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Published on: March 29, 2019
p-Sulfonato-Calix[4]arene Micelles Stabilize a Povidone Iodine Solution: Supramolecular Interactions, Iodine
Rossella Migliore1, Loredana Ferreri1, Danilo Aleo2
1Institute of Biomolecular Chemistry-National Research Council (C.N.R.), Via Paolo Gaifami 18, 95126 Catania, Italy.
Abstract:
Povidone iodine (PVPI) is an antiseptic widely used against a broad spectrum of pathogens. However, undesired side-effects are still associated with PVPI treatment due to the irritant effect of iodine. Reducing the concentration of a PVPI formulation could provide safer and more friendly formulations, for routine use and applications in very delicate organs such as the eye. However, managing the storage of a low-concentration solution of PVPI is challenging due to the high iodine volatility. In this study, we demonstrated that an amphiphilic p-sulfonato-calix[4]arene derivative forming micelles (SC4OC6) improves the stability of a 0.1% PVPI aqueous buffered solution. UV-vis and NMR spectra as well as dynamic and electrophoretic light scattering measurements showed that SC4OC6 establishes non-covalent supramolecular interactions with PVPI, resulting in the formation of nanoaggregates with a negatively charged surface. Isothermal titration calorimetry provided the aggregation parameters and evidenced that the formation of the supramolecular assembly is an enthalpically favored process. The interaction of SC4OC6 with PVPI enhances the iodine retention and stability of the solution without affecting the rapid and effective bactericidal activity of PVPI, as demonstrated by a time-killing assay with Staphylococcus epidermidis.
Insights
This study shows a new micelle-forming compound (SC4OC6) stabilizes low-concentration povidone iodine (PVPI) antiseptic solutions. This innovation enhances iodine retention and formulation safety without compromising bactericidal effectiveness.
Area of Science:
- Materials Science
- Supramolecular Chemistry
- Antimicrobial Agents
Background:
- Povidone iodine (PVPI) is a broad-spectrum antiseptic with potential irritant side-effects due to iodine.
- Lowering PVPI concentration offers safer formulations, especially for sensitive applications like ophthalmology.
- Iodine volatility poses challenges for storing low-concentration PVPI solutions.
Purpose of the Study:
- To investigate the stabilizing effect of an amphiphilic p-sulfonato-calix[4]arene derivative (SC4OC6) on 0.1% PVPI solutions.
- To elucidate the supramolecular interactions between SC4OC6 and PVPI.
- To assess the impact of SC4OC6 on PVPI stability and antimicrobial efficacy.
Main Methods:
- UV-vis and NMR spectroscopy to characterize PVPI-SC4OC6 interactions.
- Dynamic and electrophoretic light scattering for nanoaggregate analysis.
- Isothermal titration calorimetry to determine thermodynamic parameters.
- Time-killing assays to evaluate bactericidal activity against Staphylococcus epidermidis.
Main Results:
- SC4OC6 forms stable micelles that interact non-covalently with PVPI, creating negatively charged nanoaggregates.
- Spectroscopic and scattering data confirmed supramolecular complex formation.
- Isothermal titration calorimetry indicated an enthalpically favored self-assembly process.
- The SC4OC6-PVPI complex enhanced iodine retention and solution stability.
- Antimicrobial assays showed preserved bactericidal activity against S. epidermidis.
Conclusions:
- SC4OC6 effectively stabilizes low-concentration PVPI solutions by forming supramolecular nanoaggregates.
- This approach improves iodine retention and formulation stability.
- The enhanced PVPI formulations maintain rapid and effective bactericidal action, offering a safer antiseptic option.
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