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Encapsulation of Risperidone by Methylated β-Cyclodextrins: Physicochemical and Molecular Modeling Studies
Laura Sbârcea1,2, Ionuț-Mihai Tănase3, Adriana Ledeți1,2
1Department of Pharmacy I, Faculty of Pharmacy, "Victor Babeş" University of Medicine and Pharmacy, 2 Eftimie Murgu Square, 300041 Timisoara, Romania.
Molecules (Basel, Switzerland)
|December 8, 2020
Summary
This study enhanced risperidone (RSP) solubility using cyclodextrin complexation. The RSP/DM-β-CD complex showed significantly improved solubility, paving the way for better drug formulations.
Area of Science:
- Pharmaceutical Sciences
- Physical Chemistry
- Drug Delivery
Background:
- Risperidone (RSP) is an atypical antipsychotic with poor water solubility, limiting its bioavailability.
- Methylated β-cyclodextrins (DM-β-CD and TM-β-CD) are explored to improve the solubility of poorly soluble drugs.
- Enhancing RSP solubility is crucial for developing more effective therapeutic formulations.
Purpose of the Study:
- To create and characterize supramolecular adducts of risperidone (RSP) with methylated β-cyclodextrins (DM-β-CD and TM-β-CD).
- To enhance the solubility and improve the biopharmaceutical profile of risperidone.
- To investigate the stoichiometry and physicochemical properties of the formed inclusion complexes.
Main Methods:
- Formation of inclusion complexes between RSP and DM-β-CD or TM-β-CD.
- Characterization using thermoanalytical methods (TG/DTG/HF), PXRD, UATR-FTIR, and UV spectroscopy.
- Saturation solubility studies and Job's method for stoichiometry determination; molecular modeling for interaction analysis.
Main Results:
- Supramolecular adducts (inclusion complexes) of RSP with DM-β-CD and TM-β-CD were successfully formed.
- The stoichiometry of the inclusion complexes was determined to be 2:1 (RSP:CD) for both systems.
- Significant enhancement in RSP solubility was observed, particularly with DM-β-CD, indicating successful encapsulation within the cyclodextrin cavity.
Conclusions:
- The formation of inclusion complexes between RSP and methylated β-cyclodextrins effectively enhances drug solubility.
- The RSP/DM-β-CD system demonstrates potential for developing novel formulations with improved risperidone bioavailability.
- Further research into this guest-host system is recommended for advanced drug delivery applications.
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