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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
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From Mechanochemically Driven Complexation and Multimodal Characterization to Stability and Toxicological Insight: A
David Klarić1, Lucija Kutleša1, Mario Jug2
1Department of Chemistry, Faculty of Science, University of Zagreb, Horvatovac 102a, 10 000 Zagreb, Croatia.
Pharmaceutics
|October 29, 2025
Summary
Cinnarizine (CIN) complexation with cyclodextrins (CDs) via mechanical activation significantly improved drug dissolution. The resulting cinnarizine/cyclodextrin complexes show promise for new pharmaceutical formulations without compromising stability.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Materials Science
Background:
- Cinnarizine (CIN) exhibits poor solubility, limiting its therapeutic use for vestibular disorders.
- Cyclodextrins (CDs), including beta-cyclodextrin (βCD), hydroxypropyl-β-cyclodextrin (HPβCD), and sulfobutylether-β-cyclodextrin (SBEβCD), are known to enhance drug solubility.
- Mechanical activation offers a solvent-free method for preparing drug-cyclodextrin complexes.
Purpose of the Study:
- To prepare and characterize 1:1 cinnarizine/cyclodextrin complexes using mechanical activation.
- To evaluate the impact of cyclodextrin complexation on cinnarizine's dissolution rate and stability.
- To develop and validate a stability-indicating method for analyzing cinnarizine and its potential degradation products.
Main Methods:
- Complexation of cinnarizine with βCD, HPβCD, and SBEβCD using high-energy vibrational milling.
- Solid-state characterization via Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA), X-ray Powder Diffraction (XRPD), and Fourier-Transform Infrared (FTIR) spectroscopy.
- Dissolution studies in phosphate buffer (pH 4.5), stability assessments under various conditions, and UHPLC-DAD-HRMS analysis for quantification and degradation product identification.
Main Results:
- Solid-state analyses confirmed successful cinnarizine-cyclodextrin interactions in the ground products.
- Cinnarizine/HPβCD complexes exhibited the highest dissolution efficiency.
- No degradation products were detected under accelerated stability conditions, indicating good chemical stability of the complexes.
Conclusions:
- Solid-state complexation of cinnarizine with cyclodextrins effectively enhances drug dissolution.
- The prepared cinnarizine/cyclodextrin complexes demonstrate good stability, making them suitable for novel pharmaceutical formulations.
- Mechanical activation is a viable technique for producing stable and improved cinnarizine drug delivery systems.
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