:
- The RTN/SBE-β-CD inclusion complex represents a promising strategy to overcome the solubility limitations of rutin for ocular applications.
- This novel formulation offers enhanced solubility and improved therapeutic potential for treating ocular infections.
- The developed system holds potential for advancing natural product-based therapies in ophthalmology.
