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Boosting Tadalafil Bioavailability via Sono-Assisted Nano-Emulsion-Based Oral Jellies: Box-Behnken Optimization and
Hany S M Ali1,2, Sameh A Ahmed3,4, Abdulmalik A Alqurshi1
1Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, Taibah University, Al-Madinah Al-Munawarah P.O. Box 344, Saudi Arabia.
Pharmaceutics
|December 23, 2022
Summary
This study developed tadalafil (TAD) nano-emulsions using ultrasonic technology to improve oral bioavailability. The optimized nano-emulsion-based jelly formulation significantly enhanced TAD dissolution and in vivo absorption.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Nanotechnology
Background:
- Tadalafil (TAD) exhibits poor solubility, limiting its oral bioavailability for erectile dysfunction treatment.
- Ultrasonic technology offers a promising approach to formulate nano-emulsions for poorly soluble drugs.
- Addressing TAD's bioavailability challenges is crucial for effective therapeutic outcomes.
Purpose of the Study:
- To prepare and optimize tadalafil-loaded nano-emulsions using ultrasonic technology.
- To investigate the impact of emulsifier concentration, amplitude, and sonication time on nano-emulsion characteristics.
- To formulate and evaluate tadalafil nano-emulsion-based jellies (NEJ) for improved bioavailability and stability.
Main Methods:
- Box-Behnken design was employed to optimize sono-emulsification parameters (emulsifier concentration, amplitude, ultrasonication time).
- Nano-emulsions were characterized for average droplet size (ADS) and polydispersity index (PDI).
- Optimized nano-emulsions were formulated into jellies and evaluated for physical properties, drug release, and in vivo bioavailability in rats.
Main Results:
- Optimized nano-emulsions achieved small ADS (99.67 ± 7.55 nm) and PDI (0.45 ± 0.04).
- The nano-emulsion-based jelly (NEJ) demonstrated over 96% drug dissolution within 30 minutes, significantly higher than unprocessed TAD (14%).
- In vivo studies showed a substantial increase in TAD bioavailability (AUC0−24h) with NEJ compared to unprocessed TAD in rats.
Conclusions:
- Ultrasonic technology effectively produced stable tadalafil nano-emulsions with desirable characteristics.
- The developed NEJ formulation offers an improved therapeutic option for tadalafil administration with immediate-release properties.
- NEJ represents a successful strategy for enhancing tadalafil bioavailability and patient compliance.
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