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Article Abstract
The use of tacrolimus (FK506) as an immunosuppressant is limited by its low aqueous solubility and bioavailability. The self-microemulsifying drug delivery system (SMEDDS) has successfully improved the solubility of FK506 in our previous study. This study focused on the solidification of liquid SMEDDS to capture the benefits of both liquid SMEDDS and solid dosage forms. Among several porous silica adsorbents evaluated, Aeroperl® 300 Pharma showed the best performance in terms of droplet size, in vitro dissolution, adsorbent-drug compatibility, and tabletabilities. And precoating the adsorbent with polyvinylpyrrolidone K30 resulted in complete drug release. Hydroxypropyl methylcellulose based matrix tablet was developed to achieve a sustained release of FK506. Differential scanning calorimetry and X-ray powder diffraction indicated that FK506 was present in a molecular or amorphous state in the solidified SMEDDS and tablets. In vivo pharmacokinetic studies showed that the self-prepared tablet had improved bioavailability (179.02%) compared to the marketed product Advagraf®. This study provided a promising candidate with improved dissolution and bioavailability for FK506 and a prospective platform for SMEDDS development.
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Article Synopsis
- - The study investigates improving the delivery of tacrolimus (FK506), an immunosuppressant, by using a self-microemulsifying drug delivery system (SMEDDS) to enhance its solubility and bioavailability.
- - Liquid SMEDDS was solidified using Aeroperl® 300 Pharma, which showed excellent performance in drug dissolution and compatibility, and achieving complete drug release was facilitated by precoating with polyvinylpyrrolidone K30.
- - The resulting hydroxypropyl methylcellulose-based tablets demonstrated a significant increase in bioavailability (179.02%) compared to the marketed formulation Advagraf®, suggesting a promising direction for future SMEDDS applications.