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Inclusion complexes of β-cyclodextrin and polymorphs of mebendazole: Physicochemical characterization
Elbio Saidman1, Ana K Chattah2, Leslie Aragón1
1Laboratorio de Control de Calidad de Medicamentos, Facultad de Química Bioquímica y Farmacia, Universidad Nacional de San Luis, Argentina.
Summary
Mebendazole (MBZ) inclusion complexes with beta-cyclodextrin were developed to improve drug absorption. These new crystalline forms enhanced MBZ solubility while maintaining physical stability.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery
Background:
- Mebendazole (MBZ), a WHO essential drug, exhibits poor gastrointestinal absorption due to its low solubility.
- Cyclodextrins are known to enhance drug solubility and permeability.
- MBZ exists in multiple solid forms (polymorphs), potentially affecting its bioavailability.
Purpose of the Study:
- To create and characterize inclusion complexes of Mebendazole polymorphs A and C with beta-cyclodextrin.
- To evaluate the impact of complexation on the solubility and physical stability of MBZ.
- To elucidate the inclusion complexation mechanism and molecular interactions.
Main Methods:
- Preparation of inclusion complexes of MBZ polymorphs A and C with beta-cyclodextrin.
- Solid-state characterization using Fourier transform infrared spectroscopy (FTIR), powder X-ray diffractometry (PXRD), and solid-state nuclear magnetic resonance (ssNMR).
- Molecular modeling and Atoms in Molecules (AIM) theory for analyzing inclusion modes and intermolecular interactions.
- Solubility studies in simulated physiological media.
Main Results:
- New crystalline forms of MBZ-beta-cyclodextrin inclusion complexes were successfully prepared.
- Spectroscopic and diffractometry data indicated successful complex formation, with shifts and broadening observed.
- Molecular modeling suggested a favorable 'head down' orientation for MBZ within the cyclodextrin cavity.
- Complexation significantly increased MBZ solubility in simulated physiological media.
- The physical stability of MBZ polymorphs was not adversely affected by complex formation.
Conclusions:
- Beta-cyclodextrin inclusion complexation is a viable strategy to enhance the solubility of Mebendazole polymorphs A and C.
- The developed complexes represent novel crystalline entities with improved dissolution properties.
- The findings support the potential of cyclodextrin complexation for improving the oral bioavailability of poorly soluble drugs like MBZ.
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