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Design of fenofibrate microemulsion for improved bioavailability.
Liandong Hu1, Hongyu Wu, Feng Niu
1School of Pharmaceutical Sciences, Hebei University, Baoding 071002, China. hbupharm@126.com
International Journal of Pharmaceutics
|September 13, 2011
Summary
This study developed a fenofibrate microemulsion for oral delivery, significantly boosting drug solubility and bioavailability. Fenofibrate microemulsions demonstrated enhanced Cmax and AUC compared to standard capsules in canine pharmacokinetic studies.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Chemistry
Background:
- Fenofibrate exhibits poor aqueous solubility, limiting its oral bioavailability.
- Developing effective oral delivery systems is crucial for improving fenofibrate's therapeutic efficacy.
Purpose of the Study:
- To formulate and characterize a microemulsion system for oral fenofibrate administration.
- To enhance the solubility and oral bioavailability of fenofibrate.
Main Methods:
- Preparation of various microemulsion formulations using oils, surfactants, and co-surfactants.
- Construction of pseudo-ternary phase diagrams to determine microemulsion regions.
- Characterization including drug solubility, droplet size, drug content, and physicochemical stability.
- Pharmacokinetic evaluation in dogs comparing microemulsions to a commercial capsule.
Main Results:
- An optimal microemulsion formulation (25% Capryol 90, 27.75% Cremophore EL, 9.25% Transcutol P, 38% water) achieved fenofibrate solubility of ~40.96 mg/mL.
- The microemulsion exhibited physicochemical stability with a mean droplet size of 32.5-41.7 nm.
- Pharmacokinetic studies in dogs showed significantly increased Cmax and AUC for fenofibrate microemulsions compared to Lipanthy capsules (p<0.05).
Conclusions:
- Fenofibrate microemulsions (FEN-MEs) demonstrated 1.63-fold and 1.30-fold higher oral bioavailability than the capsule.
- Microemulsion systems represent a promising strategy for enhancing the oral bioavailability of poorly soluble drugs like fenofibrate.
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