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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
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Formulation Studies with Cyclodextrins for Novel Selenium NSAID Derivatives.
Sandra Ramos-Inza1,2, Cristina Morán-Serradilla1, Leire Gaviria-Soteras1
1Department of Pharmaceutical Sciences, University of Navarra, Irunlarrea 1, E-31008 Pamplona, Spain.
International Journal of Molecular Sciences
|February 10, 2024
Summary
Selenium-containing NSAID derivatives show anticancer potential but face solubility issues. Cyclodextrin (CD) complexation significantly enhances the water solubility of these compounds, aiding their pharmaceutical development.
Area of Science:
- Pharmaceutical Chemistry
- Medicinal Chemistry
- Supramolecular Chemistry
Background:
- Cyclodextrins (CDs) are widely used to improve drug solubility, stability, and bioavailability through inclusion complex (IC) formation.
- Selenium (Se)-containing compounds exhibit promising anticancer properties, but their clinical application is hindered by poor aqueous solubility and unpleasant taste.
Purpose of the Study:
- To enhance the aqueous solubility of selenium-containing nonsteroidal anti-inflammatory drug (NSAID) derivatives with demonstrated antitumoral activity using cyclodextrins.
- To investigate the interactions between CDs and Se-NSAID derivatives to overcome pharmaceutical limitations.
Main Methods:
- Formation of inclusion complexes (ICs) between various cyclodextrins (CDs) and selenium-containing NSAID derivatives (selenoester or diacyl diselenide forms).
- Analysis of CD complexes using nuclear magnetic resonance (NMR) spectroscopy.
- Construction of 3D models of theoretical CD-compound complexes using molecular modeling techniques to complement experimental data.
Main Results:
- Compounds I.3e and II.5 demonstrated a significant increase in water solubility upon complexation with CDs.
- The enhanced solubility is attributed to the formation of the most stable interactions between these specific compounds and the CDs.
- In silico studies corroborated the experimental findings, supporting the stability of the formed inclusion complexes.
Conclusions:
- Beta-cyclodextrin (β-CD) and gamma-cyclodextrin (γ-CD) were identified as the most suitable CDs for enhancing the solubility of the studied selenium derivatives.
- CD complexation is a viable strategy to overcome the pharmaceutical drawbacks of selenium-containing anticancer agents, paving the way for further clinical evaluation.
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