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A Novel Oral Disintegrating Tablet Containing Aprepitant Nanocrystal Developed by Freeze-Drying Technology: An
Yutong Li1, Meihui Yi1, Keke Ma1
1School of Pharmaceutical Sciences, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China.
The AAPS Journal
|December 10, 2025
Summary
This study created novel aprepitant (APT) nanocrystal oral disintegrating tablets (ODTs) to significantly boost drug bioavailability. The optimized ODTs demonstrated rapid disintegration and enhanced drug absorption, offering a promising new oral delivery strategy.
Area of Science:
- Pharmaceutical Technology
- Nanotechnology
- Drug Delivery
Background:
- Aprepitant (APT) exhibits poor oral bioavailability due to its low solubility.
- Novel drug delivery systems are needed to enhance APT's therapeutic efficacy.
Purpose of the Study:
- To develop and optimize aprepitant (APT) nanocrystal-containing oral disintegrating tablets (ODTs).
- To enhance the oral bioavailability of APT through a rapid disintegration approach.
Main Methods:
- Aprepitant nanocrystal suspension (APT-NS) prepared using miniaturized media milling.
- Spray-drying of APT-NS into dry powders (APT-NCS) followed by freeze-drying into ODTs.
- Central composite design-response surface methodology (CCD-RSM) for formulation optimization.
Main Results:
- Optimized APT-ODTs exhibited rapid disintegration (<5 s) and excellent dissolution (>95% in 2 min).
- Physicochemical characterization (XRD, DSC, FTIR) confirmed formulation stability.
- Pharmacokinetic studies showed approximately twofold higher AUC0-48h for APT-NS and APT-ODTs compared to free APT.
Conclusions:
- The developed APT-ODT formulation successfully improved APT's oral bioavailability.
- This nanocrystal-based ODT represents a promising strategy for enhanced APT clinical application.
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