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Evaluation of sugammadex self-association
Sergey V Kurkov1, Martin Messner, Marjoleine Lucassen
1Faculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, Iceland.
International Journal of Pharmaceutics
|May 5, 2011
Summary
Sugammadex, a cyclodextrin derivative, was investigated for self-association in water. Studies confirmed sugammadex does not self-associate across a broad concentration range, indicating solution stability.
Area of Science:
- Pharmaceutical Chemistry
- Supramolecular Chemistry
- Analytical Chemistry
Background:
- Sugammadex is a modified gamma-cyclodextrin (γCD) derivative.
- It functions as an antagonist for steroidal neuromuscular blocking agents.
- Understanding its behavior in aqueous solution is crucial for formulation and administration.
Purpose of the Study:
- To investigate the self-association tendency of sugammadex in aqueous solution.
- To determine the concentration range over which sugammadex remains stable.
- To provide data supporting the reliable use of sugammadex in clinical settings.
Main Methods:
- Permeation studies using semi-permeable cellophane membranes.
- Dynamic light scattering (DLS) for particle size analysis.
- Sedimentation equilibrium analytical ultracentrifugation (SE-AUC) for molecular weight determination.
Main Results:
- All three independent methods yielded consistent results.
- No evidence of sugammadex self-association was observed.
- This lack of self-association was consistent across a wide concentration range (0.25 to 100 mg/ml).
Conclusions:
- Sugammadex exhibits no self-association in aqueous solutions within the tested concentration range.
- The physical stability of sugammadex in solution is confirmed.
- These findings support the formulation and clinical application of sugammadex.
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