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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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Preparation and pharmacokinetic study of aprepitant-sulfobutyl ether-β-cyclodextrin complex
1School of Pharmaceutical Sciences, Nanjing University of Technology, 5th Mofan Road, Nanjing, 210009, China.
AAPS Pharmscitech
|October 30, 2013
Summary
Sulfobutyl ether-β-cyclodextrin (SBE-β-CD) complexation enhanced aprepitant (APR) solubility and dissolution. The optimized formulation showed comparable bioavailability to Emend, offering a practical solution for APR delivery.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Medicinal Chemistry
Background:
- Aprepitant (APR), a neurokinin 1 receptor antagonist, effectively treats nausea and vomiting.
- Poor water solubility of APR limits its therapeutic efficacy and formulation options.
Purpose of the Study:
- To optimize a capsule formulation of an APR-SBE-β-CD inclusion complex.
- To evaluate the solubility, dissolution rate, and bioavailability of the optimized formulation.
Main Methods:
- Complexation via saturated-aqueous solution method.
- Characterization using FTIR, XRPD, and DSC.
- Pharmacokinetic evaluation using LC-MS/MS with Emend as reference.
Main Results:
- The SBE-β-CD complex significantly enhanced APR's dissolution rate and extent of release compared to Emend.
- The optimized formulation demonstrated comparable bioavailability to Emend.
- Characterization confirmed the formation of the APR-SBE-β-CD inclusion complex.
Conclusions:
- SBE-β-CD complexation is a viable strategy to improve APR solubility and bioavailability.
- This approach offers a practical and cost-effective method for developing enhanced APR formulations.
- The optimized formulation holds potential for improved clinical application in managing chemotherapy- and post-operative nausea and vomiting.
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